Biodegradable amphiphilic block-graft copolymers based on methoxy poly(ethylene glycol)-b-(polycarbonates-g-polycarbonates) for controlled release of doxorubicin
Biodegradable amphiphilic block-graft copolymers based on methoxy poly(ethylene glycol)-b-(polycarbonates-g-polycarbonates) for controlled release of doxorubicin
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DOI：
10.1007/s10856-013-5057-4
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发表时间：
2013
期刊：
影响因子：
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通讯作者：
Tao Jiang;Youmei Li;Yin Lv;Yin‐Jia Cheng;F. He;R. Zhuo
中科院分区：
文献类型：
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作者：
Tao Jiang;Youmei Li;Yin Lv;Yin‐Jia Cheng;F. He;R. Zhuo
本文合成了一种新型的可生物降解的两亲性嵌段共聚物-甲氧基聚乙二醇-B-（聚碳酸酯-g-聚碳酸酯）（mPEG-b-（PATMC-g-PATMC）），用于阿霉素（DOX）的控制释放。以固定化猪胰脂肪酶（IPPL）为催化剂，本体法合成了主链嵌段共聚物甲氧基聚乙二醇-b-聚（5-烯丙氧基-1，3-二氧六环-2-酮）（mPEG-b-PATMC）。然后，mPEG-b-PATMC的烯丙基环氧化产物mPEG-b-PATMC-O也使用IPPL作为催化剂通过PATMC本身进一步接枝。用1 N HMR和凝胶渗透色谱对共聚物进行了表征，结果表明共聚物的分子量分布较窄。用透析法可以制备稳定的胶束溶液，并得到单峰窄的粒径分布。透射电子显微镜（TEM）观察表明，DOX负载前后胶束呈纳米级球形分散。与嵌段共聚物相比，接枝结构可以增强聚合物链与药物分子的相互作用，提高载药能力和包封率。此外，两亲性嵌段接枝共聚物mPEG-b-（PATMC-g-PATMC）具有较低的细胞毒性和较好的缓释性能。
In this paper, novel biodegradable amphiphilic block-graft copolymers based on methoxy poly(ethylene glycol)-b-(polycarbonates-g-polycarbonates) (mPEG-b-(PATMC-g-PATMC)) were synthesized successfully for controlled release of doxorubicin (DOX). Backbone block copolymer, methoxy poly(ethylene glycol)-b-poly(5-allyloxy-1,3-dioxan-2-one) (mPEG-b-PATMC) was synthesized in bulk catalyzed by immobilizedporcine pancreaslipase (IPPL). Then, mPEG-b-PATMC-O, the allyl epoxidation product of mPEG-b-PATMC, was further grafted by PATMC itself also using IPPL as the catalyst. The copolymers were characterized by1N HMR and gel permeation chromatography results showed narrow molecular weight distributions. Stable micelle solutions could be prepared by dialysis method, while a monomodal and narrow size distribution could be obtained. Transmission electron microscopy (TEM) observation showed the micelles dispersed in spherical shape with nano-size before and after DOX loading. Compared with the block copolymers, the grafted structure could enhance the interaction of polymer chains with drug molecules and improve the drug-loading capacity and entrapment efficiency. Furthermore, the amphiphilic block-graft copolymers mPEG-b-(PATMC-g-PATMC) had low cytotoxicity and more sustained drug release behavior.