【摘要】 目的考察醇质体作为非那甾胺经皮给药载体的渗透特性。方法分别采用注入法和薄膜分散法制备非那甾胺醇质体(ethosomes)和脂质体;用透射电镜观察所得醇质体和脂质体的形态;采用改良的TK-6A型Franz扩散池,用人皮进行体外经皮渗透实验;以HPLC测定一定时间点接受室中药物浓度,求算累积渗透量及稳态透皮速率,并测定药物在表皮层和真皮层中的滞留量。结果非那甾胺醇质体经皮渗透速率(134μg·cm-2·h-1)是其水饱和溶液的74倍,是脂质体的32倍,是30%乙醇溶液的26倍。24h时药物在皮肤中滞留量大小顺序为醇质体>30%乙醇溶液>脂质体>水饱和液。结论醇质体能显著促进脂溶性药物非那甾胺的经皮渗透,增加药物在皮肤中的蓄积,有望成为一类新型的皮肤给药制剂。更多还原

【Abstract】 OBJECTIVE To investigate the penetration characteristics of finasteride ethosomes as a transdermal vehicle.METHODS The ethosomes and liposomes of finasteride were prepared by injection and film dispersing method, respectively. Their morphology was observed by transmission electronic microscopy (TEM). The penetration experiments in vitro were performed using human skin on modified Franz diffusion cells. The concentrations of finasteride in receptor compartment at specified time points were determined by HPLC. The steady penetration rate and the quantity of drug accumulated in skin were calculated. RESULTS The penetration rate of finasteride from ethosomes(1.34 μg·cm~-2 ·h~-1 ) was 6.4, 2.2 and 1.6 times higher than that from saturated water solution, liposomes and hydroethanolic solution of finasteride, respectively. The quantity of drug released from the ethosomeas and accumulated in the skin by the end of the experiment was statistically greater from the ethosomes than from liposomes or other control groups.CONCLUSION Ethosomes can improve the transdermal permeation and skin accumulation of finasteride.更多还原