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皮肤的屏障作用使大部分药物无法实现透皮给药。本文以改善难溶性大分子模型药物多烯紫杉醇(docetaxel,DTX)的经皮渗透性为主体思路,研制了DTX的表面活性剂-醇质体(surfactant-ethanlic liposomes,SEL)。SEL由磷脂、乙醇、胆酸钠、DTX和磷酸盐缓冲液组成,采用薄膜分散法制备。对SEL的囊泡形态(冷冻蚀刻电镜法)、粒径大小及分布进行了表征,并测定包封率和载药量。采用体外扩散池实验研究了DTX表面活性剂-醇质体的经皮渗透性。结果表明,当磷脂与表面活性剂的比例为85:15时,DTX的稳态透皮速率和累计透皮量均为最高,且优于表面活性剂脂质体、醇质体和普通脂质体。最优处方的粒径分布、形态和载药量均较为稳定。本研究表明,通过将DTX包载于SEL中可显著改善DTX的经皮渗透性。
The skin barrier prevents most drugs from achieving transdermal delivery. In this paper, the surfactant-ethanlic liposomes (SEL) of DTX was developed in order to improve the transdermal permeability of docetaxel (DTX), a poor-solubility macromolecule model drug. SEL consists of phospholipids, ethanol, sodium cholate, DTX and phosphate buffer, prepared by the thin film dispersion method. SEL vesicles morphology (freeze-etched electron microscopy), particle size and distribution were characterized, and determination of encapsulation efficiency and drug loading. An in vitro diffusion cell experiment was performed to investigate the transdermal permeability of the DTX surfactant-ethosome. The results showed that when the ratio of phospholipid to surfactant was 85:15, the steady-state transdermal transdermal rate and cumulative transdermal volume of DTX were the highest, which was better than that of surfactant liposomes, ethosomes and common lipids body. The optimal prescription of particle size distribution, morphology and drug loading are more stable. This study shows that transdermal penetration of DTX can be significantly improved by encapsulating DTX in SEL.