Lactosamination of liposomes and hepatotropic targeting research

Table 1 Tissue distribution of ¹³¹I-labeled L-HSA-liposomes in rat

Rat No.	Tissue distribution in vivo (cpm per gram tissue)
	Liver	Spleena	Kidneyb	Heartc	Lungd
1	31777.2	15394.2	7912.1	4427.5	9568.5
2	30476.1	15464.1	5424.5	3180.8	6044.1
3	30013.1	14041.4	7932.3	3777.5	5886.1
4	36099.3	10817.5	6372.3	3722.7	8717.3
5	36479.8	17882.6	7228.6	3885.5	7695.8
Average	32969.1	14719.9	6974.1	3798.8	7582.4

¹³¹I labeled L-HSA-liposomes were injected into rats. Radioactivity in different tissues was determined 40 min after injection as described in Materials and Methods. Compared with liver:

^aP = 7.84 × 10^-6;

^bP = 1.06 × 10^-7;

^cP = 2.98 × 10^-8;

^dP = 2.1 × 10^-7

Table 2 Tissue distribution of ¹³¹I labeled L-HSA-liposomes in rat, after L-HSA pre-injection

Rat No.	Tissue distribution in vivo (cpm per gram tissue)
	Liver	Spleena	Kidneyb	Heartc	Lungd
1	34682.0	35187.6	5535.7	2474.2	6368.0
2	20587.4	19791.1	4541.8	2277.2	8507.7
3	24288.8	27297.1	4564.4	2089.5	7280.7
4	33733.1	17637.5	5560.3	2698.3	12561.1
5	25600.9	18994.5	6999.2	3227.0	11087.1
Average	27778.4	23781.6	7699.1	2553.2	8679.4

Fifteen min after L-HAS pre-injection, ¹³¹I labeled L-HSA-liposomes were injected into rats. Radioactivity in different tissues was determined 40 min af ter injection as described in Materials and methods. Compared with liver:

^aP = 0.38;

^bP = 4.35 × 10^-5;

^cP = 1.66 × 10^-5;

^dP = 2.52 × 10^-4

Table 3 Inhibitory effect on HBeAg expression in 2.2.15 cells of di fferent types of interferons

Treatment	Inhibitory effect on HBeAg expression (%)
	3 days	6 days	9 days	12 days
Liposomes	0	1.8	0	0
L-HSA-Liposomes	0	0	0	0
IFN 0.08 MUa	0	4.7	12.7	2.3
CL-IFN 0.08 MUb	0	0	22.8	5.8
LL-IFN 0.08 MU	44.8	60.7	43.5	45.5
LL-IFN 0.04 MU	6.8	47.4	28.6	12.1
LL-IFN 0.02 MU	0	24.6	23.8	4.6
LL-IFN 0.01 MU	0	4.8	15.4	5.2

IFN: interferon; CL-IFN: interferon entraped in conventional liposomes; LL-IFN: interferon entraped in L-HSA-liposomes. Compared with LL-IFN 0.08 MU:

^aP = 0.003,

^bP = 0.015