Chen Dong, Ding Ping-Tian, Deng Yi-Hui, Wang Si-Ling
School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China.
Yao Xue Xue Bao. 2010 May;45(5):560-4.
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.
由两亲性共聚物自组装而成的聚合物胶束具有热力学稳定性,它们可以通过亲水核增溶疏水性药物。由于溶解度差,许多优秀的活性化合物因口服生物利用度普遍较低而受到限制。综合考虑上述两点,聚合物胶束可作为合适的口服载体,以改善疏水性药物的溶解性,并增强其在胃肠道的渗透,从而提高药效。同时,共聚物中的链段是多变量的,因此可以获得多种胶束,如pH或温度敏感型以及粘膜粘附型胶束。改性胶束在增溶药物的同时可以改变药物释放曲线,这就是口服生物利用度进一步提高的原因。在这篇综述中,总结了用于口服给药的聚合物胶束的最新进展,并评估了聚合物胶束在该领域的应用前景。