药物纳米载体——聚合物胶束的研究进展

Research progress on drug nanocontainer—polymeric micelles

目的对目前聚合物胶束作为药物纳米载体的国内外研究进展进行综述。方法参考近年来国内外文献50篇,从聚合物胶束的类别和构成,药物的包载方法,药物从聚合物胶束中的释放,聚合物胶束的稳定性,聚合物胶束的表征,聚合物胶束对药物的药动学和体内分布的影响以及聚合物胶束作为药物载体的应用等几个方面系统地介绍了其研究进展。结果聚合物胶束包括自聚集胶束,单分子胶束和交联的胶束,可采用化学结合法、物理包载和聚离子复合法包载药物;药物分子在聚合物胶束中的分布以及聚合物的降解行为决定了药物的释放速度;聚合物胶束的热力学和动力学稳定性与其结构组成密切相关;载药聚合物胶束可改变药物的药动学和体内分布;目前聚合物胶束已被用于作为肿瘤药物、难溶性药物的载体,也可作为药物药物经皮传递载体和药物的缓释载体,发展前景较好,但同时也面临挑战。结论聚合物胶束作为药物的纳米载体具有广泛的应用前景。

Objective To review the progress on polymeric micelles as drug nanocontainer.Methods In the present paper,the classification and composition of polymeric micelles,drug loading method,drug release from micelles,stability of micelles,characteristics of polymeric micelles,influence of polymeric micelles on the pharmacokinetics and in vivo distribution of therapeutic drugs,and application of polymeric micelles as drug nanocarriers were introduced.Results Polymeric micelles include self-assembled micelles,unimolecular micelles and cross-linked micelles.Drug substance can be loaded into the micelles by chemical conjunction,physical entrapment and polyionic complexation.The distribution of the drug substance in the micelle and the degradation behavior of the polymer have significant influence on drug release.The thermodynamic and dynamic stability of the polymeric micelles is composition dependent.The pharmacokinetics and drug distribution can be changed by using different polymer micelles as drug carriers.Polymeric micelles are now extensively studied as the carrier for the delivery of antitumor and poorly soluble drug substances,it can also be used as the carrier for transdermal and sustained drug delivery.However,it meets challenges in the meantime.Conclusions Polymeric micelles,as drug nanocontainer,have promising application for the delivery of a large number of diverse therapeutic compounds.