pH-responsive polymeric micelles based on poly(ethyleneglycol)-b-poly(2-(diisopropylamino) ethyl methacrylate) block copolymer for enhanced intracellular release of anticancer drugs

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• 作者：Zhigang Xu^a ; ¹ ; ^{zgxu@swu.edu.cn} ; Peng Xue^a ; ¹ ; Yong-E Gao^a ; Shiying Liu^b ; Xiaoxiao Shi^a ; Meili Hou^a ; Yuejun Kang^a ; ^{yjkang@swu.edu.cn}
• 关键词：pH-responsive ; Micelles ; Block copolymer ; Cancer therapy ; Controlled release
• 刊名：Journal of Colloid and Interface Science
• 出版年：2017
• 出版时间：15 March 2017
• 年：2017
• 卷：490
• 期：Complete
• 页码：511-519
• 全文大小：2938 K
• 卷排序：490

文摘

We present a pH-responsive poly(ethyleneglycol)-b-poly(2-(diisopropylamino) ethyl methacrylate) block copolymer (MPEG-PPDA) that can self-assemble into micelles at very low critical micelle concentration. The formed micelles exhibit superior stability in physiological environment and pH-triggered transforming capability between self-assembly and disassembly. Moreover, the resulting micelles can load hydrophobic anticancer drug molecules such as doxorubicin in the core of micelles. The pH-triggered drug release kinetics matches the classical hydrazone bond model. The blank micelles demonstrate minimal cytotoxicity while the drug-loaded micelles exhibit significantly improved anticancer efficacy. These results indicate that this MPEG-PPDA block copolymer could be utilized as a universal pH-responsive delivery system for controlled release of hydrophobic anticancer drug in chemotherapy.