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基于环糊精接枝聚乳酸-聚乙二醇嵌段共聚物胶束的控释药物系统。

Controlled drug release system based on cyclodextrin-conjugated poly(lactic acid)-b-poly(ethylene glycol) micelles.

机构信息

College of Polymer Science and Engineering, Sichuan University, Chengdu 610065, China.

出版信息

Int J Pharm. 2013 Feb 25;443(1-2):110-9. doi: 10.1016/j.ijpharm.2012.12.042. Epub 2013 Jan 14.

DOI:10.1016/j.ijpharm.2012.12.042
PMID:23328682
Abstract

Cyclodextrin-conjugated poly(lactic acid)-b-poly(ethylene glycol) (β-CD-PLA-mPEG), a well-defined amphiphilic copolymer, was synthesized by controlled ring-open copolymerization and click coupling reaction, in order to obtain a biocompatible drug delivery system with controlled release profiles. The β-CD-PLA-mPEG copolymer could self-assemble in aqueous solution to form micelles with a mean particle size of 173.4 nm, which will decrease to 159.2 nm after loaded with a kind of hydrophobic drug (indomethacin, IND). The IND-loaded β-CD-PLA-mPEG micelles show spherical shape within the nano-size scale under TEM imaging. Compared with that formed by PLA-mPEG, the micelles formed by β-CD-PLA-mPEG copolymer present higher drug loading efficiency and controlled release profile of IND, especially in the control of its initial burst release. Meanwhile, β-CD-PLA-mPEG copolymer exhibits low toxicity to cells. The micelles formed by β-CD-PLA-mPEG copolymer could be a promising controlled release system for various hydrophobic drugs.

摘要

环糊精接枝聚乳酸-聚乙二醇（β-CD-PLA-mPEG）是一种通过可控开环共聚和点击偶联反应合成的两亲性嵌段共聚物，目的是获得具有可控释放特性的生物相容药物传递系统。β-CD-PLA-mPEG 共聚物在水溶液中自组装形成平均粒径为 173.4nm 的胶束，当负载一种疏水性药物（吲哚美辛，IND）后，粒径会减小至 159.2nm。TEM 成像显示，载有 IND 的β-CD-PLA-mPEG 胶束呈纳米级球形。与 PLA-mPEG 形成的胶束相比，β-CD-PLA-mPEG 共聚物胶束具有更高的 IND 载药效率和可控释放特性，特别是对初始突释的控制。同时，β-CD-PLA-mPEG 共聚物对细胞的毒性较低。β-CD-PLA-mPEG 共聚物形成的胶束可能是一种有前途的各种疏水性药物的控释系统。

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