秋水仙碱醇质体的制备及体外经皮渗透研究

Preparation and Transdermal Penetration of Colchicines Ethosomes in Vitro

目的制备秋水仙碱醇质体并考察醇质体作为秋水仙碱经皮给药载体的可行性。方法采用注入法制备秋水仙碱醇质体,紫外法测定其包封率,并以包封率为指标,利用正交试验法优化处方和制备工艺;采用TYJ-6A型透皮扩散实验仪,用小鼠腹部皮肤进行体外经皮渗透实验;比较不同给药形式对秋水仙碱经皮渗透的影响。结果最佳处方为乙醇3.3mL,豆磷脂0.25g和秋水仙碱0.025g,用注入法注入4min即可,包封率达57.0%。秋水仙碱醇质体的经皮渗透速率(6.54μg·cm-2·h-1)是水溶液的5.59倍,是普通脂质体的3.14倍,是体积分数为30%乙醇溶液的1.24倍。10h后皮肤中药物的滞留量大小顺序为:醇质体>体积分数为30%乙醇溶液>普通脂质体>饱和水溶液。结论醇质体能提高秋水仙碱的透皮速率,增加药物在皮肤中的滞留量。

OBJECTIVE To prepare ethosomes and investigate the feasibility ofethosome as transdermal carries ofcolchicines METHODS Colchicine ethosomes were prepared by injection method, served as quota with encapsulation efficiency of ehosomes. The encapsulation efficiency of ethosomes was determined by UV-spectrometry. The optimal formation and preparation were selected by an orthogonal design test. The effects of different dosages regimens on the transdermal penetration of colchicine were evaluated using TYJ-6A franz-diffusition cells. RESULTS The encapsulation efficiency of eolchicines ethosomes was 57.0%. The flux of colehicines from ethosome was 6.54 ~tg.cma-h-1, which were 5.59, 3.14 and 1.24 times as those of saturated aqueos solution, liposomes and 30% ethanol solution, respectively. The subsequence of retention amount in the skin after 12 h was： ethosomes〉30% ethanol solution〉 liposomes〉 saturated aqueos solution. CONCLUSION Ethomes is effective for transdermal penetration and increased the eolehieines amount retaine in the skin.