1
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Arora S, Gugulothu D. Recent Advances in Rotigotine Nanoformulations for Parkinson’s Disease Therapy. BIONANOSCIENCE 2025; 15:249. [DOI: 10.1007/s12668-025-01855-0] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Accepted: 02/05/2025] [Indexed: 04/02/2025]
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2
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Shalaby ES, Shalaby SI, Ismail SA. Advantages and therapeutic applications of different semisolids as vehicles for nano-based systems. Ther Deliv 2025:1-11. [PMID: 40118818 DOI: 10.1080/20415990.2025.2483151] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 10/04/2024] [Accepted: 03/19/2025] [Indexed: 03/24/2025] Open
Abstract
The aim of this review is to highlight the role of semisolid systems as vehicles for nanovesicles and nanoparticles. In general, nanotechnology plays a critical role in facilitating the delivery of therapeutic agents to their active sites, and several nanocarrier systems have been explored for the topical administration of active components. The major disadvantage of the prepared nanosystems is their low viscosity, which reduces the time needed for enough absorption and negatively affects their stability and bioavailability. The role of semisolid systems is to overcome this limitation. In conclusion, this review presents an updated summary of recent advances in the use of semisolids as vehicles for various nanosystems through comprehensive scrutiny of the types of semisolids and their advantages and their role in enhancing the absorption of nanoparticles and nanovesicles.
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Affiliation(s)
- Eman Samy Shalaby
- Pharmaceutical Technology Department, Pharmaceutical and Drug Industries Research Institute, National Research Centre, Giza, Egypt
| | - Samy I Shalaby
- Department of Animal Reproduction, Institute of Veterinary Researches, National Research Centre, Giza, Egypt
| | - Shaymaa A Ismail
- Department of Chemistry of Natural and Microbial Products, Pharmaceutical and Drug Industries Research Institute, National Research Centre, Giza, Egypt
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3
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Keshari R, Dewani M, Kaur N, Patel GK, Singh SK, Chandra P, Prasad R, Srivastava R. Lipid Nanocarriers as Precision Delivery Systems for Brain Tumors. Bioconjug Chem 2025; 36:347-366. [PMID: 39937652 DOI: 10.1021/acs.bioconjchem.5c00007] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [MESH Headings] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 02/14/2025]
Abstract
Brain tumors, particularly glioblastomas, represent the most complicated cancers to treat and manage due to their highly invasive nature and the protective barriers of the brain, including the blood-brain barrier (BBB). The efficacy of currently available treatments, viz., radiotherapy, chemotherapy, and immunotherapy, are frequently limited by major side effects, drug resistance, and restricted drug penetration into the brain. Lipid nanoparticles (LNPs) have emerged as a promising and targeted delivery system for brain tumors. Lipid nanocarriers have gained tremendous attention for brain tumor therapeutics due to multiple drug encapsulation abilities, controlled release, better biocompatibility, and ability to cross the BBB. Herein, a detailed analysis of the design, mechanisms, and therapeutic benefits of LNPs in brain tumor treatment is discussed. Moreover, we also discuss the safety issues and clinical developments of LNPs and their current and future challenges. Further, we also focused on the clinical transformation of LNPs in brain tumor therapy by eliminating side effects and engineering the LNPs to overcome the related biological barriers, which provide personalized, affordable, and low-risk treatment options.
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Affiliation(s)
- Roshan Keshari
- Department of Biosciences and Bioengineering, Indian Institute of Technology Bombay, Powai, Mumbai 400076, India
| | - Mahima Dewani
- Department of Biosciences and Bioengineering, Indian Institute of Technology Bombay, Powai, Mumbai 400076, India
| | - Navneet Kaur
- Department of Chemical and Biomedical Engineering, FAMU-FSU College of Engineering, Tallahassee, Florida 32310, United States
- National High Magnetic Field Laboratory, Tallahassee, Florida 32310, United States
| | - Girijesh Kumar Patel
- Cancer and Stem Cell Laboratory, Department of Biotechnology, Motilal Nehru National Institute of Technology Allahabad, Prayagraj, India-211004
| | - Sumit Kumar Singh
- School of Biochemical Engineering, Indian Institute of Technology (BHU) Varanasi, Uttar Pradesh 221005, India
| | - Pranjal Chandra
- School of Biochemical Engineering, Indian Institute of Technology (BHU) Varanasi, Uttar Pradesh 221005, India
| | - Rajendra Prasad
- School of Biochemical Engineering, Indian Institute of Technology (BHU) Varanasi, Uttar Pradesh 221005, India
| | - Rohit Srivastava
- Department of Biosciences and Bioengineering, Indian Institute of Technology Bombay, Powai, Mumbai 400076, India
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4
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Utpal BK, Sutradhar B, Zehravi M, Sweilam SH, Panigrahy UP, Urs D, Fatima AF, Nallasivan PK, Chhabra GS, Sayeed M, Alshehri MA, Rab SO, Khan SL, Emran TB. Polyphenols in wound healing: unlocking prospects with clinical applications. NAUNYN-SCHMIEDEBERG'S ARCHIVES OF PHARMACOLOGY 2025; 398:2459-2485. [PMID: 39453503 DOI: 10.1007/s00210-024-03538-1] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Subscribe] [Scholar Register] [Received: 09/01/2024] [Accepted: 10/10/2024] [Indexed: 10/26/2024]
Abstract
Wound healing is a multifaceted, complex process that factors like aging, metabolic diseases, and infections may influence. The potentiality of polyphenols, natural compounds, has shown anti-inflammatory and antimicrobial properties in promoting wound healing and their potential applications in wound management. The studies reviewed indicate that polyphenols have multiple mechanisms that promote wound healing. This involves enhancing antioxidant defenses, reducing oxidative stress, modulating inflammatory responses, improving healing times, reducing infection rates, and enhancing tissue regeneration in clinical trials and in vivo and in vitro studies. Polyphenols have been proven to be effective in managing hard-to-heal wounds, especially in diabetic and elderly populations. Polyphenols have shown significant benefits in promoting angiogenesis and stimulating collagen synthesis. Polyphenol treatment has been demonstrated to have therapeutic effects in wound healing and chronic wound management. Their ability to regulate key healing processes makes them suitable for new wound care products and treatments. Future research should enhance formulations and delivery methods to optimize polyphenols' bioavailability and therapeutic efficacy in wound management approaches.
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Affiliation(s)
- Biswajit Kumar Utpal
- Department of Pharmacy, Faculty of Health and Life Sciences, Daffodil International University, Dhaka, 1207, Bangladesh.
| | - Baishakhi Sutradhar
- Department of Microbiology, Gono University (Bishwabidyalay), Nolam, Mirzanagar, Savar, Dhaka, 1344, Bangladesh
| | - Mehrukh Zehravi
- Department of Clinical Pharmacy, College of Dentistry & Pharmacy, Buraydah Private Colleges, Buraydah, 51418, Saudi Arabia.
| | - Sherouk Hussein Sweilam
- Department of Pharmacognosy, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-Kharj, 11942, Saudi Arabia
- Department of Pharmacognosy, Faculty of Pharmacy, Egyptian Russian University, Cairo-Suez Road, Badr City, Cairo, 11829, Egypt
| | - Uttam Prasad Panigrahy
- Faculty of Pharmaceutical Science, Assam Down Town University, Gandhi Nagar, Sankar Madhab Path, Panikhaiti, Guwahati, Assam, 781026, India
| | - Deepadarshan Urs
- Inflammation Research Laboratory, Department of Studies & Research in Biochemistry, Mangalore University, Jnana Kaveri Post Graduate Campus, Kodagu, Karnataka, India
| | - Ayesha Farhath Fatima
- Department of Pharmaceutics, Anwarul Uloom College of Pharmacy, New Mallepally, Hyderabad, India
| | - P Kumar Nallasivan
- Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Karpagam Academy of Higher Education, Pollachi Main Road, Eachanari, Coimbatore, Tamilnadu, India
| | - Gurmeet Singh Chhabra
- Department Pharmaceutical Chemistry, Indore Institute of Pharmacy, Opposite Indian Institute of Management Rau, Pithampur Road, Indore, Madhya Pradesh, India
| | - Mohammed Sayeed
- Department of Pharmacology, School of Pharmacy, Anurag University, Venkatapur, Ghatkesar, Hyderabad, Telangana, India
| | - Mohammed Ali Alshehri
- Department of Biology, Faculty of Science, University of Tabuk, Tabuk, 71491, Saudi Arabia
| | - Safia Obaidur Rab
- Department of Clinical Laboratory Sciences, College of Applied Medical Science, King Khalid University, Abha, Saudi Arabia
| | - Sharuk L Khan
- Department of Pharmaceutical Chemistry, N.B.S. Institute of Pharmacy, Ausa, 413520, Maharashtra, India
| | - Talha Bin Emran
- Department of Pharmacy, Faculty of Health and Life Sciences, Daffodil International University, Dhaka, 1207, Bangladesh.
- Department of Pharmacy, BGC Trust University Bangladesh, Chittagong, 4381, Bangladesh.
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5
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Babaei A, Ebrahimi H, Shokouhi Kouchaksaraei T, Hamidi SM, Khazaeialiabad M, Siahposht-Khachaki A, Ebrahimnejad P. Development and optimization of curcumin-loaded solid lipid nanoparticles using Box-Behnken design and evaluation of its efficacy in modulating morphine-induced conditioned place preference: in vivo and in silico studies. J Drug Target 2025:1-22. [PMID: 39960800 DOI: 10.1080/1061186x.2025.2468758] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 09/29/2024] [Revised: 01/28/2025] [Accepted: 02/05/2025] [Indexed: 02/25/2025]
Abstract
Drug addiction, particularly to opioids like morphine, remains a pressing global health issue. Curcumin, a natural flavonoid, holds promise for treating neurological disorders, yet faces challenges, such as poor solubility and limited bioavailability across the blood-brain barrier. Solid lipid nanoparticles offer a solution, facilitating drug delivery to the brain. Using the Box-Behnken design, nanoparticles were optimised, yielding particles sized 152 nm, with a polydispersity index of 0.254, and an encapsulation efficiency of 70.74%. These nanoparticles enhance curcumin concentration and retention in brain tissue. Behavioural experiments using the conditioned place preference (CPP) test confirmed curcumin's impact on morphine addiction and its modulation of c-Fos gene expression. Pharmacological network analysis identified potential mechanisms of action, highlighting common targets in calcium and serotonin pathways. Docking simulations showed curcumin's affinity for proteins like 5HT1A, MAO-A, and TRPV1, relevant to addiction pathways. This research underscores the potential of curcumin-loaded solid lipid nanoparticles as a therapeutic approach for combating opioid addiction and neurological disorders.
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Affiliation(s)
- Amirhossein Babaei
- Pharmaceutical Sciences Research Center, Hemoglobinopathy Institute, Mazandaran University of Medical Sciences, Sari, Iran
- Department of Pharmaceutics, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran
| | - Hossein Ebrahimi
- Student Research Committee, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran
| | | | - Seyyed Mohammad Hamidi
- Student Research Committee, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran
| | | | - Ali Siahposht-Khachaki
- Immunogenetics Research Center, Department of Physiology, Faculty of Medicine, Mazandaran University of Medical Sciences, Sari, Iran
| | - Pedram Ebrahimnejad
- Pharmaceutical Sciences Research Center, Hemoglobinopathy Institute, Mazandaran University of Medical Sciences, Sari, Iran
- Department of Pharmaceutics, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran
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6
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Grzegorzewski J, Michalak M, Wołoszczuk M, Bulicz M, Majchrzak-Celińska A. Nanotherapy of Glioblastoma-Where Hope Grows. Int J Mol Sci 2025; 26:1814. [PMID: 40076445 PMCID: PMC11898975 DOI: 10.3390/ijms26051814] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 12/20/2024] [Revised: 02/08/2025] [Accepted: 02/17/2025] [Indexed: 03/14/2025] Open
Abstract
Localization in the central nervous system, diffuse growth, the presence of stem cells, and numerous resistance mechanisms, all make glioblastoma (GBM) an incurable tumor. The standard treatment of GBM consisting of surgery; radio- and chemotherapy with temozolomide provides insufficient therapeutic benefit and needs to be updated with effective modern solutions. One of the most promising and intensively explored therapeutic approaches against GBM is the use of nanotherapy. The first, and so far only, nanoparticle-based therapy approved for GBM treatment is NanoThermTM. It is based on iron oxide nanoparticles and the thermal ablation of the tumor with a magnetic field. Numerous other types of nanotherapies are being evaluated, including polymer and lipid-based nanoformulations, nanodiscs, dendrimers, and metallic, silica, or bioderived nanoparticles, among others. The advantages of these nanoscale drug carriers include improved penetration across the blood-brain barrier, targeted drug delivery, biocompatibility, and lower systemic toxicity, while major problems with their implementation involve scaling up their production and high costs. Nevertheless, taking all the impressive benefits of nanotherapies into consideration, it seems obvious that the combined effort of the scientific world will need to be taken to tackle these challenges and implement these novel therapies into clinics, giving hope that the battle against GBM can finally be won.
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Affiliation(s)
- Jan Grzegorzewski
- The Student Scientific Society of Poznan University of Medical Sciences, 60-806 Poznań, Poland; (J.G.); (M.M.); (M.W.); (M.B.)
- Department of Pharmaceutical Biochemistry, Poznan University of Medical Sciences, Rokietnicka 3, 60-806 Poznań, Poland
| | - Maciej Michalak
- The Student Scientific Society of Poznan University of Medical Sciences, 60-806 Poznań, Poland; (J.G.); (M.M.); (M.W.); (M.B.)
- Department of Pharmaceutical Biochemistry, Poznan University of Medical Sciences, Rokietnicka 3, 60-806 Poznań, Poland
| | - Maria Wołoszczuk
- The Student Scientific Society of Poznan University of Medical Sciences, 60-806 Poznań, Poland; (J.G.); (M.M.); (M.W.); (M.B.)
- Department of Pharmaceutical Biochemistry, Poznan University of Medical Sciences, Rokietnicka 3, 60-806 Poznań, Poland
| | - Magdalena Bulicz
- The Student Scientific Society of Poznan University of Medical Sciences, 60-806 Poznań, Poland; (J.G.); (M.M.); (M.W.); (M.B.)
- Department of Pharmaceutical Biochemistry, Poznan University of Medical Sciences, Rokietnicka 3, 60-806 Poznań, Poland
| | - Aleksandra Majchrzak-Celińska
- Department of Pharmaceutical Biochemistry, Poznan University of Medical Sciences, Rokietnicka 3, 60-806 Poznań, Poland
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7
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Svenskaya YI, Verkhovskii RA, Zaytsev SM, Lademann J, Genina EA. Current issues in optical monitoring of drug delivery via hair follicles. Adv Drug Deliv Rev 2025; 217:115477. [PMID: 39615632 DOI: 10.1016/j.addr.2024.115477] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 09/18/2024] [Revised: 11/05/2024] [Accepted: 11/22/2024] [Indexed: 12/09/2024]
Abstract
Drug delivery via hair follicles has attracted much research attention due to its potential to serve for both local and systemic therapeutic purposes. Recent studies on topical application of various particulate formulations have demonstrated a great role of this delivery route for targeting numerous cell populations located in skin and transporting the encapsulated drug molecules to the bloodstream. Despite a great promise of follicle-targeting carriers, their clinical implementation is very rare, mostly because of their poorer characterization compared to conventional topical dosage forms, such as ointments and creams, which have a history spanning over a century. Gathering as complete information as possible on the intrafollicular penetration depth, storage, degradation/metabolization profiles of such carriers and the release kinetics of drugs they contain, as well as their impact on skin health would significantly contribute to understanding the pros and cons of each carrier type and facilitate the selection of the most suitable candidates for clinical trials. Optical imaging and spectroscopic techniques are extensively applied to study dermal penetration of drugs. Current paper provides the state-of-the-art overview of techniques, which are used in optical monitoring of follicular drug delivery, with a special focus on non-invasive in vivo methods. It discusses key features, advantages and limitations of their use, as well as provide expert perspectives on future directions in this field.
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Affiliation(s)
| | | | - Sergey M Zaytsev
- CRAN UMR 7039, Université de Lorraine, Vandoeuvre-lès-Nancy, France
| | - Juergen Lademann
- Center of Experimental and Applied Cutaneous Physiology, Department of Dermatology, Venereology and Allergology, Charité-Universitätsmedizin Berlin, Berlin, Germany
| | - Elina A Genina
- Department of Optics and Biophotonics, Saratov State University, Saratov, Russia
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8
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Kushwaha P, Usmani S, Sufiyan M, Singh P. Innovating alopecia treatment: nanostructured lipid carriers as advanced delivery platforms. NAUNYN-SCHMIEDEBERG'S ARCHIVES OF PHARMACOLOGY 2025:10.1007/s00210-025-03784-x. [PMID: 39825967 DOI: 10.1007/s00210-025-03784-x] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Subscribe] [Scholar Register] [Received: 10/03/2024] [Accepted: 01/01/2025] [Indexed: 01/20/2025]
Abstract
Alopecia, a common dermatological condition, poses significant psychological and social challenges. Despite the availability of various treatments, their efficacy is often limited by poor bioavailability and delivery challenges. Nanostructured lipid carriers have emerged as promising advanced drug delivery systems for alopecia treatment due to their ability to encapsulate both hydrophilic and lipophilic compounds, enhancing their stability, solubility, and controlled release. This manuscript explores the potential of Nanostructured lipid carriers as innovative delivery platforms for alopecia therapeutics, focusing on their formulation, characterization, and application in topical treatments. The unique properties of Nanostructured lipid carriers, including their small size, biocompatibility, and ability to target specific skin layers, are discussed in relation to improving the penetration and therapeutic efficacy of active ingredients such as minoxidil, finasteride, and plant-derived compounds. Additionally, we highlight the role of Nanostructured lipid carriers in improving scalp penetration, reducing side effects, and offering a more efficient alternative to conventional treatments. The manuscript concludes with insights into future trends, challenges, and the clinical potential of Nanostructured lipid carriers-based formulations in revolutionizing alopecia treatment.
