盐酸青藤碱醇质体的制备及其体外经皮渗透研究

目的制备盐酸青藤碱醇质体并考察醇质体作为盐酸青藤碱经皮给药载体的渗透特性。方法采用注入法制备盐酸青藤碱醇质体,并对其形态、粒径及包封率进行分析;采用透皮扩散仪,以小鼠皮肤进行体外透皮试验,比较盐酸青藤碱在水溶液、脂质体以及醇质体中的透皮行为。结果制得的盐酸青藤碱醇质体外形圆整,平均粒径为88.7 nm,包封率为62.8%,累积透皮量和透皮速率均明显高于盐酸青藤碱脂质体和水溶液。结论醇质体能明显促进盐酸青藤碱的经皮渗透,有望成为盐酸青藤碱透皮给药的新载体。

Sinomenine hydrochloride ethosome preparation and its transdermal penetration

Objective To prepare sinomenine hydrochloride ethosome and evaluate the transdermal penetration of sinomenine hydrochloride taking ethosome as carrier.Methods Sinomenine hydrochloride ethosome was prepared with injection method and its appearance,particle size,and entrapment efficiency(EE) were analyzed.In transdermal test of mice,the transdermal behavior and accumulated permeation amounts of sinomenine hydrochloride in ethosome,liposomes,and water solution were compared by using Franz diffusion device.Results The shape of the sinomenine hydrochloride ethosome was spherical in an average diameter of 88.7 nm and the EE was 62.8%.The accumulated permeation amounts and permeation rates were significantly higher than those in liposomes and water solution.Conclusion The ethosome could greatly improve the transdermal penetration of sinomenine hydrochloride and it may be a potential carrier for transdermal use.