聚合物胶束用于口服给药的研究进展

Advances in the study of polymeric micelles used in oral administration

聚合物胶束是由两亲性聚合物自发形成的热力学稳定体系,它对难溶性药物具有良好的增溶效果。许多具有良好活性的药物由于溶解性差,其口服给药受到限制。将聚合物胶束作为口服给药的载体可以显著改善药物的溶解性,增加透过生物膜的药量,进而提高药效。此外,聚合物组成和性质具有多样性,利用聚合物的这一特性可以制备出对pH值、温度敏感或者具有黏膜黏附性的胶束。在提高药物溶解度的同时,通过改变药物在胃肠道中的释放过程,进一步提高其生物利用度。本文主要介绍聚合物胶束在口服给药方面的研究进展,分析并总结其作为口服给药载体应用的特点和前景。

Polymeric micelles which are self-assembled from amphiphilic copolymers are thermodynamically stable,and they can solubilize hydrophobic drugs by the hydrophilic core.Many excellent active compounds are confined because of general low oral bioavailability due to poor solubility.Take into account from the two points above,polymeric micelles may be used as proper oral carrier to improve the dissolubility of hydrophobic drugs,and enhance the permeation though gastrointestinal tract,therefore,the pharmacodynamics is elevated.Meanwhile,the segments in copolymers are multivariate,so many kinds of micelles can be obtained,such as,pH-or thermo-sensitive as well as mucoadhesive ones.The modified micelles can alter drug release profiles while solubilizing them,that is why the oral bioavailability increase further.In this review,recent progress of polymeric micelles used in oral administration is summarized,and the prospect of polymeric micelles’ application in this field is also evaluated.