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Affiliation(s)
- Poonam Kushwaha
- Faculty of Pharmacy, Integral University, Lucknow, 226026, India.
| | - Shazia Usmani
- Faculty of Pharmacy, Integral University, Lucknow, 226026, India
| | - Mohd Sufiyan
- Faculty of Pharmacy, Integral University, Lucknow, 226026, India
| | - Priyanka Singh
- Faculty of Pharmacy, Integral University, Lucknow, 226026, India
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9
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Zazuli Z, Hartati R, Rowa CR, Asyarie S, Satrialdi. The Potential Application of Nanocarriers in Delivering Topical Antioxidants. Pharmaceuticals (Basel) 2025; 18:56. [PMID: 39861119 PMCID: PMC11769529 DOI: 10.3390/ph18010056] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 12/03/2024] [Revised: 12/28/2024] [Accepted: 01/03/2025] [Indexed: 01/27/2025] Open
Abstract
The imbalance in the production of reactive oxygen species (ROS) with endogenous antioxidant capacity leads to oxidative stress, which drives many disorders, especially in the skin. In such conditions, supplementing exogenous antioxidants may help the body prevent the negative effect of ROS. However, the skin, as the outermost barrier of the body, provides a perfect barricade, making the antioxidant delivery complicated. Several strategies have been developed to enhance the penetration of antioxidants through the skin, one of which is nanotechnology. This review focuses on utilizing several nanocarrier systems, including nanoemulsions, liposomes, solid lipid nanoparticles (SLNs), nanostructured lipid carriers (NLCs), and polymeric nanoparticles, for transporting antioxidants into the skin. We also reveal ROS formation in the skin and the role of antioxidant therapy, as well as the natural sources of antioxidants. Furthermore, we discuss the clinical application of topical antioxidant therapy concomitantly with the current status of using nanotechnology to deliver topical antioxidants. This review will accelerate the advancement of topical antioxidant therapy.
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Affiliation(s)
- Zulfan Zazuli
- Department of Pharmacology and Clinical Pharmacy, School of Pharmacy, Institut Teknologi Bandung, Bandung 40132, Indonesia;
| | - Rika Hartati
- Department of Pharmaceutical Biology, School of Pharmacy, Institut Teknologi Bandung, Bandung 40132, Indonesia;
| | - Cornelia Rosasepti Rowa
- Department of Pharmaceutics, School of Pharmacy, Institut Teknologi Bandung, Bandung 40132, Indonesia; (C.R.R.); (S.A.)
| | - Sukmadjaja Asyarie
- Department of Pharmaceutics, School of Pharmacy, Institut Teknologi Bandung, Bandung 40132, Indonesia; (C.R.R.); (S.A.)
| | - Satrialdi
- Department of Pharmaceutics, School of Pharmacy, Institut Teknologi Bandung, Bandung 40132, Indonesia; (C.R.R.); (S.A.)
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10
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Chaudhary K, Rajora A. Elevating Therapeutic Penetration: Innovations in Drug Delivery for Enhanced Permeation and Skin Cancer Management. Crit Rev Ther Drug Carrier Syst 2025; 42:1-34. [PMID: 39819462 DOI: 10.1615/critrevtherdrugcarriersyst.2024047670] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [MESH Headings] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 01/19/2025]
Abstract
Skin cancer stands as a challenging global health concern, necessitating innovative approaches to cure deficiencies within traditional therapeutic modalities. While conventional drug delivery methods through injection or oral administration have long prevailed, the emergence of topical drug administration presents a compelling alternative. The skin, aside from offering a swift and painless procedure, serves as a reservoir, maintaining drug efficacy over extended durations. This comprehensive review seeks to shed light on the potential of nanotechnology as a promising avenue for efficacious cancer treatment, with a particular emphasis on skin cancer. Additionally, it underscores the transdermal approach as a viable strategy for addressing various types of cancer. This work also explores into the delivery of peptides and proteins along with in-depth explanations of different delivery systems currently under investigation for localized skin cancer treatment. Furthermore, the review discusses the formidable challenges that must be surmounted before these innovations can find their way into clinical practice, offering a roadmap for future research and therapeutic development.
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Affiliation(s)
- Kajal Chaudhary
- Ram-Eesh Institute of Pharmacy, Knowledge Park I, Greater Noida, Uttar Pradesh 201306, India
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11
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Tiwari A, Tiwari V, Palaria B, Aslam R, Kumar M, Kumar N. Network pharmacology, molecular docking-driven, Qbd-Engineered antifungal in-situ gel loaded with voriconazole nanostructured lipid carriers. J Biomol Struct Dyn 2025; 43:305-324. [PMID: 37990482 DOI: 10.1080/07391102.2023.2280779] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 06/05/2023] [Accepted: 11/01/2023] [Indexed: 11/23/2023]
Abstract
Fungal infections (FIs) affect majority of the population, but the current treatments face challenges in terms of their effectiveness. This study focused on specific fungal targets, including dihydrofolate reductase (DHFR), acetohydroxy-acid synthase (AHAS), farnesyltransferase and endoglucanase. The docking studies were conducted with the drug voriconazole (VCZ), comparing it with Fluconazole (FCZ) and Amphotericin B (ATB) against 11 protein data bank (PDB) IDs (IDYR, 3NZB, 6DEQ, 1KS5, 7T0C, 1FY4, 5AJH, 7R79, 6TZ6 and 6IDY). Molecular dynamics (MD) analysis, including RMSD, RMSF, PCA and FEL, confirmed the stability of VCZ. The solubility of VCZ was a problem, so nanostructured lipid carriers (NLCs) were developed to improve ocular penetration. VCF5 was the optimized formulation by using 32 full factorial design. VCZF5-NLCs were the best in terms of nanoparticle size (126.6 nm), Zeta potential (33.5 mV), drug content (DC; 97.38 ± 0.210), encapsulation efficiency (EE; 88.01 ± 0.272) and extended drug release. The results of the ex-vivo corneal diffusion study indicate that VCZ-NLC-loaded in-situ gel (VCZ-NLC-IG3) exhibited DC of 88.25% and drug entrapment (DE) of 74.2%. The results of the zone of inhibition indicated that VCZ-NLC-IG3 had superior efficacy compared to ATB. Network pharmacology showed VCZ interacts with the genes which are responsible for fungus ergosterol biosynthesis, including lanosterol 14-alpha demethylase inhibitors (ERG11), ergosterol biosynthesis protein 5 (ERG5), dimethylallyltransferase 2 (DIT2), ketosynthase (KCN), methylsterol monooxygenase (MSMO1), lamin B receptor (LBR), squalene epoxidase (SQLE), 3-hydroxy-3-methylglutaryl-coenzyme A Reductase (MGCR), 3-hydroxy-3-methylglutaryl-coenzyme A Synthase (HMGCS) and 3-keto-steroid reductase (HSD17B7). In conclusion, the optimized VCZ-loaded NLCs present a promising approach to treat ocular FIs.Communicated by Ramaswamy H. Sarma.
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Affiliation(s)
- Abhishek Tiwari
- Department of Pharmacy, Pharmacy Academy, IFTM University, Moradabad, India
| | - Varsha Tiwari
- Department of Pharmacy, Pharmacy Academy, IFTM University, Moradabad, India
| | - Binita Palaria
- Department of Pharmacy, Devsthali Vidyapeeth College of Pharmacy, Rudrapur, India
| | - Ramsha Aslam
- Department of Pharmacy, Devsthali Vidyapeeth College of Pharmacy, Rudrapur, India
| | - Manish Kumar
- School of Pharmaceutical Sciences, C.T. University, Ludhiana, India
| | - Neeraj Kumar
- Department of Pharmaceutical Chemistry, Bhupal Nobles' College of Pharmacy, Bhupal Nobles' University, Udaipur, India
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12
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Mukhopadhyay B, Singh S, Singh A. Utilizing nanomaterials for cancer treatment and diagnosis: an overview. DISCOVER NANO 2024; 19:215. [PMID: 39718700 DOI: 10.1186/s11671-024-04128-z] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Subscribe] [Scholar Register] [Received: 04/16/2024] [Accepted: 10/14/2024] [Indexed: 12/25/2024]
Abstract
Cancer is a deadly disease with complex pathophysiological nature and is the leading cause of death worldwide. Traditional diagnosis methods often detect cancer at a considerably critical stage and the conventional methods of treatment like chemotherapy, radiation therapy, targeted therapy, and immunotherapy have several limitations, multidrug resistance, cytotoxicity, and lack of specificity are a few examples. These pose substantial challenge for effective and favourable cancer treatment. The advent of nanotechnology has revolutionized the face of cancer diagnosis and treatment. Nanoparticles, which have a size range of 1-100 nm, are biocompatible and have special optical, magnetic, and electrical capabilities, less toxic, more stable, exhibit permeability and retention effect, and are used for precise targeting. There are several classes of nanoparticles each having their own sets of unique properties. NPs have played an important role in the drug delivery system, overcoming the multi-drug resistance, reducing the side-effects as seen in conventional therapeutic methods and hence able to solve the limitations of conventional methods of diagnosis and treatment. This review discusses the four major classes of nanoparticles (Lipid based NPs, Carbon NPs and Metallic NPs and Polymeric NPs): their discovery and introduction in medical field, unique properties and characteristics, advantages and disadvantages, sub-categories and characteristics of these categories, major area of application in Cancer diagnosis and treatment, and latest methodologies where these are used in cancer treatment.
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Affiliation(s)
- Bageesha Mukhopadhyay
- Department of Biomedical Engineering, School of Bioengineering & Biosciences, Lovely Professional University, Phagwara, Punjab, 144001, India
| | - Sudhakar Singh
- Department of Biomedical Engineering, School of Bioengineering & Biosciences, Lovely Professional University, Phagwara, Punjab, 144001, India
| | - Avtar Singh
- School of Electrical Engineering and Computing (SoEEC), Adama Science and Technology University (AS-TU), 1888, Adama, Ethiopia.
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13
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Ibrahim M, Fathalla Z, Fatease AA, Alamri AH, Abdelkader H. Breast cancer epidemiology, diagnostic barriers, and contemporary trends in breast nanotheranostics and mechanisms of targeting. Expert Opin Drug Deliv 2024; 21:1735-1754. [PMID: 39361257 DOI: 10.1080/17425247.2024.2412823] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 10/23/2023] [Accepted: 10/01/2024] [Indexed: 10/08/2024]
Abstract
INTRODUCTION Breast cancer is one of the main causes of mortality in women globally. Early and accurate diagnosis represents a milestone in cancer management. Several breast cancer diagnostic agents are available. Many chemotherapeutic agents in conventional dosage forms are approved; nevertheless, they lack cancer cell specificity, resulting in improper treatment and undesirable side effects. Recently, nanotheranostics has emerged as a new paradigm to achieve safe and effective cancer diagnosis and management. AREA COVERED This review provides insight into breast cancer epidemiology, barriers hindering the early diagnosis, and effective delivery of chemotherapeutics. Also, conventional diagnostic agents and recent nanotheranostic platforms have been used in breast cancer. In addition, mechanisms of cancer cell targeting and nano-carrier surface functionalization as an effective approach for chemotherapeutic targeting were reviewed along with future perspectives. EXPERT OPINION We proposed that modified nano-carriers may provide an efficacious approach for breast cancer drug targeting. These nanotheranostics need more clinical evaluations to confirm their efficacy in cancer management. In addition, we recommend the use of artificial intelligence (AI) as a promising approach for early and efficient assessment of breast lesions. AI allows better interpretation and analysis of nanotheranostic data, which minimizes misdiagnosis and avoids the belated intervention of health care providers.
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Affiliation(s)
- Mohamed Ibrahim
- Department of Pharmaceutics, Faculty of Pharmacy, Minia University, Minia, Egypt
| | - Zeinab Fathalla
- Department of Pharmaceutics, Faculty of Pharmacy, Minia University, Minia, Egypt
| | - Adel Al Fatease
- Department of Pharmaceutics, College of Pharmacy, King Khalid University, Abha, Saudi Arabia
| | - Ali H Alamri
- Department of Pharmaceutics, College of Pharmacy, King Khalid University, Abha, Saudi Arabia
| | - Hamdy Abdelkader
- Department of Pharmaceutics, College of Pharmacy, King Khalid University, Abha, Saudi Arabia
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14
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Buya AB, Mahlangu P, Witika BA. From lab to industrial development of lipid nanocarriers using quality by design approach. Int J Pharm X 2024; 8:100266. [PMID: 39050378 PMCID: PMC11268122 DOI: 10.1016/j.ijpx.2024.100266] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 03/30/2024] [Revised: 06/25/2024] [Accepted: 06/29/2024] [Indexed: 07/27/2024] Open
Abstract
Lipid nanocarriers have attracted a great deal of interest in the delivery of therapeutic molecules. Despite their many advantages, compliance with quality standards and reproducibility requirements still constrain their industrial production. The relatively high failure rate in lipid nanocarrier research and development can be attributed to immature bottom-up manufacturing practices, leading to suboptimal control of quality attributes. Recently, the pharmaceutical industry has moved toward quality-driven manufacturing, emphasizing the integration of product and process development through the principles of quality by design. Quality by design in the pharmaceutical industry involves a thorough understanding of the quality profile of the target product and involves an assessment of potential risks during the design and development phases of pharmaceutical dosage forms. By identifying essential quality characteristics, such as the active ingredients, excipients and manufacturing processes used during research and development, it becomes possible to effectively control these aspects throughout the life cycle of the drug. Successful commercialization of lipid nanocarriers can be achieved if large-scale challenges are addressed using the QbD approach. QbD has become an essential tool because of its advantages in improving processes and product quality. The application of the QbD approach to the development of lipid nanocarriers can provide comprehensive and remarkable knowledge enabling the manufacture of high-quality products with a high degree of regulatory flexibility. This article reviews the basic considerations of QbD and its application in the laboratory and large-scale development of lipid nanocarriers. Furthermore, it provides forward-looking guidance for the industrial production of lipid nanocarriers using the QbD approach.
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Affiliation(s)
- Aristote B. Buya
- Centre de Recherche en Sciences Humaines (CRESH), Ministère de la Recherche Scientifique et Innovation Technologique, Kinshasa XI, B.P. 212, Democratic Republic of the Congo
- University of Kinshasa, Faculty of Pharmaceutical Sciences, BP 212 Kinshasa XI, Democratic Republic of the Congo
| | - Phindile Mahlangu
- Department of Pharmaceutical Science, School of Pharmacy, Sefako Makgatho Health Sciences University, Pretoria, South Africa
| | - Bwalya A. Witika
- Department of Pharmaceutical Science, School of Pharmacy, Sefako Makgatho Health Sciences University, Pretoria, South Africa
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15
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Favas R, Almeida H, Peixoto AF, Ferreira D, Silva AC. Advances in Encapsulating Marine Bioactive Compounds Using Nanostructured Lipid Carriers (NLCs) and Solid Lipid Nanoparticles (SLNs) for Health Applications. Pharmaceutics 2024; 16:1517. [PMID: 39771497 PMCID: PMC11728729 DOI: 10.3390/pharmaceutics16121517] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [Grants] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 10/18/2024] [Revised: 11/13/2024] [Accepted: 11/20/2024] [Indexed: 01/16/2025] Open
Abstract
As life expectancy rises and modern lifestyles improve, there is an increasing focus on health, disease prevention, and enhancing physical appearance. Consumers are more aware of the benefits of natural ingredients in healthcare products while also being mindful of sustainability challenges. Consequently, marine bioactive compounds have gained popularity as ingredients in cosmetics and food supplements due to their diverse beneficial properties. Nonetheless, the use of some of these compounds is restricted by their low stability and poor aqueous solubility, necessitating solutions to overcome these limitations. In this context, lipid nanoparticles, such as solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs), have been investigated for their potential to protect and improve the absorption of molecules through various routes, including oral and cutaneous. Numerous studies have shown that nanoencapsulating these compounds and incorporating them into cosmetics and food supplements can be effective. However, this application remains unregulated at the global level and is not currently addressed by existing legislation. Additional in vivo studies in both animals and humans are necessary to fully assess safety concerns.
