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

机译:基于受控药物释放的硫代烯反应的GSH响应聚合物胶束

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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:我们报告了一种基于烯烃键和GSH之间的迈克尔添加反应的谷胱甘肽(GSH)响应药物载体。通过去激活增强的原子转移自由基聚合(DE-ATRP)成功地合成了具有多线性环状的和支链结构的两亲性共聚物,其含有乙烯基。聚合物自组装成GSH响应胶束,尺寸为68至97nm和球形形态。确认核心交联胶束大大降低由于浓度梯度引起的多柔比蛋白(DOX)泄漏。药物释放实验表明,不含二硫化物的药物载体具有与具有类似聚合物结构的常规GSH还原响应载体相同的响应能力。 MTT测定表明,坯料胶束是完全非细胞毒性的,而DOX加载的胶束表现出GSH依赖性的行为。

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