Wu Zheng-hong, Ping Qi-neng, Wei Yi, Lai Jia-ming
Department of Pharmaceutics, China Pharmaceutical University, Nanjing 210009, China.
Acta Pharmacol Sin. 2004 Jul;25(7):966-72.
To evaluate the hypoglycemic efficacy of insulin liposomes coated by chitosan with different molecular weights and concentrations after oral administration in mice.
Insulin-liposomes were prepared by reversed-phase evaporation. Chitosan coating was carried out by incubation of the liposomal suspensions with the chitosan solution. The hypoglycemic efficacies of chitosan-coated insulin liposomes were investigated by monitoring the blood glucose level using the glucose oxidase method after oral administration to healthy mice.
In all the insulin liposomes, the insulin liposomes coated by 0.2% chitosan (Mr 1000 kDa) showed a better hypoglycemic efficacy as compared with the other liposomes coated by chitosan. The minimum blood glucose level was 15.1%+/-6.0 % of the initial (n=6). The hypoglycemic efficacy lasted for 4 h after oral administration to mice.
Chitosan-coated liposomes could reduce tryptic digestion on insulin, and enhance enteral absorption of insulin. The molecular weights and concentrations of chitosan had significant effects on hypoglycemic efficacy of chitosan-coated insulin liposomes after oral administration to healthy mice.
评估不同分子量和浓度的壳聚糖包衣胰岛素脂质体经口服给药后在小鼠体内的降血糖效果。
采用逆相蒸发法制备胰岛素脂质体。通过将脂质体悬浮液与壳聚糖溶液孵育进行壳聚糖包衣。对健康小鼠口服给药后,采用葡萄糖氧化酶法监测血糖水平,研究壳聚糖包衣胰岛素脂质体的降血糖效果。
在所有胰岛素脂质体中,与其他壳聚糖包衣的脂质体相比,用0.2%壳聚糖(分子量1000 kDa)包衣的胰岛素脂质体显示出更好的降血糖效果。最低血糖水平为初始值的15.1%±6.0%(n = 6)。给小鼠口服给药后,降血糖效果持续4小时。
壳聚糖包衣脂质体可减少胰岛素的胰蛋白酶消化,并增强胰岛素的肠道吸收。壳聚糖的分子量和浓度对健康小鼠口服给药后壳聚糖包衣胰岛素脂质体的降血糖效果有显著影响。