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Affiliation(s)
- Rita Favas
- UCIBIO (Applied Molecular Biosciences Unit), Laboratory of Pharmaceutical Technology, Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal
- Associate Laboratory i4HB Institute for Health and Bioeconomy, Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal
| | - Hugo Almeida
- UCIBIO (Applied Molecular Biosciences Unit), Laboratory of Pharmaceutical Technology, Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal
- Associate Laboratory i4HB Institute for Health and Bioeconomy, Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal
- Mesosystem Investigação & Investimentos by Spinpark, 4805-017 Guimarães, Portugal
| | - Andreia F. Peixoto
- LAQV-REQUIMTE (Associated Laboratory for Green Chemistry of the Network of Chemistry and Technology), Departamento de Química e Bioquímica, Faculdade de Ciências, Universidade do Porto, 4169-007 Porto, Portugal
| | - Domingos Ferreira
- UCIBIO (Applied Molecular Biosciences Unit), Laboratory of Pharmaceutical Technology, Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal
- Associate Laboratory i4HB Institute for Health and Bioeconomy, Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal
| | - Ana C. Silva
- UCIBIO (Applied Molecular Biosciences Unit), Laboratory of Pharmaceutical Technology, Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal
- Associate Laboratory i4HB Institute for Health and Bioeconomy, Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal
- FP-BHS (Biomedical and Health Sciences Research Unit), FP-I3ID (Instituto de Investigação, Inovação e Desenvolvimento), Faculty of Health Sciences, University Fernando Pessoa, 4249-004 Porto, Portugal
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16
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Abd-Elrasheed E, Fahim SA, Nessim CK, El-Helaly SN. Innovative anti-proliferative effect of the antiviral favipiravir against MCF-7 breast cancer cells using green nanoemulsion and eco-friendly assessment tools. Sci Rep 2024; 14:27939. [PMID: 39537766 PMCID: PMC11561084 DOI: 10.1038/s41598-024-78422-2] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Grants] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 03/15/2024] [Accepted: 10/30/2024] [Indexed: 11/16/2024] Open
Abstract
Telomerase enzyme prevents telomere shortening during division, having human telomerase reverse transcriptase (hTERT) as its catalytic subunit. Favipiravir (FAV), an RNA-dependent RNA polymerases inhibitor, shared structural similarity with hTERT and thus assumed to have cytotoxic effect on cancer cells, in addition to its prophylactic effect to immunocompromised cancer patients. Nanoemulsion (NE) is a potential tumor cells targeting delivery system, thereby enhancing therapeutic efficacy at the intended site, mitigating systemic toxicity, and overcoming multidrug resistance. The objective of this study is to develop a green FAV nanoemulsion (FNE) that is environmentally friendly and safe for patients, while aiming to enhance its cytotoxic effects. The study also highlights the environmental sustainability of the developed RP-HPLC method and assesses its greenness impact. The FNE formulation underwent thermodynamic stability testing and invitro characterization. Greenness was assessed using advanced selected tools like the Analytical Eco-Scale (AES), Analytical Greenness Metric for Sample Preparation (AGREEprep), and green analytical procedure index (GAPI). The cytotoxic potential of FNE was screened against MCF-7 breast cancer and Vero normal cell lines using SRB assay. Stable and ecofriendly FNE was formulated having a particle size (PS) of 25.29 ± 0.57 nm and a zeta potential of -6.79 ± 5.52 mV. The cytotoxic effect of FNE on MCF-7 cells was more potent than FAV with lower IC50 while FNE showed non-toxic effect on VERO normal cell line. Therefore, the FAV nanoemulsion formulation showed targeted cytotoxicity on MCF-7 cells while being non-toxic on normal Vero cells.
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Affiliation(s)
- Eman Abd-Elrasheed
- Department of Pharmaceutics and Industrial pharmacy, Pharmacy Program, St. Petersburg University, Cairo, Egypt
| | - Sally A Fahim
- Department of Biochemistry, School of Pharmacy, Newgiza University (NGU), Newgiza, km 22 Cairo-Alexandria Desert Road, Giza, 12577, Egypt.
| | - Christine K Nessim
- Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ahram Canadian University, 6th October City, Cairo, Egypt
| | - Sara Nageeb El-Helaly
- Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt
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17
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Gerardos AM, Pispas S. Double Hydrophilic Hyperbranched Copolymer-Based Lipomer Nanoparticles: Copolymer Synthesis and Co-Assembly Studies. Polymers (Basel) 2024; 16:3129. [PMID: 39599220 PMCID: PMC11598649 DOI: 10.3390/polym16223129] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 10/09/2024] [Revised: 11/01/2024] [Accepted: 11/04/2024] [Indexed: 11/29/2024] Open
Abstract
Double hydrophilic, random, hyperbranched copolymers were synthesized via reversible addition-fragmentation chain transfer (RAFT) polymerization of oligo(ethylene glycol) methyl ether methacrylate (OEGMA) and 2-(dimethylamino)ethyl methacrylate (DMAEMA) utilizing ethylene glycol dimethacrylate (EGDMA) as the branching agent. The resulting copolymers were characterized in terms of their molecular weight and dispersity using size exclusion chromatography (SEC), and their chemical structure was confirmed using FT-IR and 1H-NMR spectroscopy techniques. The choice of the two hydrophilic blocks and the design of the macromolecular structure allowed the formation of self-assembled nanoparticles, partially due to the pH-responsive character of the DMAEMA segments and their interaction with -COOH end groups remaining from the chain transfer agent. The copolymers showed pH-responsive properties, mainly due to the protonation-deprotonation equilibria of the DMAEMA segments. Subsequently, a nanoscopic polymer-lipid (lipomer) mixed system was formulated by complexing the synthesized copolymers with cosmetic amphiphilic emulsifiers, specifically glyceryl stearate (GS) and glyceryl stearate citrate (GSC). This study aims to show that developing lipid-polymer hybrid nanoparticles can effectively address the limitations of both liposomes and polymeric nanoparticles. The effects of varying the ionic strength and pH on stimuli-sensitive polymeric and mixed polymer-lipid nanostructures were thoroughly investigated. To achieve this, the structural properties of the hybrid nanoparticles were comprehensively characterized using physicochemical techniques providing insights into their size distribution and stability.
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Affiliation(s)
- Angelica Maria Gerardos
- Theoretical and Physical Chemistry Institute, National Hellenic Research Foundation, 48 Vassileos Constantinou Avenue, 11635 Athens, Greece;
- Department of Chemistry, National and Kapodistrian University of Athens, Panepistimiopolis Zografou, 15771 Athens, Greece
| | - Stergios Pispas
- Theoretical and Physical Chemistry Institute, National Hellenic Research Foundation, 48 Vassileos Constantinou Avenue, 11635 Athens, Greece;
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18
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Gomes Daré R, Beatriz Chieco Costa A, Silva Martins T, Lopes LB. Simvastatin and adenosine-co-loaded nanostructured lipid carriers for wound healing: Development, characterization and cell-based investigation. Eur J Pharm Biopharm 2024:114533. [PMID: 39414092 DOI: 10.1016/j.ejpb.2024.114533] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 08/13/2024] [Revised: 09/29/2024] [Accepted: 10/12/2024] [Indexed: 10/18/2024]
Abstract
Chronic wounds represent a significant global health burden, characterized by delayed skin healing and associated comorbidities. The present study aimed to develop nanostructured lipid carriers (NLCs) as a topical delivery system for the co-administration of simvastatin and adenosine to address chronic wound management. The rationale behind the co-delivery approach was to mitigate the cytotoxicity associated with high-dose simvastatin, while preserving its therapeutic benefits through a potential synergistic or additive effect. A significant challenge in the development of these NLCs was the encapsulation of the highly hydrophilic adenosine within the hydrophobic lipid matrix. The NLCs were prepared using a hot homogenization-sonication method with a double emulsion technique and optimized through a series of formulation trials, employing various surfactants, solid and liquid lipids, to achieve efficient drug encapsulation, particularly for the hydrophilic adenosine. Optimized formulations F5- and F10-S/A 0.6 %/2 % (containing 0.6 % simvastatin and 2 % adenosine), exhibited promising physicochemical properties. The main difference was the liquid lipid used: F5 containing Miglyol 810 N, while F10 Capmul MCM C-8. Both formulations displayed a mean particle size below 230 nm, a polydispersity index (PDI) of approximately 0.2, and a zeta potential of around -22 mV. While simvastatin association efficiency (AE) was nearly 100 %, adenosine AE was higher for F10 (24 %), compared to F5 (13.5 %). F5 demonstrated superior stability compared to F10, maintaining consistent particle size and PDI over a 60-day period. Formulation F5 also demonstrated superior cell-based in vitro performance compared to F10, with higher cell viability (MTT assay), greater cell proliferation induction (SRB assay), and enhanced cell proliferation and migration in the wound-scratch assay. While F10 displayed higher adenosine AE, F5 excelled in terms of stability and biological activity. The slightly increase in intracellular reactive oxygen species levels observed with F5 may contribute to its enhanced proliferative effects. In-depth characterization revealed that F5 comprised spherical nanoparticles, and thermal analysis indicated no significant changes in the nanocarrier structure upon drug encapsulation. Additionally, ex vivo permeability study demonstrated superior skin retention of both simvastatin and adenosine for F5 compared to an emulsion control. Overall, the F5 nanocarrier demonstrated suitable physicochemical properties, cellular biocompatibility, induction of cell proliferation and migration events, and drug retention capacity in the skin layers, indicating its potential as a promising topical treatment for difficult-to-heal wounds.
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Affiliation(s)
- Regina Gomes Daré
- Institute of Biomedical Sciences, University of São Paulo, 1524 Professor Lineu Prestes Avenue, 05508-000 São Paulo, SP, Brazil.
| | - Ana Beatriz Chieco Costa
- Institute of Biomedical Sciences, University of São Paulo, 1524 Professor Lineu Prestes Avenue, 05508-000 São Paulo, SP, Brazil
| | - Tereza Silva Martins
- Institute of Environmental, Chemical and Pharmaceutical Sciences, Federal University of São Paulo, 210 São Nicolau Street, 09913-030 Diadema, SP, Brazil
| | - Luciana B Lopes
- Institute of Biomedical Sciences, University of São Paulo, 1524 Professor Lineu Prestes Avenue, 05508-000 São Paulo, SP, Brazil.
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19
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Xu F, Xu S, Yang L, Qu A, Li D, Yu M, Wu Y, Zheng S, Ruan X, Wang Q. Preparing a Phytosome for Promoting Delivery Efficiency and Biological Activities of Methyl Jasmonate-Treated Dendropanax morbifera Adventitious Root Extract (DMARE). Biomolecules 2024; 14:1273. [PMID: 39456206 PMCID: PMC11505992 DOI: 10.3390/biom14101273] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Grants] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 08/09/2024] [Revised: 09/12/2024] [Accepted: 09/23/2024] [Indexed: 10/28/2024] Open
Abstract
(1) Background: Methyl jasmonate-treated D. morbifera adventitious root extract (MeJA-DMARE), enriched with phenolics, has enhanced bioactivities. However, phenolics possess low stability and bioavailability. Substantial evidence indicates that plant extract-phospholipid complex assemblies, known as phytosomes, represent an innovative drug delivery system. (2) Methods: The phytosome complex was created by combining MeJA-DMARE with Soy-L-α-phosphatidylcholine (PC) using three different ratios through two distinct methods (co-solvency method: A1, A2, and A3; thin-layer film method: B1, B2, and B3). (3) Results: Initial evaluation based on UV-Vis, entrapment efficiency (EE%), and loading content (LC%) indicated that B2 exhibited the highest EE% (79.98 ± 1.45) and LC% (69.17 ± 0.14). The phytosome displayed a spherical morphology with a particle size of 210 nm, a notably low polydispersity index of 0.16, and a superior zeta potential value at -25.19 mV. The synthesized phytosome exhibited superior anti-inflammatory activities by inhibiting NO and ROS production (reduced to 8.9% and 55.1% at 250 μg/mL) in RAW cells and adjusting the expression of related inflammatory cytokines; they also slowed lung tumor cell migration (only 2.3% of A549 cells migrated after treatment with phytosomes at 250 μg/mL), promoting ROS generation in A549 cell lines (123.7% compared to control) and stimulating apoptosis of lung cancer-related genes. (4) Conclusions: In conclusion, the MeJA-DMARE phytosome offers stable, economically efficient, and environmentally friendly nanoparticles with superior inflammation and lung tumor inhibition properties. Thus, the MeJA-DMARE phytosome holds promise as an applicable and favorable creation for drug delivery and lung cancer treatment.
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Affiliation(s)
- Fengjiao Xu
- School of Biological and Chemical Engineering, NingboTech University, Ningbo 315100, China; (F.X.); (L.Y.); (A.Q.); (Y.W.)
- State Key Laboratory of Plant Environmental Resilience, College of Life Sciences, Zhejiang University, Hangzhou 310058, China;
| | - Shican Xu
- National Key Laboratory of Cotton Bio-Breeding and Integrated Utilization, College of Agriculture, Henan University, Kaifeng 475004, China;
| | - Li Yang
- School of Biological and Chemical Engineering, NingboTech University, Ningbo 315100, China; (F.X.); (L.Y.); (A.Q.); (Y.W.)
| | - Aili Qu
- School of Biological and Chemical Engineering, NingboTech University, Ningbo 315100, China; (F.X.); (L.Y.); (A.Q.); (Y.W.)
| | - Dongbin Li
- Ningbo Forest Farm, Ningbo Bureau of Natural Resources and Planning, Ningbo 315440, China; (D.L.); (M.Y.)
| | - Minfen Yu
- Ningbo Forest Farm, Ningbo Bureau of Natural Resources and Planning, Ningbo 315440, China; (D.L.); (M.Y.)
| | - Yongping Wu
- School of Biological and Chemical Engineering, NingboTech University, Ningbo 315100, China; (F.X.); (L.Y.); (A.Q.); (Y.W.)
| | - Shaojian Zheng
- State Key Laboratory of Plant Environmental Resilience, College of Life Sciences, Zhejiang University, Hangzhou 310058, China;
| | - Xiao Ruan
- School of Biological and Chemical Engineering, NingboTech University, Ningbo 315100, China; (F.X.); (L.Y.); (A.Q.); (Y.W.)
| | - Qiang Wang
- School of Biological and Chemical Engineering, NingboTech University, Ningbo 315100, China; (F.X.); (L.Y.); (A.Q.); (Y.W.)
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20
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Tawfeek HM, Mekkawy AI, Abdelatif AAH, Aldosari BN, Mohammed-Saeid WA, Elnaggar MG. Intranasal delivery of sulpiride nanostructured lipid carrier to central nervous system; in vitro characterization and in vivo study. Pharm Dev Technol 2024; 29:841-854. [PMID: 39264666 DOI: 10.1080/10837450.2024.2404034] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 05/09/2024] [Revised: 08/05/2024] [Accepted: 09/10/2024] [Indexed: 09/13/2024]
Abstract
The low and erratic oral absorption of sulpiride (SUL) a dopaminergic receptor antagonist, and its P-glycoprotein efflux in the gastrointestinal tract restricted its oral route for central nervous system disorders. An intranasal formulation was formulated based on nanostructured lipid carrier to tackle these obstacles and deliver SUL directly to the brain. Sulipride-loaded nanostructured lipid carrier (SUL-NLC) was prepared using compritol®888 ATO and different types of liquid lipids and emulsifiers. SUL-NLCs were characterized for their particle size, charge, and encapsulation efficiency. Morphology and compatibility with other NLC excipients were also studied. Moreover, SUL in vitro release, nanodispersion stability, in vivo performance and SUL pharmacokinetics were investigated. Results delineates that SUL-NLC have a particle size ranging from 366.2 ± 62.1 to 640.4 ± 50.2 nm and encapsulation efficiency of 75.5 ± 1.5%. SUL showed a sustained release pattern over 24 h and maintained its physical stability for three months. Intranasal SUL-NLC showed a significantly (p < 0.01) higher SUL brain concentration than that found in plasma after oral administration of commercial SUL product with 4.47-fold increase in the relative bioavailability. SUL-NLCs as a nose to brain approach is a promising formulation for enhancing the SUL bioavailability and efficient management of neurological disorders.
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Affiliation(s)
- Hesham M Tawfeek
- Department of Industrial Pharmacy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
| | - Aml I Mekkawy
- Department of Pharmaceutics and Clinical Pharmacy, Faculty of Pharmacy, Sohag University, Sohag, Egypt
| | - Ahmed A H Abdelatif
- Department of Pharmaceutics, College of Pharmacy, Qassim University, Buraydah, Saudi Arabia
| | - Basmah N Aldosari
- Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia
| | - Waleed A Mohammed-Saeid
- Department of Pharmaceutics and Pharmaceutical Industries, College of Pharmacy, Taibah University, Madinah, Saudi Arabia
| | - Marwa G Elnaggar
- Department of Industrial Pharmacy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
- Department of Industrial and Molecular Pharmaceutics, Purdue University, West Lafayette, IN, USA
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21
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Deepak V, El-Balawi L, Harris LK. Placental Drug Delivery to Treat Pre-Eclampsia and Fetal Growth Restriction. SMALL (WEINHEIM AN DER BERGSTRASSE, GERMANY) 2024; 20:e2311165. [PMID: 38745536 DOI: 10.1002/smll.202311165] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Grants] [Track Full Text] [Subscribe] [Scholar Register] [Received: 12/01/2023] [Revised: 04/23/2024] [Indexed: 05/16/2024]
Abstract
Pre-eclampsia and fetal growth restriction (FGR) continue to cause unacceptably high levels of morbidity and mortality, despite significant pharmaceutical and technological advances in other disease areas. The recent pandemic has also impacted obstetric care, as COVID-19 infection increases the risk of poor pregnancy outcomes. This review explores the reasons why it lacks effective drug treatments for the placental dysfunction that underlies many common obstetric conditions and describes how nanomedicines and targeted drug delivery approaches may provide the solution to the current drug drought. The ever-increasing range of biocompatible nanoparticle formulations available is now making it possible to selectively deliver drugs to uterine and placental tissues and dramatically limit fetal drug transfer. Formulations that are refractory to placental uptake offer the possibility of retaining drugs within the maternal circulation, allowing pregnant individuals to take medicines previously considered too harmful to the developing baby. Liposomes, ionizable lipid nanoparticles, polymeric nanoparticles, and adenoviral vectors have all been used to create efficacious drug delivery systems for use in pregnancy, although each approach offers distinct advantages and limitations. It is imperative that recent advances continue to be built upon and that there is an overdue investment of intellectual and financial capital in this field.
