新型经皮渗透促进剂及作用机制的研究进展

Advance in the research of novel penetration enhancers and their mechanisms of action

角质层(stratumcorneum,SC)是皮肤给药的主要屏障,无论是局部经皮的皮内给药还是经皮吸收进入体循环发挥全身作用都必须克服SC的屏障作用。但绝大部分药物都难以有效地透过SC,在众多克服SC的方法中,化学渗透促进剂(chemical penetration enhancers,CPE)的应用最广泛。除传统的醇类、亚砜类、脂肪酸类、酯类、氮酮、多元醇类等,又发现或合成了许多新型高效的促进剂。文中对近年来国内外关于新型渗透促进剂的文献进行综述,以期为合成和发现更加安全、高效的渗透促进剂提供线索。

The outermost layer of human skin, the stratum corneum, is responsible for its barrier function. Before topically administered drugs act either dermally or transdermally, they have to penetrate into the deeper skin layers or permeate the skin. However, most topically administered drugs do not have the ability to penetrate the stratum eorneum. Many approaches have been employed to breach the stratum corneum, of which, the most widely used one is chemical penetration enhancers. In addition to the traditional alcohols, sulphoxides, fatty acids, esters, azone, polyoles and so on, several representative new chemical enhancers have been discovered or synthesized. This article reviewed the novel penetration enhancers reported recently to provide clues for synthesizing and discoverying safer and more efficient penetration enhancers.