Study on liver targeting 5-fluorouracil solid lipid nanoparticles

doi:10.3748/wjg.v6.iSuppl3.112

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World Journal of Gastroenterology

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1007-9327

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Baishideng Publishing Group Inc, 7041 Koll Center Parkway, Suite 160, Pleasanton, CA 94566, USA

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World J Gastroenterol. Sep 15, 2000; 6(Suppl3): 112-112
Published online Sep 15, 2000. doi: 10.3748/wjg.v6.iSuppl3.112

Study on liver targeting 5-fluorouracil solid lipid nanoparticles

Zhi-Rong Zhang, Bo-Tao Yu

Zhi-Rong Zhang, School of Pharmacy, West China University of Medical Sciences, Chengdu 610041, Sichuan Province, China

Bo-Tao Yu, General Hospital of Chengdu Command, Chengdu 610083, Sichuan Province, China

Author contributions: All authors contributed equally to the work.

Supported by the National Outstanding Youth Foundation of China, No. 39925039

Correspondence to: Dr. Zhi-Rong Zhang, Professor, School of Pharmacy, West China University of Medical Sciences, Chengdu 610041, Sichuan Province, China. zrzzl@mail.sc.coinfo.net

Telephone: 28-5501566 Fax: 28-5583252

Received: January 10, 2000
Revised: June 2, 2000
Accepted: July 10, 2000
Published online: September 15, 2000

Abstract

AIM: To prepare 5-fluorouracil solid lipid nanoparticles (5-FuE-SLN) with liver targeting.

METHODS: 5-Fu was employed as model drug to acylate with stearyl chloride and obtain 5-Fu precurser N1-stearyl-5-Fu (5-FuE). The precurser was determined by nuclear magnetic resonance and infrared spectrometry and used to prepare 5-FuE-SLN by the method of physical agglomeration. Transmission Electron Microscopy (TEM) was employed to study the shape, mean size and particle distribution of 5-FuE-SLN. The drug loading, and releasing characteristics in vivo, the drug distribution and pharmacokinetics in vivo were also investigated by HPLC method.

RESULTS: The average diameter was 240.19 nm, and the drug loading was 20.53%. The releasing characteristics in vivo was fitted to first-order pharmacokinetic model. The distribution of 5-FuE-SLN in mice showed that 5-FuE-SLN had significant liver targeting being compared with 5-Fu injection. The concentration of 5-FuE-SLN group in mice liver was double over that of control group. The main pharmacokinetics parameters in rabbits were as follows: Vc = 0.04336 L·kg^-1, T_1/2β - 1.2834 h, CL = 0.1632 L·h^-1.

CONCLUSION: 5-FuE-SLN has the characteristic of liver targeting. Using 5-Fu precurser to enhance its liposoluble properties and the method of preparation presented in this paper seems to have significant advantages and important reference value.

Key Words: Liver; Fluorouracil; Solid lipid nanoparticles; Frug delivery systems; Pharmacokinetics

Citation: Zhang ZR, Yu BT. Study on liver targeting 5-fluorouracil solid lipid nanoparticles. World J Gastroenterol 2000; 6(Suppl3): 112-112
URL: https://www.wjgnet.com/1007-9327/full/v6/iSuppl3/112.htm
DOI: https://dx.doi.org/10.3748/wjg.v6.iSuppl3.112

Footnotes

E- Editor: Hu S