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Affiliation(s)
- Venkataraman Deepak
- Maternal and Fetal Health Research Centre, Division of Developmental Biology and Medicine, Faculty of Biology, Medicine and Health, The University of Manchester, Oxford Road, Manchester, M13 9WL, UK
- St Mary's Hospital, Manchester Academic Health Science Centre, Manchester University NHS Foundation Trust, Manchester, M13 9WL, UK
| | - Lujain El-Balawi
- Division of Pharmacy and Optometry, Faculty of Biology, Medicine and Health, The University of Manchester, Manchester, M13 9PL, UK
| | - Lynda K Harris
- Maternal and Fetal Health Research Centre, Division of Developmental Biology and Medicine, Faculty of Biology, Medicine and Health, The University of Manchester, Oxford Road, Manchester, M13 9WL, UK
- St Mary's Hospital, Manchester Academic Health Science Centre, Manchester University NHS Foundation Trust, Manchester, M13 9WL, UK
- Division of Pharmacy and Optometry, Faculty of Biology, Medicine and Health, The University of Manchester, Manchester, M13 9PL, UK
- Olson Center for Women's Health, Department of Obstetrics and Gynecology, University of Nebraska Medical Center, Omaha, NE, 68198, USA
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22
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Song Q, Li J, Li T, Li H. Nanomaterials that Aid in the Diagnosis and Treatment of Alzheimer's Disease, Resolving Blood-Brain Barrier Crossing Ability. ADVANCED SCIENCE (WEINHEIM, BADEN-WURTTEMBERG, GERMANY) 2024; 11:e2403473. [PMID: 39101248 PMCID: PMC11481234 DOI: 10.1002/advs.202403473] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Grants] [Track Full Text] [Subscribe] [Scholar Register] [Received: 05/06/2024] [Revised: 07/04/2024] [Indexed: 08/06/2024]
Abstract
As a form of dementia, Alzheimer's disease (AD) suffers from no efficacious cure, yet AD treatment is still imperative, as it ameliorates the symptoms or prevents it from deteriorating or maintains the current status to the longest extent. The human brain is the most sensitive and complex organ in the body, which is protected by the blood-brain barrier (BBB). This yet induces the difficulty in curing AD as the drugs or nanomaterials that are much inhibited from reaching the lesion site. Thus, BBB crossing capability of drug delivery system remains a significant challenge in the development of neurological therapeutics. Fortunately, nano-enabled delivery systems possess promising potential to achieve multifunctional diagnostics/therapeutics against various targets of AD owing to their intriguing advantages of nanocarriers, including easy multifunctionalization on surfaces, high surface-to-volume ratio with large payloads, and potential ability to cross the BBB, making them capable of conquering the limitations of conventional drug candidates. This review, which focuses on the BBB crossing ability of the multifunctional nanomaterials in AD diagnosis and treatment, will provide an insightful vision that is conducive to the development of AD-related nanomaterials.
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Affiliation(s)
- Qingting Song
- Department of ChemistryThe Chinese University of Hong KongHong KongChina
| | - Junyou Li
- Department of ChemistryThe Chinese University of Hong KongHong KongChina
| | - Ting Li
- Department of ChemistryThe Chinese University of Hong KongHong KongChina
| | - Hung‐Wing Li
- Department of ChemistryThe Chinese University of Hong KongHong KongChina
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23
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Wang Y, Liu C, Fang C, Peng Q, Qin W, Yan X, Zhang K. Engineered Cancer Nanovaccines: A New Frontier in Cancer Therapy. NANO-MICRO LETTERS 2024; 17:30. [PMID: 39347944 PMCID: PMC11442722 DOI: 10.1007/s40820-024-01533-y] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Subscribe] [Scholar Register] [Received: 06/25/2024] [Accepted: 09/08/2024] [Indexed: 10/01/2024]
Abstract
Vaccinations are essential for preventing and treating disease, especially cancer nanovaccines, which have gained considerable interest recently for their strong anti-tumor immune capabilities. Vaccines can prompt the immune system to generate antibodies and activate various immune cells, leading to a response against tumor tissues and reducing the negative effects and recurrence risks of traditional chemotherapy and surgery. To enhance the flexibility and targeting of vaccines, nanovaccines utilize nanotechnology to encapsulate or carry antigens at the nanoscale level, enabling more controlled and precise drug delivery to enhance immune responses. Cancer nanovaccines function by encapsulating tumor-specific antigens or tumor-associated antigens within nanomaterials. The small size of these nanomaterials allows for precise targeting of T cells, dendritic cells, or cancer cells, thereby eliciting a more potent anti-tumor response. In this paper, we focus on the classification of carriers for cancer nanovaccines, the roles of different target cells, and clinically tested cancer nanovaccines, discussing strategies for effectively inducing cytotoxic T lymphocytes responses and optimizing antigen presentation, while also looking ahead to the translational challenges of moving from animal experiments to clinical trials.
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Affiliation(s)
- Yijie Wang
- Central Laboratory and Department of Medical Ultrasound, Sichuan Academy of Medical Sciences, Sichuan Provincial People's Hospital, School of Medicine, University of Electronic Science and Technology of China, No. 32, West Second Section, First Ring Road, Chengdu, 610072, People's Republic of China
| | - Congrui Liu
- Central Laboratory and Department of Medical Ultrasound, Sichuan Academy of Medical Sciences, Sichuan Provincial People's Hospital, School of Medicine, University of Electronic Science and Technology of China, No. 32, West Second Section, First Ring Road, Chengdu, 610072, People's Republic of China
| | - Chao Fang
- Central Laboratory and Department of Medical Ultrasound, Sichuan Academy of Medical Sciences, Sichuan Provincial People's Hospital, School of Medicine, University of Electronic Science and Technology of China, No. 32, West Second Section, First Ring Road, Chengdu, 610072, People's Republic of China
| | - Qiuxia Peng
- Central Laboratory and Department of Medical Ultrasound, Sichuan Academy of Medical Sciences, Sichuan Provincial People's Hospital, School of Medicine, University of Electronic Science and Technology of China, No. 32, West Second Section, First Ring Road, Chengdu, 610072, People's Republic of China
- Department of Stomatology and Central Laboratory, School of Medicine, Shanghai Tenth People's Hospital, Tongji University, NO. 301 Yan-Chang-Zhong Road, Shanghai, 200072, People's Republic of China
| | - Wen Qin
- Central Laboratory and Department of Medical Ultrasound, Sichuan Academy of Medical Sciences, Sichuan Provincial People's Hospital, School of Medicine, University of Electronic Science and Technology of China, No. 32, West Second Section, First Ring Road, Chengdu, 610072, People's Republic of China
| | - Xuebing Yan
- Jiangsu Provincial Innovation and Practice Base for Postdoctors, Suining People's Hospital, Affiliated Hospital of Xuzhou Medical University, No.2, Bayi West Road, Suining, Xu Zhou, 221000, Jiangsu Province, People's Republic of China.
| | - Kun Zhang
- Central Laboratory and Department of Medical Ultrasound, Sichuan Academy of Medical Sciences, Sichuan Provincial People's Hospital, School of Medicine, University of Electronic Science and Technology of China, No. 32, West Second Section, First Ring Road, Chengdu, 610072, People's Republic of China.
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Gaddala P, Choudhary S, Sethi S, Sainaga Jyothi VG, Katta C, Bahuguna D, Singh PK, Pandey M, Madan J. Etodolac utility in osteoarthritis: drug delivery challenges, topical nanotherapeutic strategies and potential synergies. Ther Deliv 2024; 15:977-995. [PMID: 39345034 PMCID: PMC11583675 DOI: 10.1080/20415990.2024.2405456] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 06/29/2024] [Accepted: 09/13/2024] [Indexed: 10/01/2024] Open
Abstract
Osteoarthritis (OSA) is a prevalent joint disorder characterized by losing articular cartilage, primarily affecting the hip, knee and spine joints. The impact of OSA offers a major challenge to health systems globally. Therapeutic approaches encompass surgical interventions, non-pharmacological therapies (exercise, rehabilitation, behavioral interventions) and pharmacological treatments. Inflammatory processes within OSA joints are regulated by pro-inflammatory and anti-inflammatory cytokines. Etodolac, a COX-2-selective inhibitor, is the gold standard for OSA management and uniquely does not inhibit gastric prostaglandins. This comprehensive review offers insights into OSA's pathophysiology, genetic factors and biological determinants influencing disease progression. Emphasis is placed on the pivotal role of etodolac in OSA management, supported by both preclinical and clinical evidences in topical drug delivery. Notably, in-silico docking studies suggested potential synergies between etodolac and baicalein, considering ADAMTS-4, COX-2, MMP-3 and MMP-13 as essential therapeutic targets. Integration of artificial neural network (ANN) techniques with nanotechnology approaches emerges as a promising strategy for optimizing and personalizing topical etodolac delivery. Furthermore, the synergistic potential of etodolac and baicalein warrants in-depth exploration. Hence, by embracing cutting-edge technologies like ANN and nanomedicine, the optimization of topical etodolac delivery could guide a new era of OSA treatment.
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Affiliation(s)
- Pavani Gaddala
- Department of Pharmaceutics, National Institute of Pharmaceutical Education & Research, Hyderabad, Telangana, India
| | - Shalki Choudhary
- Department of Pharmaceutical Sciences & Drug Research, Punjabi University, Patiala, Punjab, India
| | - Sheshank Sethi
- Department of Pharmaceutical Sciences & Drug Research, Punjabi University, Patiala, Punjab, India
| | - Vaskuri Gs Sainaga Jyothi
- Department of Pharmaceutics, National Institute of Pharmaceutical Education & Research, Hyderabad, Telangana, India
| | - Chantibabu Katta
- Department of Pharmaceutics, National Institute of Pharmaceutical Education & Research, Hyderabad, Telangana, India
| | - Deepankar Bahuguna
- Department of Pharmaceutics, National Institute of Pharmaceutical Education & Research, Hyderabad, Telangana, India
| | - Pankaj Kumar Singh
- Department of Pharmaceutics, National Institute of Pharmaceutical Education & Research, Hyderabad, Telangana, India
| | - Manisha Pandey
- Department of Pharmaceutical Sciences, Central University of Haryana, SSH 17, Jant, Haryana, 123031, India
| | - Jitender Madan
- Department of Pharmaceutics, National Institute of Pharmaceutical Education & Research, Hyderabad, Telangana, India
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25
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Basso J, Fortuna A, Vitorino R, Vitorino C. Old drugs, new tricks: Delivering pitavastatin-loaded nanostructured lipid carriers for glioblastoma treatment. Colloids Surf B Biointerfaces 2024; 245:114253. [PMID: 39303387 DOI: 10.1016/j.colsurfb.2024.114253] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 07/21/2024] [Revised: 09/01/2024] [Accepted: 09/16/2024] [Indexed: 09/22/2024]
Abstract
Glioblastoma (GB) is the most common and lethal primary form of malignant brain cancers. Its intrinsic aggressiveness and the blood-brain barrier (BBB) are two major factors that limit the efficacy of standard therapies. In recent years, nanostructured lipid carriers (NLCs) have established themselves as a promising avenue for improving drug delivery to the brain, overcoming the challenges associated with the low drug permeability of the BBB. This work delves into the systematic development of a novel carrier for pitavastatin delivery by establishing a "get it right at the first time" quality by design perspective, supported by multivariate analysis, computational modelling, and molecular docking. The manufacturing process was comprehensively evaluated at each step, from raw material selection to NLC purification, thus leading to a carrier with optimal colloidal, encapsulation and stability properties. The cytotoxic behaviour of the carrier was assessed in a panel of GB cell lines, which includes a low, a medium and a highly sensitive cell line to pitavastatin, providing a better discriminatory power and addressing the different potential in the therapeutic responses. The results obtained reflect a strong antiglioblastoma activity in concentrations where the standard of care lacks activity, as well as a swift and prominent internalization by GB cells. Overall, this work positions these long-term stable parenteral systems in line with the hypothesis of providing more effective surrogate therapeutics in the field of GB.
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Affiliation(s)
- João Basso
- Faculty of Pharmacy, University of Coimbra, Coimbra 3000-548, Portugal; Coimbra Chemistry Centre, Institute of Molecular Sciences-IMS, Faculty of Sciences and Technology, University of Coimbra, Coimbra 3004-535, Portugal
| | - Ana Fortuna
- Faculty of Pharmacy, University of Coimbra, Coimbra 3000-548, Portugal; Coimbra Institute for Biomedical Imaging and Translational Research, CIBIT, University of Coimbra, Coimbra 3000-548, Portugal
| | - Rui Vitorino
- Department of Medical Sciences, Institute of Biomedicine-iBiMED, University of Aveiro, Aveiro 3810-193, Portugal; UnIC@RISE, Department of Surgery and Physiology, Faculty of Medicine, University of Porto, Porto 4200-319, Portugal; LAQV/REQUIMTE, Department of Chemistry, University of Aveiro, Aveiro 3810-193, Portugal
| | - Carla Vitorino
- Faculty of Pharmacy, University of Coimbra, Coimbra 3000-548, Portugal; Coimbra Chemistry Centre, Institute of Molecular Sciences-IMS, Faculty of Sciences and Technology, University of Coimbra, Coimbra 3004-535, Portugal.
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26
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Nwagwu C, Onugwu A, Echezona A, Uzondu S, Agbo C, Kenechukwu F, Ogbonna J, Ugorji L, Nwobi L, Nwobi O, Mmuotoo O, Ezeibe E, Loretz B, Tarirai C, Mbara KC, Agumah N, Nnamani P, Ofokansi K, Lehr CM, Attama A. Biopolymeric and lipid-based nanotechnological strategies for the design and development of novel mosquito repellent systems: recent advances. NANOSCALE ADVANCES 2024:d4na00474d. [PMID: 39247861 PMCID: PMC11378059 DOI: 10.1039/d4na00474d] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Track Full Text] [Subscribe] [Scholar Register] [Received: 06/08/2024] [Accepted: 08/15/2024] [Indexed: 09/10/2024]
Abstract
Mosquitoes are the most medically important arthropod vectors of several human diseases. These diseases are known to severely incapacitate and debilitate millions of people, resulting in countless loss of lives. Over the years, several measures have been put in place to control the transmission of mosquito-borne diseases, one of which is using repellents. Repellents are one of the most effective personal protective measures against mosquito-borne diseases. However, conventional delivery systems of repellents (e.g., creams, gels, and sprays) are plagued with toxicity and short-term efficacy issues. The application of biopolymeric and lipid-based systems has been explored over the years to develop better delivery systems for active pharmaceutical ingredients including mosquito repellents. These delivery systems (e.g., solid lipid micro/nanoparticles, micro/nanoemulsions, or liposomes) possess desirable properties such as high biocompatibility, versatility, and controlled/sustained drug delivery, and thus are very important in tackling the clinical challenges of conventional repellent systems. Their capability for controlled/sustained drug release has improved patient compliance as it removes the need for consistent reapplication of repellents. They can also be engineered to reduce repellents' skin permeation, consequently improving their safety. However, despite the benefits that these systems offer very few of them have been successfully translated to the global market for commercial use, a vital challenge that previous reports have not thoroughly examined. The issue of limited clinical translation of novel repellent systems is a vital aspect to consider, as the ultimate goal is to move these systems from bench to bedside. As such, this study seeks to highlight the recent advances in the use of biopolymeric and lipid-based systems for the development of novel mosquito-repellent systems and also analyze the challenges that have limited the clinical translation of these systems while proposing possible strategies to overcome these challenges.
