枝化-环化结构共聚物用于酸响应载药体系
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上海市重点学科和重点实验室项目,上海市浦江人才计划


Synthesis of Branched & Cyclized Copolymer for pH-responsive drug delivery system
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    摘要:

    药物载体系统对癌症的靶向性治疗有重要意义,本文制备了一种嵌段共聚物用于药物载体系统,探究其用于载药系统的可行性。将大分子引发剂溴代聚乙二醇(PEG2KBr)和缩醛化物二(2-丙烯酰氧基乙氧基)-(4-甲氧基苯基)甲烷(ACD)分别作为引发剂和单体,采用逆向增强原子转移自由基聚合(DE-ATRP)法得到嵌段共聚物聚乙二醇-b-聚[二(2-丙烯酰氧基乙氧基)-(4-甲氧基苯基)甲烷](PEG-b-PACDs)。通过核磁共振和凝胶渗透色谱表征该聚合物的结构;用动态光散射和透射电镜表征胶束的尺寸和形貌。结果表明聚合物呈现枝化-环结构,空白胶束的尺寸在70 nm左右,载药胶束尺寸在90 nm左右,胶束的药物包封率为48.7%,在酸性条件下具有良好的药物缓释放性。证明了该聚合物在载药系统有一定的应用价值。

    Abstract:

    Drug delivery system has great significance for the targeted treatment of cancer. A cyclized & branched amphiphilic block copolymer was synthesized by DE-ATRP with brominated polyethylene glycol (PEG2KBr) as initiator and di(2-acry-loyloxy ethoxy)-[4-methoxy-phenyl]methane (ACD) as hydrophobic monomer and explore for its potential application to drug delivery. The structure of polymer was characterized by hydrogen spectrum nuclear magnetic resonance (1HNMR) and gel permeation chromatography (GPC). The size and morphology of micelles was measured by dynamic light scattering (DLS) and transmission scanning microscopy (TEM). The structure was identified to be branched-cyclized. The blank micelles were spherical with the size of 70 nm, and Doxorubicin hydrochloride loaded micelles were with the size of 90 nm. The drug loading efficiency was 48.7%, DOX-loaded micelles have good pH-responsive and drug release. It is proved that the polymer has a certain application value in drug delivery system.

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陈新.枝化-环化结构共聚物用于酸响应载药体系[J].精细化工,2017,34(10):

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  • 收稿日期:2017-01-03
  • 最后修改日期:2017-03-22
  • 录用日期:2017-04-25
  • 在线发布日期: 2017-09-04
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