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

Chemo-enzymatic synthesis of degradable PTMC-b-PECA-b-PTMC triblock copolymers and their micelle formation for pH-dependent controlled release.
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DOI:
10.1002/mabi.200800308
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发表时间:
2009-06
影响因子:
4.6
通讯作者:
S. Kaihara;J. Fisher;S. Matsumura
S. Kaihara;J. Fisher;S. Matsumura
中科院分区:
工程技术3区
文献类型:
--
作者:
S. Kaihara;J. Fisher;S. Matsumura

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采用化学酶法合成了一系列可降解的三嵌段共聚物,即聚(三亚甲基碳酸酯)-嵌段-聚[聚乙二醇-共环缩醛]-嵌段-聚三亚甲基碳酸酯(PTMC-b-PECA-b-PTMC)。在聚乙二醇链段中引入环缩醛作为可降解链段,赋予其依赖于pH的降解性质,并防止酸性降解产物的产生。成功地制备了两亲性聚合物胶束,胶束的化学组成和相对分子质量对胶束的性质有很大影响。药物释放研究表明,由于环缩醛链段的降解,随着缓冲液pH值的降低,其释放速率增加,表明其在pH敏感的控释方面具有很高的实用价值。
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.