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Affiliation(s)
- Chinekwu Nwagwu
- Drug Delivery and Nanomedicines Research Laboratory, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Nigeria Nsukka Nigeria
- Helmholtz Institute for Pharmaceutical Research Saarland Saarbrucken Germany
| | - Adaeze Onugwu
- Drug Delivery and Nanomedicines Research Laboratory, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Nigeria Nsukka Nigeria
| | - Adaeze Echezona
- Drug Delivery and Nanomedicines Research Laboratory, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Nigeria Nsukka Nigeria
| | - Samuel Uzondu
- Drug Delivery and Nanomedicines Research Laboratory, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Nigeria Nsukka Nigeria
| | - Chinazom Agbo
- Drug Delivery and Nanomedicines Research Laboratory, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Nigeria Nsukka Nigeria
| | - Frankline Kenechukwu
- Drug Delivery and Nanomedicines Research Laboratory, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Nigeria Nsukka Nigeria
| | - John Ogbonna
- Drug Delivery and Nanomedicines Research Laboratory, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Nigeria Nsukka Nigeria
| | - Lydia Ugorji
- Department of Pharmaceutical Technology and Industrial Pharmacy, University of Nigeria Nsukka Nigeria
| | - Lotanna Nwobi
- Department of Veterinary Physiology and Pharmacology, University of Nigeria Nsukka Nigeria
| | - Obichukwu Nwobi
- Department of Veterinary Public Health and Preventive Medicine, Faculty of Veterinary Medicine, University of Nigeria Nsukka Enugu State Nigeria
| | - Oluchi Mmuotoo
- Faculty of Pharmaceutical Sciences, University of Nigeria Nsukka Nigeria
| | - Ezinwanne Ezeibe
- Department of Pharmaceutical Microbiology and Biotechnology, University of Nigeria Nsukka Nigeria
| | - Brigitta Loretz
- Helmholtz Institute for Pharmaceutical Research Saarland Saarbrucken Germany
| | - Clemence Tarirai
- Department of Pharmaceutical Sciences, Faculty of Sciences, Tshwane University of Technology Pretoria South Africa
| | - Kingsley Chimaeze Mbara
- Department of Pharmaceutical Sciences, Faculty of Sciences, Tshwane University of Technology Pretoria South Africa
| | - Nnabuife Agumah
- Department of Applied Microbiology, Faculty of Science, Ebonyi State University Nigeria
| | - Petra Nnamani
- Drug Delivery and Nanomedicines Research Laboratory, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Nigeria Nsukka Nigeria
- Helmholtz Institute for Pharmaceutical Research Saarland Saarbrucken Germany
| | - Kenneth Ofokansi
- Drug Delivery and Nanomedicines Research Laboratory, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Nigeria Nsukka Nigeria
| | - Claus-Micheal Lehr
- Helmholtz Institute for Pharmaceutical Research Saarland Saarbrucken Germany
| | - Anthony Attama
- Drug Delivery and Nanomedicines Research Laboratory, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Nigeria Nsukka Nigeria
- Institute for Drug-Herbal Medicine-Excipient Research and Development, University of Nigeria Nsukka Nigeria
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Subramanian G, Kalidasan K, Quah S, Han QCG, Chan J, Wacker MG, Sampath P. Breaking barriers: Innovative approaches for skin delivery of RNA therapeutics. Int J Pharm 2024; 661:124435. [PMID: 38986965 DOI: 10.1016/j.ijpharm.2024.124435] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 12/26/2023] [Revised: 06/30/2024] [Accepted: 07/04/2024] [Indexed: 07/12/2024]
Abstract
RNA therapeutics represent a rapidly expanding platform with game-changing prospects in personalized medicine. The disruptive potential of this technology will overhaul the standard of care with reference to both primary and specialty care. To date, RNA therapeutics have mostly been delivered parenterally via injection, but topical administration followed by intradermal or transdermal delivery represents an attractive method that is convenient to patients and minimally invasive. The skin barrier, particularly the lipid-rich stratum corneum, presents a significant hurdle to the uptake of large, charged oligonucleotide drugs. Therapeutic oligonucleotides need to be engineered for stability and specificity and formulated with state-of-the-art delivery strategies for efficient uptake. This review will cover various passive and active strategies deployed to enhance permeation through the stratum corneum and achieve effective delivery of RNA therapeutics to treat both local skin disorders and systemic diseases. Some strategies to achieve selectivity between local and systemic administration will also be discussed.
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Affiliation(s)
- Gowtham Subramanian
- A*STAR Skin Research Labs (A*SRL), Agency for Science, Technology and Research (A*STAR), 8A Biomedical Grove #06-06 Immunos, Singapore 138648, Singapore
| | - Kamaladasan Kalidasan
- A*STAR Skin Research Labs (A*SRL), Agency for Science, Technology and Research (A*STAR), 8A Biomedical Grove #06-06 Immunos, Singapore 138648, Singapore
| | - Shan Quah
- A*STAR Skin Research Labs (A*SRL), Agency for Science, Technology and Research (A*STAR), 8A Biomedical Grove #06-06 Immunos, Singapore 138648, Singapore
| | - Qi Chou Gavin Han
- Department of Pharmacy and Pharmaceutical Sciences, Faculty of Science, National University of Singapore (NUS), 4 Science Drive 2, Singapore 117544, Singapore
| | - Justin Chan
- A*STAR Skin Research Labs (A*SRL), Agency for Science, Technology and Research (A*STAR), 8A Biomedical Grove #06-06 Immunos, Singapore 138648, Singapore
| | - Matthias G Wacker
- Department of Pharmacy and Pharmaceutical Sciences, Faculty of Science, National University of Singapore (NUS), 4 Science Drive 2, Singapore 117544, Singapore.
| | - Prabha Sampath
- A*STAR Skin Research Labs (A*SRL), Agency for Science, Technology and Research (A*STAR), 8A Biomedical Grove #06-06 Immunos, Singapore 138648, Singapore; Skin Research Institute of Singapore (SRIS), 11 Mandalay Road #17-01 Clinical Sciences Building, Singapore 308232, Singapore; Genome Institute of Singapore, Agency for Science, Technology and Research (A*STAR), 60 Biopolis Street, #02-01 Genome, Singapore 138672, Singapore; Program in Cancer & Stem Cell Biology, Duke-NUS Medical School, 8 College Road, Singapore 169857, Singapore.
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Cortesi R, Sguizzato M, Ferrara F. Lipid-based nanosystems for wound healing. Expert Opin Drug Deliv 2024; 21:1191-1211. [PMID: 39172249 DOI: 10.1080/17425247.2024.2391473] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 05/14/2024] [Revised: 07/31/2024] [Accepted: 08/08/2024] [Indexed: 08/23/2024]
Abstract
INTRODUCTION Wounds, resulting from traumas, surgery, burns or diabetes, are important medical problems due to the complexity of wound healing process regarding healing times and healthcare costs. Nanosystems have emerged as promising candidates in this field thank to their properties and versatile applications in drugs delivery. AREAS COVERED Lipid-based nanosystems (LBN) are described for wound treatment, highlighting their different behaviors when interacting with the cutaneous tissue. The role of nanosystems in delivering mostly natural compounds on skin as well as the technological and engineering strategies to increase their efficiency in wound healing effect are reviewed. Finally, in vitro, ex-vivo and in vivo studies are reported. EXPERT OPINION LBN have shown promise in addressing the challenges of wound healing as they can improve the stability of drugs used in wound therapy, leading to higher efficacy and fewer adverse effects as compared to traditional formulations. LBNs being involved in the inflammatory and proliferation stages of the wound healing process, enable the modification of wound healing through multiple ways. In addition, the use of new technologies, including 3D bioprinting and photobiomodulation, may lead to potential breakthroughs in wound healing. This would provide clinicians with more potent forms of therapy for wound healing.
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Affiliation(s)
- Rita Cortesi
- Department of Chemical, Pharmaceutical and Agricultural Sciences (Docpas), University of Ferrara, University of Ferrara, Ferrara, Italy
- Biotechnology InterUniversity Consortium (C.I.B.), Ferrara Section, University of Ferrara, Ferrara, Italy
| | - Maddalena Sguizzato
- Department of Chemical, Pharmaceutical and Agricultural Sciences (Docpas), University of Ferrara, University of Ferrara, Ferrara, Italy
- Biotechnology InterUniversity Consortium (C.I.B.), Ferrara Section, University of Ferrara, Ferrara, Italy
| | - Francesca Ferrara
- Department of Chemical, Pharmaceutical and Agricultural Sciences (Docpas), University of Ferrara, University of Ferrara, Ferrara, Italy
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Cocoș FI, Anuța V, Popa L, Ghica MV, Nica MA, Mihăilă M, Fierăscu RC, Trică B, Nicolae CA, Dinu-Pîrvu CE. Development and Evaluation of Docetaxel-Loaded Nanostructured Lipid Carriers for Skin Cancer Therapy. Pharmaceutics 2024; 16:960. [PMID: 39065657 PMCID: PMC11279931 DOI: 10.3390/pharmaceutics16070960] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [Grants] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 05/01/2024] [Revised: 07/12/2024] [Accepted: 07/14/2024] [Indexed: 07/28/2024] Open
Abstract
This study focuses on the design, characterization, and optimization of nanostructured lipid carriers (NLCs) loaded with docetaxel for the treatment of skin cancer. Employing a systematic formulation development process guided by Design of Experiments (DoE) principles, key parameters such as particle size, polydispersity index (PDI), zeta potential, and entrapment efficiency were optimized to ensure the stability and drug-loading efficacy of the NLCs. Combined XRD and cryo-TEM analysis were employed for NLC nanostructure evaluation, confirming the formation of well-defined nanostructures. In vitro kinetics studies demonstrated controlled and sustained docetaxel release over 48 h, emphasizing the potential for prolonged therapeutic effects. Cytotoxicity assays on human umbilical vein endothelial cells (HUVEC) and SK-MEL-24 melanoma cell line revealed enhanced efficacy against cancer cells, with significant selective cytotoxicity and minimal impact on normal cells. This multidimensional approach, encompassing formulation optimization and comprehensive characterization, positions the docetaxel-loaded NLCs as promising candidates for advanced skin cancer therapy. The findings underscore the potential translational impact of these nanocarriers, paving the way for future preclinical investigations and clinical applications in skin cancer treatment.
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Affiliation(s)
- Florentina-Iuliana Cocoș
- Department of Physical and Colloidal Chemistry, Faculty of Pharmacy, “Carol Davila” University of Medicine and Pharmacy, 6 Traian Vuia Str., 020956 Bucharest, Romania; (F.-I.C.); (L.P.); (M.V.G.); (M.-A.N.); (C.-E.D.-P.)
- Innovative Therapeutic Structures Research and Development Centre (InnoTher), “Carol Davila” University of Medicine and Pharmacy, 6 Traian Vuia Str., 020956 Bucharest, Romania
| | - Valentina Anuța
- Department of Physical and Colloidal Chemistry, Faculty of Pharmacy, “Carol Davila” University of Medicine and Pharmacy, 6 Traian Vuia Str., 020956 Bucharest, Romania; (F.-I.C.); (L.P.); (M.V.G.); (M.-A.N.); (C.-E.D.-P.)
- Innovative Therapeutic Structures Research and Development Centre (InnoTher), “Carol Davila” University of Medicine and Pharmacy, 6 Traian Vuia Str., 020956 Bucharest, Romania
| | - Lăcrămioara Popa
- Department of Physical and Colloidal Chemistry, Faculty of Pharmacy, “Carol Davila” University of Medicine and Pharmacy, 6 Traian Vuia Str., 020956 Bucharest, Romania; (F.-I.C.); (L.P.); (M.V.G.); (M.-A.N.); (C.-E.D.-P.)
- Innovative Therapeutic Structures Research and Development Centre (InnoTher), “Carol Davila” University of Medicine and Pharmacy, 6 Traian Vuia Str., 020956 Bucharest, Romania
| | - Mihaela Violeta Ghica
- Department of Physical and Colloidal Chemistry, Faculty of Pharmacy, “Carol Davila” University of Medicine and Pharmacy, 6 Traian Vuia Str., 020956 Bucharest, Romania; (F.-I.C.); (L.P.); (M.V.G.); (M.-A.N.); (C.-E.D.-P.)
- Innovative Therapeutic Structures Research and Development Centre (InnoTher), “Carol Davila” University of Medicine and Pharmacy, 6 Traian Vuia Str., 020956 Bucharest, Romania
| | - Mihaela-Alexandra Nica
- Department of Physical and Colloidal Chemistry, Faculty of Pharmacy, “Carol Davila” University of Medicine and Pharmacy, 6 Traian Vuia Str., 020956 Bucharest, Romania; (F.-I.C.); (L.P.); (M.V.G.); (M.-A.N.); (C.-E.D.-P.)
- Innovative Therapeutic Structures Research and Development Centre (InnoTher), “Carol Davila” University of Medicine and Pharmacy, 6 Traian Vuia Str., 020956 Bucharest, Romania
| | - Mirela Mihăilă
- Center of Immunology, Ștefan S. Nicolau Institute of Virology, Romanian Academy, 030304 Bucharest, Romania;
- Faculty of Pharmacy, Titu Maiorescu University, 16 Gheorghe Sincai Blvd, 040314 Bucharest, Romania
| | - Radu Claudiu Fierăscu
- National Institute for Research & Development in Chemistry and Petrochemistry—ICECHIM Bucharest, 202 Spl. Independentei, 060021 Bucharest, Romania; (R.C.F.); (B.T.); (C.A.N.)
- Faculty of Chemical Engineering and Biotechnology, National University of Science and Technology Politehnica Bucharest, 1-7 Gh. Polizu Str., 011061 Bucharest, Romania
| | - Bogdan Trică
- National Institute for Research & Development in Chemistry and Petrochemistry—ICECHIM Bucharest, 202 Spl. Independentei, 060021 Bucharest, Romania; (R.C.F.); (B.T.); (C.A.N.)
| | - Cristian Andi Nicolae
- National Institute for Research & Development in Chemistry and Petrochemistry—ICECHIM Bucharest, 202 Spl. Independentei, 060021 Bucharest, Romania; (R.C.F.); (B.T.); (C.A.N.)
| | - Cristina-Elena Dinu-Pîrvu
- Department of Physical and Colloidal Chemistry, Faculty of Pharmacy, “Carol Davila” University of Medicine and Pharmacy, 6 Traian Vuia Str., 020956 Bucharest, Romania; (F.-I.C.); (L.P.); (M.V.G.); (M.-A.N.); (C.-E.D.-P.)
- Innovative Therapeutic Structures Research and Development Centre (InnoTher), “Carol Davila” University of Medicine and Pharmacy, 6 Traian Vuia Str., 020956 Bucharest, Romania
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Atapour-Mashhad H, Tayarani-Najaran Z, Golmohammadzadeh S. Preparation and characterization of novel nanostructured lipid carriers (NLC) and solid lipid nanoparticles (SLN) containing coenzyme Q10 as potent antioxidants and antityrosinase agents. Heliyon 2024; 10:e31429. [PMID: 38882272 PMCID: PMC11180323 DOI: 10.1016/j.heliyon.2024.e31429] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 05/11/2024] [Accepted: 05/15/2024] [Indexed: 06/18/2024] Open
Abstract
We developed novel and optimal Q10-NLC/SLN formulations as antioxidant and anti-tyrosinase agents. The formulations were analyzed for particle size, morphology, entrapment efficiency (EE %), and long-term stability. The in vitro drug release and in vivo skin penetration were evaluated using dialysis bag diffusion and Sprague Dawley (SD) rats, respectively. Cytotoxicity and protecting effects were assessed by AlamarBlue® assay, ROS level by DCFH-DA, and tyrosinase activity by l-DOPA assay, measuring the absorbance at 470 nm. The selected formulations had optimal surface characterizations, including Z-average size, PDI, and Zeta potential ranging from 125 to 207 nm, 0.09-0.22, and -7 to -24, respectively. They also exhibited physiochemical stability for up to 6 months and EE% above 80 %. The lipids ratio and co-Q10 amount as variable factors significantly affected particle size and zeta potential but were insignificant on PDI. The in vitro release diagram showed that Q10-NLC/SLN revealed a fast release during the first 8 h and prolonged release afterward. The in vivo skin permeation revealed a higher accumulative uptake of co-Q10 in the skin for Q10-NLC/SLN compared to Q10 emulsions. Both selected Q10-NLC and Q10-SLN could reduce intracellular ROS after exposure to H2O2. The Q10-NLC was found to be more potent for inhibiting the tyrosinase activity compared to O10-SLN. The results suggest that the new formulations are promising carriers for topical delivery of co-Q10 as an anti-aging and skin-whitening agent.
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Affiliation(s)
- Hoda Atapour-Mashhad
- Nanotechnology Research Center, Pharmaceutical Technology Institute, Mashhad University of Medical Sciences, Mashhad, Iran
- Department of Pharmaceutics, Faculty of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran
| | - Zahra Tayarani-Najaran
- Medical Toxicology Research Center, Mashhad University of Medical Sciences, Mashhad, Iran
- Targeted Drug Delivery Research Center, Pharmaceutical Technology Institute, Mashhad University of Medical Sciences, Mashhad, Iran
| | - Shiva Golmohammadzadeh
- Nanotechnology Research Center, Pharmaceutical Technology Institute, Mashhad University of Medical Sciences, Mashhad, Iran
- Department of Pharmaceutics, Faculty of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran
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Shalaby ES, Abdelhameed MF, Ismail SA, Ahmed YH, Aboutaleb S. Innovative Indian Propolis Loaded Carnauba Wax Based Lipid Structured Nanocarriers: Preparation, Characterization and In Vitro /In Vivo Antifungal Activities. BIONANOSCIENCE 2024; 14:1726-1743. [DOI: 10.1007/s12668-024-01361-9] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Accepted: 03/08/2024] [Indexed: 01/03/2025]
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Munir M, Zaman M, Waqar MA, Khan MA, Alvi MN. Solid lipid nanoparticles: a versatile approach for controlled release and targeted drug delivery. J Liposome Res 2024; 34:335-348. [PMID: 37840238 DOI: 10.1080/08982104.2023.2268711] [Citation(s) in RCA: 3] [Impact Index Per Article: 3.0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 06/08/2023] [Accepted: 10/02/2023] [Indexed: 10/17/2023]
Abstract
Solid Lipid Nanoparticles (SLN), the first type of lipid-based solid carrier systems in the nanometer range, were introduced as a replacement for liposomes. SLN are aqueous colloidal dispersions with solid biodegradable lipids as their matrix. SLN is produced using processes like solvent diffusion method and high-pressure homogenization, among others. Major benefits include regulated release, increased bioavailability, preservation of peptides and chemically labile compounds like retinol against degradation, cost-effective excipients, better drug integration, and a broad range of applications. Solid lipid nanoparticles can be administered via different routes, such as oral, parenteral, pulmonary, etc. SLN can be prepared by using high shear mixing as well as low shear mixing. The next generation of solid lipids, nanostructured lipid carriers (NLC), can reduce some of the drawbacks of SLN, such as its restricted capacity for drug loading and drug expulsion during storage. NLC are controlled nanostructured lipid particles that enhance drug loading. This review covers a brief introduction of solid lipid nanoparticles, manufacturing techniques, benefits, limitations, and their characterization tests.
