聚合物纳米粒应用于透皮给药及促渗机制研究进展

Research Progress in Polymeric Nanoparticles for Transdermal Drug Delivery and the Mechanism of Enhanced Penetration

透皮给药系统因具有避免肝脏首过效应、血药浓度稳定、局部靶向性及给药方便等优势而备受青睐。然而角质层作为一种生物屏障限制了很多药物,特别是亲水性药物的经皮渗透,因此采用有效的方法促进药物经皮渗透成为透皮给药的关键。聚合物纳米粒因具有药物包封率高、减小酶降解、可控释性能好、比表面积大等优势,易于在皮肤表面富集,从而促进药物渗透,其作为药物载体用于透皮给药逐渐成为近几年的研究热点。本文综述了近年来纳米粒在促进药物渗透方面的研究进展,包括纳米粒促进药物渗透的机制,以及纳米粒联合主动透皮给药方式在促进药物经皮渗透中的应用,并对研究中存在的问题提出适当建议。

Transdermal drug delivery system(TDDS)has attracted more and more attention due to its significant potential in avoiding the hepatic first-pass metabolism,maintaining a constant and prolonged drug level,and providing a local target and convenience for administration.However,the stratum corneum,namely the outermost layer of the skin,acts as a biological barrier,which would limit the transdermal delivery of drug molecules,especially the hydrophilic ones.For this reason,the development of effective methods to enhance the penetration of drugs through skin has become important.In recent years,as a kind of drug carrier for TDDS,the nanoparticle has become popular because of its excellent properties such as high entrapment efficiency,reduced enzymatic degradation,controlled release rate and large specific surface area which can easily accumulate on the surface of the skin to promote the penetration of the drug.This article mainly reviews the research progress in polymeric nanoparticles for TDDS,including the mechanism of enhanced penetration,the combination of nanoparticles and active penetration methods for TDDS.With reference to the problems existing in current studies,suggestions are also proposed.