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超支化聚合物纳米胶束的制备及其 pH/氧化还原响应性药物释放行为。

Preparations of hyperbranched polymer nano micelles and the pH/redox controlled drug release behaviors.

机构信息

Key Laboratory of Synthetic and Biological Colloids, Ministry of Education, School of Chemical and Material Engineering, Jiangnan University, Wuxi 214122, China.

Key Laboratory of Synthetic and Biological Colloids, Ministry of Education, School of Chemical and Material Engineering, Jiangnan University, Wuxi 214122, China.

出版信息

Mater Sci Eng C Mater Biol Appl. 2017 Oct 1;79:116-122. doi: 10.1016/j.msec.2017.05.027. Epub 2017 May 8.

Abstract

Hyperbranched polymer nano micelles (NMs) were prepared through a nucleophilic ring opening polymerization between cystamine and polyethylene glycol diglycidyl ether, followed by a reaction of amino groups and dimethyl maleic anhydride. The NMs showed spheric morphologies with hydrodynamic diameters of 106-120nm. Doxorubicin was loaded in the NMs with loading rate as high as 15.38wt%; The NMs possessed negative zeta potentials in aqueous solutions of pH7.4 due to the carboxyl ions on the particle surfaces, but the zeta potentials were converted to positive ones due to the hydrolysis of amide bonds at pH5.0-6.5, leading to the leaving of carboxyl groups and remaining of amino groups. The disulfide bonds in cystamine were designed in the hyperbranched polymer structures of the NMs, and bonds could be broken by a reducing agent l-glutathione (GSH) (10mM), resulting in a targeted drug release. The smart NMs displayed good biodegradability and biocompatibility, and they could be potentially used in drug controlled release field.

摘要

超支化聚合物纳米胶束(NMs)是通过半胱胺和聚乙二醇二缩水甘油醚之间的亲核开环聚合反应,然后与二甲基马来酸酐反应制备得到的,具有 106-120nm 的水动力直径的球形形态。阿霉素的载药率高达 15.38wt%;由于粒子表面上的羧基离子,NMs 在 pH7.4 的水溶液中带有负的 zeta 电位,但由于酰胺键在 pH5.0-6.5 下的水解,zeta 电位转变为正,导致羧基基团离开而留下氨基基团。半胱胺中的二硫键被设计在 NMs 的超支化聚合物结构中,并且可以通过还原剂 l-谷胱甘肽(GSH)(10mM)打破键,从而实现靶向药物释放。智能 NMs 表现出良好的生物降解性和生物相容性,它们有可能被用于药物控制释放领域。

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