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Affiliation(s)
- Minahal Munir
- Faculty of Pharmaceutical Sciences, University of Central Punjab, Lahore, Pakistan
| | - Muhammad Zaman
- Faculty of Pharmaceutical Sciences, University of Central Punjab, Lahore, Pakistan
| | - Muhammad Ahsan Waqar
- Faculty of Pharmaceutical Sciences, University of Central Punjab, Lahore, Pakistan
| | - Mahtab Ahmad Khan
- Faculty of Pharmaceutical Sciences, University of Central Punjab, Lahore, Pakistan
| | - Muhammad Nadeem Alvi
- Faculty of Pharmaceutical Sciences, University of Central Punjab, Lahore, Pakistan
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Hegde AR, Kunder MU, Narayanaswamy M, Murugesan S, Furtado SC, Veerabhadraiah BB, Srinivasan B. Advancements in sunscreen formulations: integrating polyphenolic nanocarriers and nanotechnology for enhanced UV protection. ENVIRONMENTAL SCIENCE AND POLLUTION RESEARCH INTERNATIONAL 2024; 31:38061-38082. [PMID: 38806984 DOI: 10.1007/s11356-024-33712-0] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Grants] [Track Full Text] [Subscribe] [Scholar Register] [Received: 11/28/2023] [Accepted: 05/12/2024] [Indexed: 05/30/2024]
Abstract
Sunscreens are essential in protecting the skin from harmful effects of ultraviolet radiation (UVR). These formulations, designed to absorb, block, or scatter UVR, offer vital protection against skin aging, sunburns, and the development of skin cancers like melanomas. However, some sunscreens, especially those containing organic/chemical compounds, can cause allergic reactions. To address this, researchers are extensively investigating formulations that incorporate plant extracts rich in polyphenols, such as flavonoids and carotenoids, which can be considered safer alternatives. Products derived from plants are commonly used in cosmetics to counteract skin aging due to their antioxidant activity that combat harmful free radicals. This review focuses on evaluating the advancements in chemical and natural sunscreens, exploring the integration of polyphenolic nanocarriers within sunscreen formulas, their interaction with UVR, and utilizing nanotechnology to enhance their effectiveness. An attempt has been made to highlight the concerns related to toxicity associated with their use and notable advancements in the regulatory aspects governing their utilization.
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Affiliation(s)
- Aswathi Raju Hegde
- Department of Pharmaceutics, Faculty of Pharmacy, M.S. Ramaiah University of Applied Sciences, Gnanagangothri Campus, New B.E.L. Road, M.S.R. Nagar, M.S.R.I.T Post, Bengaluru, 560054, Karnataka, India.
| | - Manisha Uday Kunder
- Department of Pharmaceutics, Faculty of Pharmacy, M.S. Ramaiah University of Applied Sciences, Gnanagangothri Campus, New B.E.L. Road, M.S.R. Nagar, M.S.R.I.T Post, Bengaluru, 560054, Karnataka, India
| | - Megha Narayanaswamy
- Department of Pharmaceutics, Faculty of Pharmacy, M.S. Ramaiah University of Applied Sciences, Gnanagangothri Campus, New B.E.L. Road, M.S.R. Nagar, M.S.R.I.T Post, Bengaluru, 560054, Karnataka, India
| | - Shruthi Murugesan
- Department of Pharmaceutics, Faculty of Pharmacy, M.S. Ramaiah University of Applied Sciences, Gnanagangothri Campus, New B.E.L. Road, M.S.R. Nagar, M.S.R.I.T Post, Bengaluru, 560054, Karnataka, India
| | - Sharon Caroline Furtado
- Department of Pharmaceutics, Faculty of Pharmacy, M.S. Ramaiah University of Applied Sciences, Gnanagangothri Campus, New B.E.L. Road, M.S.R. Nagar, M.S.R.I.T Post, Bengaluru, 560054, Karnataka, India
| | - Basavaraj Basappa Veerabhadraiah
- Department of Pharmaceutics, Faculty of Pharmacy, M.S. Ramaiah University of Applied Sciences, Gnanagangothri Campus, New B.E.L. Road, M.S.R. Nagar, M.S.R.I.T Post, Bengaluru, 560054, Karnataka, India
| | - Bharath Srinivasan
- Department of Pharmaceutics, Faculty of Pharmacy, M.S. Ramaiah University of Applied Sciences, Gnanagangothri Campus, New B.E.L. Road, M.S.R. Nagar, M.S.R.I.T Post, Bengaluru, 560054, Karnataka, India
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Fang Q, Li Y, Xiong F, Hu X, Song Y, Shen W, Dong H, Shi X, Wang H. Formulation and Characterization of Ethosomes for Transdermal Delivery of Prinsepia Utilis Rogle Seed Oil with Ameliorative Effects against UVB-Induced Skin Damage. AAPS PharmSciTech 2024; 25:122. [PMID: 38816546 DOI: 10.1208/s12249-024-02822-w] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 02/23/2024] [Accepted: 04/23/2024] [Indexed: 06/01/2024] Open
Abstract
Prinsepia utilis seed oil (PUSO) is a natural medication obtained from Prinsepia utilis Rogle seed, which has been used for the treatment of skin diseases. The study aims to prepare ethosomes with high drug loading as a water-soluble transdermal vehicle to enhance the transdermal delivery of PUSO. PUSO-loaded ethosomes (PEs) were prepared using a cold method, and optimized by an orthogonal experimental design with entrapment efficiency (EE) as the dependent variable. The PEs prepared with the optimized formulation showed good stability, with a spherical shape under transmission electron microscopy (TEM), average particle size of 39.12 ± 0.85 nm, PDI of 0.270 ± 0.01, zeta potential of -11.3 ± 0.24 mV, and EE of 95.93 ± 0.43%. PEs significantly increased the skin deposition of PUSO compared to the PUSO suspension (P < 0.001). Moreover, the optimum formula showed significant ameliorative effects on ultraviolet B (UVB) irradiation-associated macroscopic and histopathological changes in mice skin. Therefore, PEs represent a promising therapeutic approach for the treatment of UVB-induced skin inflammation, with the potential for industrialization.
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Affiliation(s)
- Qianqian Fang
- State Key Laboratory of Natural Medicines, School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing, 210009, People's Republic of China
| | - You Li
- State Key Laboratory of Natural Medicines, School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing, 210009, People's Republic of China
| | - Fei Xiong
- State Key Laboratory of Bioelectronics, Jiangsu Laboratory for Biomaterials and Devices, Southeast University, Nanjing, 210009, People's Republic of China
| | - Xiaolong Hu
- State Key Laboratory of Natural Medicines, School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing, 210009, People's Republic of China
| | - Ying Song
- State Key Laboratory of Natural Medicines, School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing, 210009, People's Republic of China
| | - Wenbing Shen
- Instrumental Analysis Center, China Pharmaceutical University, Nanjing, 210009, People's Republic of China
| | - Haijuan Dong
- Instrumental Analysis Center, China Pharmaceutical University, Nanjing, 210009, People's Republic of China
| | - Xinhong Shi
- State Key Laboratory of Natural Medicines, School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing, 210009, People's Republic of China.
| | - Hao Wang
- State Key Laboratory of Natural Medicines, School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing, 210009, People's Republic of China.
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Yeo S, Wu H, Yoon I, Lee WK, Hwang SJ. Design of smart chemotherapy of doxorubicin hydrochloride using nanostructured lipid carriers and solid lipid nanoparticles for improved anticancer efficacy. Int J Pharm 2024; 657:124048. [PMID: 38537925 DOI: 10.1016/j.ijpharm.2024.124048] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 12/21/2023] [Revised: 03/21/2024] [Accepted: 03/24/2024] [Indexed: 04/20/2024]
Abstract
Doxorubicin hydrochloride (DOX) is an anticancer agent used in cancer chemotherapy. The purpose of this study was to design nanostructured lipid carriers (NLCs) of DOX as smart chemotherapy to improve its photostability and anticancer efficacy. The characteristics of DOX and DOX-loaded NLCs were investigated using UV-Vis spectroscopy, Fourier transform infrared (FTIR) spectroscopy, particle size, and zeta potential study. The cytotoxicity of DOX was evaluated against three cancer cell lines (HeLa, A549, and CT-26). The particle size and zeta potential were in the range 58.45-94.08 nm and -5.80 mV - -18.27 mV, respectively. The chemical interactions, particularly hydrogen bonding and van der Waals forces, between DOX and the main components of NLCs was confirmed by FTIR. NLCs showed the sustained release profile of DOX. The photostability results revealed that the NLC system improved the photostability of DOX. Cytotoxicity results using the three cell lines showed that all formulations improved the anticancer efficacy of free DOX, and the efficacy was dependent on cell type and particle size. These results suggest that DOX-loaded NLCs are promising chemotherapeutic agents for cancer treatment.
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Affiliation(s)
- Sooho Yeo
- Yonsei Institute of Pharmaceutical Sciences, College of Pharmacy, Yonsei University, Incheon 21983, Republic of Korea; Center for Nano Manufacturing and Department of Nanoscience and Engineering, Inje University, 197 Injero, Gimhae 50834, Gyeongnam, Republic of Korea
| | - Huiqiang Wu
- Center for Nano Manufacturing and Department of Nanoscience and Engineering, Inje University, 197 Injero, Gimhae 50834, Gyeongnam, Republic of Korea
| | - Il Yoon
- Center for Nano Manufacturing and Department of Nanoscience and Engineering, Inje University, 197 Injero, Gimhae 50834, Gyeongnam, Republic of Korea.
| | - Woo Kyoung Lee
- Center for Nano Manufacturing and Department of Nanoscience and Engineering, Inje University, 197 Injero, Gimhae 50834, Gyeongnam, Republic of Korea.
| | - Sung-Joo Hwang
- Yonsei Institute of Pharmaceutical Sciences, College of Pharmacy, Yonsei University, Incheon 21983, Republic of Korea.
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Chen C, Wang X, Chen W, Liu Q, Wang L. Encapsulation of phenolic acids within food-grade carriers systems: a systematic review. Crit Rev Food Sci Nutr 2024:1-20. [PMID: 38764436 DOI: 10.1080/10408398.2024.2350616] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 05/21/2024]
Abstract
Phenolic acids are natural compounds with potential therapeutic effects against various diseases. However, their incorporation into food and pharmaceutical products is limited by challenges such as instability, low solubility, and reduced bioavailability. This systematic review summarizes recent advances in phenolic acid encapsulation using food-grade carrier systems, focusing on proteins, lipids, and polysaccharides. Encapsulation efficiency, release behavior, and bioavailability are examined, as well as the potential health benefits of encapsulated phenolic acids in food products. Strategies to address limitations of current encapsulation systems are also proposed. Encapsulation has emerged as a promising method to enhance the stability and bioavailability of phenolic acids in food products, and various encapsulation technologies have been developed for this purpose. The use of proteins, lipids, and carbohydrates as carriers in food-grade encapsulation systems remains a common approach, but it is associated with certain limitations. Future research on phenolic acid encapsulation should focus on developing environmentally friendly, organic solvent-free, low-energy, scalable, and stable encapsulation systems, as well as co-encapsulation methods that combine multiple phenolic acids or phenolic acids with other bioactive substances to produce synergistic effects.
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Affiliation(s)
- Chao Chen
- College of Food Science and Engineering, Collaborative Innovation Center for Modern Grain Circulation and Safety, Nanjing University of Finance and Economics, Nanjing, Jiangsu, China
| | - Xiao Wang
- School of Food and Biological Engineering, Jiangsu University, Zhenjiang, Jiangsu, China
| | - Wenqi Chen
- School of Food and Biological Engineering, Jiangsu University, Zhenjiang, Jiangsu, China
| | - Qin Liu
- School of Food and Biological Engineering, Jiangsu University, Zhenjiang, Jiangsu, China
| | - Lifeng Wang
- College of Food Science and Engineering, Collaborative Innovation Center for Modern Grain Circulation and Safety, Nanjing University of Finance and Economics, Nanjing, Jiangsu, China
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Abu Elella MH, Al Khatib AO, Al-Obaidi H. Spray-Dried Nanolipid Powders for Pulmonary Drug Delivery: A Comprehensive Mini Review. Pharmaceutics 2024; 16:680. [PMID: 38794342 PMCID: PMC11125033 DOI: 10.3390/pharmaceutics16050680] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 03/16/2024] [Revised: 04/28/2024] [Accepted: 05/15/2024] [Indexed: 05/26/2024] Open
Abstract
Lung diseases have received great attention in the past years because they contribute approximately one-third of the total global mortality. Pulmonary drug delivery is regarded as one of the most appealing routes to treat lung diseases. It addresses numerous drawbacks linked to traditional dosage forms. It presents notable features, such as, for example, a non-invasive route, localized lung drug delivery, low enzymatic activity, low drug degradation, higher patient compliance, and avoiding first-pass metabolism. Therefore, the pulmonary route is commonly explored for delivering drugs both locally and systemically. Inhalable nanocarrier powders, especially, lipid nanoparticle formulations, including solid-lipid and nanostructured-lipid nanocarriers, are attracting considerable interest in addressing respiratory diseases thanks to their significant advantages, including deep lung deposition, biocompatibility, biodegradability, mucoadhesion, and controlled drug released. Spray drying is a scalable, fast, and commercially viable technique to produce nanolipid powders. This review highlights the ideal criteria for inhalable spray-dried SLN and NLC powders for the pulmonary administration route. Additionally, the most promising inhalation devices, known as dry powder inhalers (DPIs) for the pulmonary delivery of nanolipid powder-based medications, and pulmonary applications of SLN and NLC powders for treating chronic lung conditions, are considered.
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Affiliation(s)
- Mahmoud H. Abu Elella
- School of Pharmacy, University of Reading, Reading RG6 6UR, UK; (M.H.A.E.); (A.O.A.K.)
| | - Arwa Omar Al Khatib
- School of Pharmacy, University of Reading, Reading RG6 6UR, UK; (M.H.A.E.); (A.O.A.K.)
- Faculty of Pharmacy, Al Ahliyya Amman University, Amman 19111, Jordan
| | - Hisham Al-Obaidi
- School of Pharmacy, University of Reading, Reading RG6 6UR, UK; (M.H.A.E.); (A.O.A.K.)
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Saeidi Z, Giti R, Emami A, Rostami M, Mohammadi F. Thermosensitive and mucoadhesive gels containing solid lipid nanoparticles loaded with fluconazole and niosomes loaded with clindamycin for the treatment of periodontal diseases: a laboratory experiment. BMC Oral Health 2024; 24:551. [PMID: 38734599 PMCID: PMC11088776 DOI: 10.1186/s12903-024-04322-6] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 10/17/2023] [Accepted: 05/02/2024] [Indexed: 05/13/2024] Open
Abstract
BACKGROUND Periodontal diseases may benefit more from topical treatments with nanoparticles rather than systemic treatments due to advantages such as higher stability and controlled release profile. This study investigated the preparation and characterization of thermosensitive gel formulations containing clindamycin-loaded niosomes and solid lipid nanoparticles (SLNs) loaded with fluconazole (FLZ), as well as their in vitro antibacterial and antifungal effects in the treatment of common microorganisms that cause periodontal diseases. METHODS This study loaded niosomes and SLNs with clindamycin and FLZ, respectively, and assessed their loading efficiency, particle size, and zeta potential. The particles were characterized using a variety of methods such as differential scanning calorimetry (DSC), dynamic light scattering (DLS), and Transmission Electron Microscopy (TEM). Thermosensitive gels were formulated by combining these particles and their viscosity, gelation temperature, in-vitro release profile, as well as antibacterial and antifungal effects were evaluated. RESULTS Both types of these nanoparticles were found to be spherical (TEM) with a mean particle size of 243.03 nm in niosomes and 171.97 nm in SLNs (DLS), and respective zeta potentials of -23.3 and -15. The loading rate was 98% in niosomes and 51% in SLNs. The release profiles of niosomal formulations were slower than those of the SLNs. Both formulations allowed the release of the drug by first-order kinetic. Additionally, the gel formulation presented a slower release of both drugs compared to niosomes and SLNs suspensions. CONCLUSION Thermosensitive gels containing clindamycin-loaded niosomes and/or FLZ-SLNs were found to effectively fight the periodontitis-causing bacteria and fungi.
