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GSH-responsive polymeric micelles based on the thio-ene reaction for controlled drug release

机译：基于硫烯反应的GSH响应性聚合物胶束可控制药物释放

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摘要

We report a glutathione (GSH) responsive drug carrier that is based on the Michael addition reaction between an olefinic bond and GSH. Amphiphilic copolymers with multi-linear-cyclized and branched structures that contain vinyl groups were successfully synthesized by deactivation enhanced atom transfer radical polymerization (DE-ATRP). The polymers self-assembled into GSH responsive micelles with sizes of 68 to 97 nm and spherical morphology. The core cross-linked micelles were confirmed to greatly decrease doxorubicin (DOX) leakage due to the concentration gradient. Drug release experiments indicated that the drug carrier containing no disulfide has the same responsive ability as a conventional GSH reduction responsive carrier with a similar polymer structure. MTT assays showed that the blank micelles are totally non-cytotoxic, while the DOX-loaded micelles exhibit GSH-dependent behaviour.
机译：我们报告了基于烯烃键和GSH之间的迈克尔加成反应的谷胱甘肽（GSH）响应药物载体。通过失活增强的原子转移自由基聚合（DE-ATRP）成功地合成了具有乙烯基的多线性环化和支化结构的两亲共聚物。聚合物自组装成GSH反应性胶束，尺寸为68至97 nm，球形。由于浓度梯度，核心交联的胶束被证实可大大减少阿霉素（DOX）的泄漏。药物释放实验表明，不含二硫键的药物载体具有与具有相似聚合物结构的常规GSH还原反应载体相同的反应能力。 MTT分析表明，空白胶束完全无细胞毒性，而DOX加载的胶束表现出GSH依赖性行为。

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