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可降解聚三亚甲基碳酸酯-b-聚(2-乙氧基-2-恶唑啉)-b-聚三亚甲基碳酸酯三嵌段共聚物的化学酶法合成及其pH依赖性控释的胶束形成

Chemo-enzymatic synthesis of degradable PTMC-b-PECA-b-PTMC triblock copolymers and their micelle formation for pH-dependent controlled release.

作者信息

Kaihara Sachiko, Fisher John P, Matsumura Shuichi

机构信息

Department of Applied Chemistry, Keio University, Yokohama 223-8522, Japan.

出版信息

Macromol Biosci. 2009 Jun 11;9(6):613-21. doi: 10.1002/mabi.200800308.

Abstract

A series of degradable triblock copolymers, poly(trimethylene carbonate)-block-poly[poly(ethylene glycol)-co-cyclic acetal]-block-poly(trimethylene carbonate) (PTMC-b-PECA-b-PTMC), were chemo-enzymatically synthesized. Cyclic acetal was introduced into a poly(ethylene glycol) segment as a degradable segment to impart a pH-dependent degradation nature and to prevent the production of acidic degradation products. Amphiphilic polymeric micelles were successfully prepared, and the properties of the micelles were significantly affected by their chemical compositions and the molecular weights. A drug release study showed that the release rate increased as the pH of the buffer decreased due to the degradation of the cyclic acetal segments, indicating its high utility for pH-sensitive controlled release.

摘要

通过化学酶法合成了一系列可降解的三嵌段共聚物,聚(碳酸三亚甲基酯)-嵌段-聚[聚(乙二醇)-共-环状缩醛]-嵌段-聚(碳酸三亚甲基酯)(PTMC-b-PECA-b-PTMC)。将环状缩醛引入聚(乙二醇)链段作为可降解链段,以赋予其pH依赖性降解特性并防止产生酸性降解产物。成功制备了两亲性聚合物胶束,其化学组成和分子量对胶束的性质有显著影响。药物释放研究表明,由于环状缩醛链段的降解,缓冲液pH值降低时释放速率增加,表明其在pH敏感控释方面具有很高的实用性。

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