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Affiliation(s)
- Zahra Saeidi
- Department of Pharmaceutics, Faculty of Pharmacy, Shahid Sadoughi University of Medical Sciences and Healthcare Services, Yazd, Iran
| | - Rashin Giti
- Department of Prosthodontics, Faculty of Dentistry, Shiraz University of Medical Sciences, Shiraz, Iran
| | - Azadeh Emami
- Department of Pharmaceutics, Faculty of Pharmacy, Shahid Sadoughi University of Medical Sciences and Healthcare Services, Yazd, Iran
| | - Mehdi Rostami
- Department of Pharmaceutics, Faculty of Pharmacy, Shahid Sadoughi University of Medical Sciences and Healthcare Services, Yazd, Iran
| | - Farhad Mohammadi
- Department of Pharmaceutics, Faculty of Pharmacy, Shahid Sadoughi University of Medical Sciences and Healthcare Services, Yazd, Iran.
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Abdella S, Kim S, Afinjuomo F, Song Y, Upton R, Garg S. Combining the potential of 3D printed buccal films and nanostructured lipid carriers for personalised cannabidiol delivery. Drug Deliv Transl Res 2024; 14:984-1004. [PMID: 37903964 DOI: 10.1007/s13346-023-01446-0] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Accepted: 09/29/2023] [Indexed: 11/01/2023]
Abstract
Cannabidiol (CBD) has been recognized for its numerous therapeutic benefits, such as neuroprotection, anti-inflammatory effects, and cardioprotection. However, CBD has some limitations, including unpredictable pharmacokinetics and low oral bioavailability. To overcome the challenges associated with CBD delivery, we employed Design of Experiments (DoE), lipid carriers, and 3D printing techniques to optimize and develop buccal film loaded with CBD-NLCs. Three-factor Box-Behnken Design was carried out to optimise the NLCs and analyse the effect of independent factors on dependent factors. The emulsification-ultrasonication technique was used to prepare the NLCs. A pressure-assisted micro-syringe printing technique was used to produce the films. The produced films were studied for physicochemical, and mechanical properties, release profiles, and predicted in vivo performance. The observed particle size of the NLCs ranged from 12.17 to 84.91 nm whereas the PDI varied from 0.099 to 0.298. Lipid and sonication time positively affected the particle size whereas the surfactant concentration was inversely related. CBD was incorporated into the optimal formulation and the observed particle size, PDI, and zeta potential for the CBD-NLCs were 94.2 ± 0.47 nm, 0.11 ± 0.01 and - 11.8 ± 0.52 mV. Hydroxyethyl cellulose (HEC)-based gel containing the CBD-NLCs was prepared and used as a feed for 3D printing. The CBD-NLCs film demonstrated a slow and sustained in vitro release profile (84. 11 ± 7.02% in 6 h). The predicted AUC0-10 h, Cmax, and Tmax were 201.5 µg·h/L, 0.74 µg/L, and 1.28 h for a film with 0.4 mg of CBD, respectively. The finding demonstrates that a buccal film of CBD-NLCs can be fabricated using 3D printing.
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Affiliation(s)
- Sadikalmahdi Abdella
- Centre for Pharmaceutical Innovation (CPI), Clinical and Health Sciences, University of South Australia, Adelaide, SA, 5000, Australia
| | - Sangseo Kim
- Centre for Pharmaceutical Innovation (CPI), Clinical and Health Sciences, University of South Australia, Adelaide, SA, 5000, Australia
| | - Franklin Afinjuomo
- Centre for Pharmaceutical Innovation (CPI), Clinical and Health Sciences, University of South Australia, Adelaide, SA, 5000, Australia
| | - Yunmei Song
- Centre for Pharmaceutical Innovation (CPI), Clinical and Health Sciences, University of South Australia, Adelaide, SA, 5000, Australia
| | - Richard Upton
- Centre for Pharmaceutical Innovation (CPI), Clinical and Health Sciences, University of South Australia, Adelaide, SA, 5000, Australia
| | - Sanjay Garg
- Centre for Pharmaceutical Innovation (CPI), Clinical and Health Sciences, University of South Australia, Adelaide, SA, 5000, Australia.
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Saeedi M, Morteza-Semnani K, Akbari J, Hajheydari Z, Goodarzi A, Rostamkalaei SS, Hashemi SMH, Rahimnia SM. Green Formulation of Spironolactone Loaded Chitosan-Coated Nano Lipid Carrier for Treatment of Acne Vulgaris: A Randomized Double-Blind Clinical Trial. Adv Pharm Bull 2024; 14:161-175. [PMID: 38585452 PMCID: PMC10997933 DOI: 10.34172/apb.2024.011] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 04/04/2023] [Revised: 08/18/2023] [Accepted: 09/20/2023] [Indexed: 04/09/2024] Open
Abstract
Purpose Spironolactone (SPN), which is classified as an anti-androgen, has demonstrated efficacy in treating acne. This study aimed to utilize ultrasonication to create a chitosan-coated nano lipid carrier (NLC) for enhancing the delivery of SPN to the skin and treating acne. Methods Various hydrophilic-lipophilic balance (HLB) values were investigated to optimize the SPN-NLCs. Photon correlation spectroscopy, attenuated total reflectance-Fourier transform infrared spectroscopy (ATR-FTIR), transmission electron microscopy (TEM), and differential scanning calorimetry (DSC) were employed to characterize the solid state of SPN in nanoparticle form. Additionally, the optimized formulation was used in a double-blind, randomized clinical trial. Results Reducing the HLB of the surfactant mixtures resulted in a reduction in the size of SPNNLCs. The formula with the smallest particle diameter (238.4±0.74 nm) and the lowest HLB value (9.65) exhibited the highest encapsulation efficiency (EE) of 79.88±1.807%. Coating the optimized SPN-NLC with chitosan increased the diameter, polydispersity index (PDI), zeta potential (ZP), and EE. In vitro skin absorption studies demonstrated sustained release profiles for chitosan-coated SPN-NLC. In the double-blind trial, a gel containing chitosan-coated SPN-NLC effectively treated mild to moderate acne vulgaris, leading to improved healing and reduced lesion count after 8 weeks of therapy compared to the placebo. It successfully addressed both non-inflammatory and inflammatory lesions without adverse effects on the skin. Conclusion The findings indicate that chitosan-coated SPN-NLCs have the potential as nanoparticles for targeted SPN delivery to the skin, offering novel options for the treatment of acne vulgaris.
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Affiliation(s)
- Majid Saeedi
- Pharmaceutical Sciences Research Center, Haemoglobinopathy Institute, Mazandaran University of Medical Sciences, Sari, Iran
- Department of Pharmaceutics, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran
| | - Katayoun Morteza-Semnani
- Department of Medicinal Chemistry, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran
| | - Jafar Akbari
- Department of Pharmaceutics, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran
| | - Zohreh Hajheydari
- Department of Dermatology, Boo Ali Sina (Avicenna) Hospital, Faculty of Medicine, Mazandaran University of Medical Sciences, Sari, Iran
| | - Amin Goodarzi
- Student Research Committee, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran
| | - Seyyed Sohrab Rostamkalaei
- Department of Pharmaceutics, Faculty of Pharmacy, Ayatollah Amoli Branch, Islamic Azad University, Amol, Iran
| | | | - Seyyed Mobin Rahimnia
- Department of Pharmaceutics, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran
- Student Research Committee, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran
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Aydin BS, Sagiroglu AA, Ozturk Civelek D, Gokce M, Bahadori F. Development of Curcumin and Turmerone Loaded Solid Lipid Nanoparticle for Topical Delivery: Optimization, Characterization and Skin Irritation Evaluation with 3D Tissue Model. Int J Nanomedicine 2024; 19:1951-1966. [PMID: 38435752 PMCID: PMC10907133 DOI: 10.2147/ijn.s453347] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 12/05/2023] [Accepted: 02/16/2024] [Indexed: 03/05/2024] Open
Abstract
Background Curcuma longa L., commonly known as turmeric, is renowned for its therapeutic benefits attributed to bioactive compounds, namely curcumin (Cur) and aromatic turmerone (Tur), present in its rhizome. These compounds exhibit diverse therapeutic properties, including anti-inflammatory, antioxidant, and anti-tumor effects. However, the topical application of these compounds has a significant potential for inducing skin irritation. This study focuses on formulating solid lipid nanoparticle (SLN) carriers encapsulating both Cur and Tur for reduced irritation and enhanced stability. Methods SLN formulations were prepared by a method using homogenization followed by ultrasonication procedures and optimized by applying response surface methodology (RSM). Results The optimized SLN formulation demonstrated entrapment efficiencies, with 77.21 ± 4.28% for Cur and 75.12 ± 2.51% for Tur. A size distribution of 292.11 ± 9.43 nm was obtained, which was confirmed to be a spherical and uniform shape via environmental scanning electron microscopy (ESEM) images. The in vitro release study indicated cumulative releases of 71.32 ± 3.73% for Cur and 67.23 ± 1.64% for Tur after 24 hours under sink conditions. Physical stability tests confirmed the stability of formulation, allowing storage at 4°C for a minimum of 60 days. Notably, in vitro skin irritation studies, utilizing the reconstructed human epidermal model (EPI-200-SIT), revealed a significant reduction in irritation with the SLN containing Cur and Tur compared to nonencapsulated Cur and Tur. Conclusion These findings collectively endorse the optimized SLN formulation as a favorable delivery system for Cur and Tur in diverse topical uses, offering enhanced stability, controlled release and reduced irritation.
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Affiliation(s)
- Beyza Sümeyye Aydin
- Bezmialem Vakif University, Health Sciences Institute, Department of Biotechnology, Istanbul, 34093, Turkey
| | - Ali Asram Sagiroglu
- Istanbul University-Cerrahpasa, Faculty of Pharmacy, Department of Pharmaceutical Technology, Istanbul, 34500, Turkey
- Bezmialem Vakif University, Faculty of Pharmacy, Department of Pharmaceutical Technology, Istanbul, 34093, Turkey
| | - Dilek Ozturk Civelek
- Bezmialem Vakif University, Faculty of Pharmacy, Department of Pharmacology, Istanbul, 34093, Türkiye
| | - Mustafa Gokce
- Bezmialem Vakif University, Faculty of Pharmacy, Department of Pharmacology, Istanbul, 34093, Türkiye
| | - Fatemeh Bahadori
- Istanbul University-Cerrahpasa, Faculty of Pharmacy, Department of Analytical Chemistry, Istanbul, 34500, Turkey
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Chen L, Guo W, Mao C, Shen J, Wan M. Liver fibrosis: pathological features, clinical treatment and application of therapeutic nanoagents. J Mater Chem B 2024; 12:1446-1466. [PMID: 38265305 DOI: 10.1039/d3tb02790b] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [MESH Headings] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 01/25/2024]
Abstract
Liver fibrosis is a reversible damage-repair response, the pathological features of which mainly include damage to hepatocytes, sinusoid capillarization, hepatic stellate cells activation, excessive accumulation of extracellular matrix and inflammatory response. Although some treatments (including drugs and stem cell therapy) for these pathological features have been shown to be effective, more clinical trials are needed to confirm their effectiveness. In recent years, nanomaterials-based therapies have emerged as an innovative and promising alternative to traditional drugs, being explored for the treatment of liver fibrosis diseases. Natural nanomaterials (including extracellular vesicles) and synthetic nanomaterials (including inorganic nanomaterials and organic nanomaterials) are developed to facilitate drug targeting delivery and combination therapy. In this review, the pathological features of liver fibrosis and the current anti-fibrosis drugs in clinical trials are briefly introduced, followed by a detailed introduction of the therapeutic nanoagents for the precise delivery of anti-fibrosis drugs. Finally, the future development trend in this field is discussed.
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Affiliation(s)
- Lin Chen
- National and Local Joint Engineering Research Center of Biomedical Functional Materials, School of Chemistry and Materials Science, Nanjing Normal University, Nanjing 210023, China.
| | - Wenyan Guo
- National and Local Joint Engineering Research Center of Biomedical Functional Materials, School of Chemistry and Materials Science, Nanjing Normal University, Nanjing 210023, China.
| | - Chun Mao
- National and Local Joint Engineering Research Center of Biomedical Functional Materials, School of Chemistry and Materials Science, Nanjing Normal University, Nanjing 210023, China.
| | - Jian Shen
- National and Local Joint Engineering Research Center of Biomedical Functional Materials, School of Chemistry and Materials Science, Nanjing Normal University, Nanjing 210023, China.
| | - Mimi Wan
- National and Local Joint Engineering Research Center of Biomedical Functional Materials, School of Chemistry and Materials Science, Nanjing Normal University, Nanjing 210023, China.
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Flieger J, Raszewska-Famielec M, Radzikowska-Büchner E, Flieger W. Skin Protection by Carotenoid Pigments. Int J Mol Sci 2024; 25:1431. [PMID: 38338710 PMCID: PMC10855854 DOI: 10.3390/ijms25031431] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 12/18/2023] [Revised: 01/19/2024] [Accepted: 01/22/2024] [Indexed: 02/12/2024] Open
Abstract
Sunlight, despite its benefits, can pose a threat to the skin, which is a natural protective barrier. Phototoxicity caused by overexposure, especially to ultraviolet radiation (UVR), results in burns, accelerates photoaging, and causes skin cancer formation. Natural substances of plant origin, i.e., polyphenols, flavonoids, and photosynthetic pigments, can protect the skin against the effects of radiation, acting not only as photoprotectors like natural filters but as antioxidant and anti-inflammatory remedies, alleviating the effects of photodamage to the skin. Plant-based formulations are gaining popularity as an attractive alternative to synthetic filters. Over the past 20 years, a large number of studies have been published to assess the photoprotective effects of natural plant products, primarily through their antioxidant, antimutagenic, and anti-immunosuppressive activities. This review selects the most important data on skin photodamage and photoprotective efficacy of selected plant carotenoid representatives from in vivo studies on animal models and humans, as well as in vitro experiments performed on fibroblast and keratinocyte cell lines. Recent research on carotenoids associated with lipid nanoparticles, nanoemulsions, liposomes, and micelles is reviewed. The focus was on collecting those nanomaterials that serve to improve the bioavailability and stability of carotenoids as natural antioxidants with photoprotective activity.
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Affiliation(s)
- Jolanta Flieger
- Department of Analytical Chemistry, Medical University of Lublin, Chodźki 4A, 20-093 Lublin, Poland
| | - Magdalena Raszewska-Famielec
- Faculty of Physical Education and Health, University of Physicl Education, Akademicka 2, 21-500 Biała Podlaska, Poland;
| | - Elżbieta Radzikowska-Büchner
- Department of Plastic, Reconstructive and Maxillary Surgery, National Medical Institute of the Ministry of the Interior and Administration, Wołoska 137 Street, 02-507 Warszawa, Poland;
| | - Wojciech Flieger
- Chair and Department of Anatomy, Medical University of Lublin, K. Jaczewskiego 4, 20-090 Lublin, Poland;
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Leon MM, Maștaleru A, Oancea A, Alexa-Stratulat T, Peptu CA, Tamba BI, Harabagiu V, Grosu C, Alexa AI, Cojocaru E. Lidocaine-Liposomes-A Promising Frontier for Transdermal Pain Management. J Clin Med 2024; 13:271. [PMID: 38202278 PMCID: PMC10779996 DOI: 10.3390/jcm13010271] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [Grants] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 11/15/2023] [Revised: 12/16/2023] [Accepted: 12/25/2023] [Indexed: 01/12/2024] Open
Abstract
(1) Background: We aim to develop novel gel formulations for transdermal drug delivery systems in acute and inflammatory pain therapy. (2) Methods: We induced inflammation by the injection of λ-carrageenan on the hind paw of 80 Wistar male rats. The animals were randomized into eight groups of 10 rats each: C (placebo gel), E (EMLATM), L (lidocaine 2%), L-CD (lidocaine + cyclodextrin 2.5%), L-LP (lidocaine + liposomes 1.7%), L-CS (lidocaine + chitosan 4%), L-CSh (lidocaine + chitosan hydrochloride), and L-CS-LP (lidocaine + chitosan + liposomes). The behavior response was determined with a hot plate, cold plate, and algesimeter, each being performed at 30, 60, 120, 180, and 240 min after pain induction. At the end of the experiment, tissue samples were collected for histological assessment. (3) Results: L-LP had the greatest anesthetic effects, which was proven on the cold plate test compared to placebo and EMLATM (all p ≤ 0.001). L-CS-LP had a significant effect on cold plate evaluation compared to placebo (p ≤ 0.001) and on hot plate evaluation compared to EMLATM (p = 0.018). (4) Conclusions: L-LP is a new substance with a substantial analgesic effect demonstrated by the cold plate in the first 120 min. Further studies with more animals are needed to determine the maximum doses that can be applied for a better analgesia with minimum side effects.
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Affiliation(s)
- Maria Magdalena Leon
- Department of Medical Specialties I, “Grigore T. Popa” University of Medicine and Pharmacy, 700115 Iaşi, Romania;
| | - Alexandra Maștaleru
- Department of Medical Specialties I, “Grigore T. Popa” University of Medicine and Pharmacy, 700115 Iaşi, Romania;
| | - Andra Oancea
- Department of Medical Specialties I, “Grigore T. Popa” University of Medicine and Pharmacy, 700115 Iaşi, Romania;
| | - Teodora Alexa-Stratulat
- Department of Medical Oncology–Radiotherapy, Faculty of Medicine, “Grigore T. Popa” University of Medicine and Pharmacy, 700115 Iaşi, Romania;
| | - Cătălina Anișoara Peptu
- Department of Natural and Synthetic Polymers, Faculty of Chemical Engineering and Environmental Protection, “Gheorghe Asachi” Technical University of Iasi, 700050 Iasi, Romania;
| | - Bogdan-Ionel Tamba
- CEMEX Laboratory, “Grigore T. Popa” University of Medicine and Pharmacy, 700259 Iaşi, Romania;
| | - Valeria Harabagiu
- “Petru Poni” Institute of Macromolecular Chemistry, 700487 Iaşi, Romania;
| | - Cristina Grosu
- Department of Medical Specialties III, “Grigore T. Popa” University of Medicine and Pharmacy, 700115 Iaşi, Romania;
| | - Anisia Iuliana Alexa
- Department of Surgery II, Discipline of Ophthalmology, “Grigore T. Popa” University of Medicine and Pharmacy, 700115 Iasi, Romania;
| | - Elena Cojocaru
- Department of Morphofunctional Sciences I, “Grigore T. Popa” University of Medicine and Pharmacy, 700115 Iaşi, Romania;
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Khil NHS, Sharma S, Sharma PK, Alam A. Several Applications of Solid Lipid Nanoparticles in Drug Delivery. Curr Mol Med 2024; 24:1077-1090. [PMID: 37475554 DOI: 10.2174/1566524023666230720110351] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 11/30/2022] [Revised: 04/12/2023] [Accepted: 05/08/2023] [Indexed: 07/22/2023]
Abstract
Rapid progress is being made in the area of nanotechnology; solid lipid nanoparticles are currently at the forefront of research and development. They have the capability of becoming employed in an extensive number of applications, including the delivery of medications, clinical treatment, and research, in addition to uses in other areas of academic inquiry that could benefit from their utilisation. This article presents a thorough analysis of solid lipid nanoparticles, covering subjects such as their goals, preparation strategy, applications, advantages, and possible remedies for the issues that have been raised. This review provides a discussion of solid lipids that is both in-depth and comprehensive. Studies that investigate the manner in which SLNs are prepared and the routes via which they are administered are typical. Aspects concerning the route of administration of SLNs as well as the destiny of the carriers in vivo are also investigated in this paper.
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Affiliation(s)
| | - Shaweta Sharma
- Department of Pharmacy, School of Medical & Allied Sciences, Greater Noida, Uttar Pradesh, India
| | - Pramod Kumar Sharma
- Department of Pharmacy, School of Medical & Allied Sciences, Greater Noida, Uttar Pradesh, India
| | - Aftab Alam
- Department of Pharmacy, School of Medical & Allied Sciences, Greater Noida, Uttar Pradesh, India
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Manandhar B, Paudel KR, Clarence DD, De Rubis G, Madheswaran T, Panneerselvam J, Zacconi FC, Williams KA, Pont LG, Warkiani ME, MacLoughlin R, Oliver BG, Gupta G, Singh SK, Chellappan DK, Hansbro PM, Dua K. Zerumbone-incorporated liquid crystalline nanoparticles inhibit proliferation and migration of non-small-cell lung cancer in vitro. NAUNYN-SCHMIEDEBERG'S ARCHIVES OF PHARMACOLOGY 2024; 397:343-356. [PMID: 37439806 PMCID: PMC10771618 DOI: 10.1007/s00210-023-02603-5] [Citation(s) in RCA: 6] [Impact Index Per Article: 6.0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Grants] [Track Full Text] [Subscribe] [Scholar Register] [Received: 05/14/2023] [Accepted: 06/25/2023] [Indexed: 07/14/2023]
Abstract
Lung cancer is the second most prevalent type of cancer and is responsible for the highest number of cancer-related deaths worldwide. Non-small-cell lung cancer (NSCLC) makes up the majority of lung cancer cases. Zerumbone (ZER) is natural compound commonly found in the roots of Zingiber zerumbet which has recently demonstrated anti-cancer activity in both in vitro and in vivo studies. Despite their medical benefits, ZER has low aqueous solubility, poor GI absorption and oral bioavailability that hinders its effectiveness. Liquid crystalline nanoparticles (LCNs) are novel drug delivery carrier that have tuneable characteristics to enhance and ease the delivery of bioactive compounds. This study aimed to formulate ZER-loaded LCNs and investigate their effectiveness against NSCLC in vitro using A549 lung cancer cells. ZER-LCNs, prepared in the study, inhibited the proliferation and migration of A549 cells. These inhibitory effects were superior to the effects of ZER alone at a concentration 10 times lower than that of free ZER, demonstrating a potent anti-cancer activity of ZER-LCNs. The underlying mechanisms of the anti-cancer effects by ZER-LCNs were associated with the transcriptional regulation of tumor suppressor genes P53 and PTEN, and metastasis-associated gene KRT18. The protein array data showed downregulation of several proliferation associated proteins such as AXL, HER1, PGRN, and BIRC5 and metastasis-associated proteins such as DKK1, CAPG, CTSS, CTSB, CTSD, and PLAU. This study provides evidence of potential for increasing the potency and effectiveness of ZER with LCN formulation and developing ZER-LCNs as a treatment strategy for mitigation and treatment of NSCLC.
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Affiliation(s)
- Bikash Manandhar
- Discipline of Pharmacy, Graduate School of Health, University of Technology Sydney, Sydney, NSW, 2007, Australia
- Australian Research Centre in Complementary and Integrative Medicine, Faculty of Health, University of Technology Sydney, Sydney, NSW, 2007, Australia
| | - Keshav Raj Paudel
- Centre for Inflammation, Centenary Institute and University of Technology Sydney, Faculty of Science, School of Life Sciences, Sydney, NSW 2050, Australia
| | - Dvya Delilaa Clarence
- School of Postgraduate Studies, International Medical University (IMU), 57000, Kuala Lumpur, Malaysia
| | - Gabriele De Rubis
- Discipline of Pharmacy, Graduate School of Health, University of Technology Sydney, Sydney, NSW, 2007, Australia
- Australian Research Centre in Complementary and Integrative Medicine, Faculty of Health, University of Technology Sydney, Sydney, NSW, 2007, Australia
| | - Thiagarajan Madheswaran
- Department of Pharmaceutical Technology, School of Pharmacy, International Medical University, 57000, Kuala Lumpur, Malaysia
| | - Jithendra Panneerselvam
- Department of Pharmaceutical Technology, School of Pharmacy, International Medical University, 57000, Kuala Lumpur, Malaysia
| | - Flavia C Zacconi
- Departamento de Química Orgánica, Facultad de Química y de Farmacia, Pontificia Universidad Católica de Chile, Av. Vicuña Mackenna 4860, 7820436, Macul, Santiago, Chile
- Centro de Investigación en Nanotecnología y Materiales Avanzados, CIEN-UC, Pontificia Universidad Católica de Chile, Av. Vicuña Mackenna 4860, 7820436, Macul, Santiago, Chile
- Institute for Biological and Medical Engineering, Schools of Engineering, Medicine and Biological Sciences, Pontificia Universidad Católica de Chile, Santiago, Chile
| | - Kylie A Williams
- Discipline of Pharmacy, Graduate School of Health, University of Technology Sydney, Sydney, NSW, 2007, Australia
| | - Lisa G Pont
- Discipline of Pharmacy, Graduate School of Health, University of Technology Sydney, Sydney, NSW, 2007, Australia
| | - Majid Ebrahimi Warkiani
- School of Biomedical Engineering, University of Technology Sydney, Sydney, New South Wales, Australia
- Institute for Biomedical Materials and Devices, Faculty of Science, University of Technology Sydney, Sydney, New South Wales, Australia
| | - Ronan MacLoughlin
- Research and Development, Aerogen Limited, IDA Business Park, Galway, Connacht, H91 HE94, Ireland
- School of Pharmacy & Biomolecular Sciences, Royal College of Surgeons in Ireland, Dublin, Leinster, D02 YN77, Ireland
- School of Pharmacy & Pharmaceutical Sciences, Trinity College, Dublin, Leinster, D02 PN40, Ireland
| | - Brian Gregory Oliver
- Woolcock Institute of Medical Research, Macquarie University, Sydney, NSW, 2137, Australia
- School of Life Sciences, Faculty of Science, University of Technology Sydney, Sydney, NSW, 2007, Australia
| | - Gaurav Gupta
- School of Pharmacy, Suresh Gyan Vihar University, Jaipur, Rajasthan, India
- Center for Transdisciplinary Research, Saveetha Institute of Medical and Technical Science, Saveetha University, Chennai, India
| | - Sachin Kumar Singh
- Australian Research Centre in Complementary and Integrative Medicine, Faculty of Health, University of Technology Sydney, Sydney, NSW, 2007, Australia
- School of Pharmaceutical Sciences, Lovely Professional University, Jalandhar-Delhi G.T Road, Phagwara, 144411, India
| | - Dinesh Kumar Chellappan
- Department of Life Sciences, School of Pharmacy, International Medical University, 57000, Kuala Lumpur, Malaysia.
| | - Philip M Hansbro
- Centre for Inflammation, Centenary Institute and University of Technology Sydney, Faculty of Science, School of Life Sciences, Sydney, NSW 2050, Australia.
| | - Kamal Dua
- Discipline of Pharmacy, Graduate School of Health, University of Technology Sydney, Sydney, NSW, 2007, Australia.
- Australian Research Centre in Complementary and Integrative Medicine, Faculty of Health, University of Technology Sydney, Sydney, NSW, 2007, Australia.
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47
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Sheoran S, Arora S, Velingkar A, Pawar SC, Vuree S. Empowering treatment strategies for pancreatic cancer by employing lipid nanoparticle-driven drug delivery. RECENT ADVANCES IN NANOCARRIERS FOR PANCREATIC CANCER THERAPY 2024:239-266. [DOI: 10.1016/b978-0-443-19142-8.00016-4] [Citation(s) in RCA: 1] [Impact Index Per Article: 1.0] [Reference Citation Analysis] [Track Full Text] [Subscribe] [Scholar Register] [Indexed: 01/02/2025]
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48
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Rani S, Dey P, Pruthi K, Singh S, Mahajan S, Alajangi HK, Kapoor S, Pandey A, Gupta D, Barnwal RP, Singh G. Nanotechnology-Based Approaches for Cosmeceutical and Skin Care: A Systematic Review. Crit Rev Ther Drug Carrier Syst 2024; 41:65-110. [PMID: 38608133 DOI: 10.1615/critrevtherdrugcarriersyst.v41.i5.20] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [MESH Headings] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 04/14/2024]
Abstract
Cosmeceuticals have gained great importance and are among the top-selling products used for skin care. Because of changing lifestyles, climate, and increasing pollution, cosmeceuticals are utilized by every individual, thereby making cosmeceuticals a fruitful field for research and the economy. Cosmeceuticals provide incredibly pleasing aesthetic results by fusing the qualities of both cosmetics and medicinal substances. Cosmeceuticals are primarily utilized to improve the appearance of skin by making it smoother, moisturized, and wrinkle-free, in addition to treating dermatological conditions, including photoaging, burns, dandruff, acne, eczema, and erythema. Nanocosmeceuticals are cosmetic products that combine therapeutic effects utilizing nanotechnology, allowing for more precise and effective target-specific delivery of active ingredients, and improving bioavailability.
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Affiliation(s)
- Shital Rani
- Department of Biophysics, Panjab University, Chandigarh, India
| | - Piyush Dey
- Department of Biophysics, Panjab University, Chandigarh, India; University Institute of Pharmaceutical Sciences (UIPS), Panjab University, Chandigarh, India
| | - Kritika Pruthi
- University Institute of Pharmaceutical Sciences (UIPS), Panjab University, Chandigarh, India
| | - Sahajdeep Singh
- University Institute of Pharmaceutical Sciences (UIPS), Panjab University, Chandigarh, India
| | - Shivansh Mahajan
- University Institute of Pharmaceutical Sciences (UIPS), Panjab University, Chandigarh, India
| | - Hema K Alajangi
- University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, 160014, India; Department of Biophysics, Panjab University, Chandigarh, 160014, India
| | - Sumeet Kapoor
- Centre for Biomedical Engineering, Indian Institute of Technology, New Delhi, India
| | - Ankur Pandey
- Department of Chemistry, Panjab University, Chandigarh India
| | - Dikshi Gupta
- Centre for Biomedical Engineering, Indian Institute of Technology, New Delhi, India
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49
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Zhang T, Luo X, Xu K, Zhong W. Peptide-containing nanoformulations: Skin barrier penetration and activity contribution. Adv Drug Deliv Rev 2023; 203:115139. [PMID: 37951358 DOI: 10.1016/j.addr.2023.115139] [Citation(s) in RCA: 3] [Impact Index Per Article: 1.5] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 08/31/2023] [Revised: 10/21/2023] [Accepted: 11/08/2023] [Indexed: 11/14/2023]
Abstract
Transdermal drug delivery presents a less invasive pathway, circumventing the need to pass through the gastrointestinal tract and liver, thereby reducing drug breakdown, initial metabolism, and gastrointestinal discomfort. Nevertheless, the unique composition and dense structure of the stratum corneum present a significant barrier to transdermal delivery. This article presents an overview of the current developments in peptides and nanotechnology to address this challenge. Initially, we sum up peptide-containing nanoformulations for transdermal drug delivery, examining them through the lenses of both inorganic and organic materials. Particular emphasis is placed on the diverse roles that peptides play within these nanoformulations, including conferring functionality upon nanocarriers and enhancing the biological efficacy of drugs. Subsequently, we summarize innovative strategies for enhancing skin penetration, categorizing them into passive and active approaches. Lastly, we discuss the therapeutic potential of peptide-containing nanoformulations in addressing a range of diseases, drawing insights from the biological activities and functions of peptides. Furthermore, the challenges hindering clinical translation are also discussed, providing valuable insights for future advancements in transdermal drug delivery.
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Affiliation(s)
- Tingting Zhang
- Department of Chemistry, China Pharmaceutical University, Nanjing 210009, China
| | - Xuan Luo
- Department of Chemistry, China Pharmaceutical University, Nanjing 210009, China
| | - Keming Xu
- Department of Chemistry, China Pharmaceutical University, Nanjing 210009, China; Key Laboratory of Biomedical Functional Materials, China Pharmaceutical University, Nanjing 210009, China.
| | - Wenying Zhong
- Department of Chemistry, China Pharmaceutical University, Nanjing 210009, China; Key Laboratory of Biomedical Functional Materials, China Pharmaceutical University, Nanjing 210009, China; Key Laboratory of Drug Quality Control and Pharmacovigilance, China Pharmaceutical University, Nanjing 210009, China.
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50
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Uner B, Macit Celebi MS. Anti-obesity effects of chlorogenic acid and caffeine- lipid nanoparticles through PPAR-γ/C/EBP-ɑ pathways. Int J Obes (Lond) 2023; 47:1108-1119. [PMID: 37596386 DOI: 10.1038/s41366-023-01365-7] [Citation(s) in RCA: 7] [Impact Index Per Article: 3.5] [Reference Citation Analysis] [Abstract] [MESH Headings] [Track Full Text] [Journal Information] [Submit a Manuscript] [Subscribe] [Scholar Register] [Received: 04/03/2023] [Revised: 07/21/2023] [Accepted: 08/09/2023] [Indexed: 08/20/2023]
Abstract
Obesity is considered one of the most crucial health problems of the century. Therefore, reducing obesity is critically important. Caffeine (CF) and chlorogenic acid (CLA), which are substantial components in green bean coffee which maximize thermogenesis in brown adipose tissue. In our study, we have prepared CF, CLA, and CF + CLA loaded-solid lipid nanoparticles (SLN) since the SLNs are cost-effective, tissue-localized, and highly stable. The central composite design model was preferred to select the optimized formulation. UHPLC was used for quantification related to the CF and CLA amounts. The high-pressure homogenization (HPH) method was used while SLN formulations were prepared in the presence of poloxamer® 407 (surfactant) and Compritol® 888 ATO (solid lipid). The nanoparticles were characterized, followed by the utilization of 3T3-F442A cell lines for the evaluation of the adipogenesis activity of the formulations. Then, rt-PCR and ELISA studies of adipogenic markers were conducted. After optimal formulations were selected with an average of 110.2 ± 0.1 nm, CF (1 mM) + CLA (0.5 mM)-loaded SLN formulation has been proven significantly effective by using PPAR-γ/C/EBP-a pathways. In a nutshell, our study has shown that CF + CLA loaded-SLN has been affected 45.8% times more than regular extracted coffee (p < 0.05) on the adipocyte cells.
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Affiliation(s)
- Burcu Uner
- Department of Pharmaceutical and Administrative Sciences, University of Health Science and Pharmacy in St Louis, St. Louis, MO, USA.
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