title: pH-responsive polymeric micelles based on poly(ethyleneglycol)-b-poly(2-(diisopropylamino) ethyl methacrylate) block copolymer for enhanced intracellular release of anticancer drugs.
abstract: 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.
authors.affiliation: Institute for Clean Energy and Advanced Materials, Faculty of Materials and Energy, Southwest University, Chongqing 400715, China. Electronic address: zgxu@swu.edu.cn.
authors.forename: Zhigang
authors.initials: Z
authors.lastname: Xu
authors.affiliation: Institute for Clean Energy and Advanced Materials, Faculty of Materials and Energy, Southwest University, Chongqing 400715, China.
authors.forename: Peng
authors.initials: P
authors.lastname: Xue
authors.affiliation: Institute for Clean Energy and Advanced Materials, Faculty of Materials and Energy, Southwest University, Chongqing 400715, China.
authors.forename: Yong-E
authors.initials: YE
authors.lastname: Gao
authors.affiliation: School of Chemical and Biomedical Engineering, Nanyang Technological University, 62 Nanyang Drive, Singapore 637459, Singapore.
authors.forename: Shiying
authors.initials: S
authors.lastname: Liu
authors.affiliation: Institute for Clean Energy and Advanced Materials, Faculty of Materials and Energy, Southwest University, Chongqing 400715, China.
authors.forename: Xiaoxiao
authors.initials: X
authors.lastname: Shi
authors.affiliation: Institute for Clean Energy and Advanced Materials, Faculty of Materials and Energy, Southwest University, Chongqing 400715, China.
authors.forename: Meili
authors.initials: M
authors.lastname: Hou
authors.affiliation: Institute for Clean Energy and Advanced Materials, Faculty of Materials and Energy, Southwest University, Chongqing 400715, China. Electronic address: yjkang@swu.edu.cn.
authors.forename: Yuejun
authors.initials: Y
authors.lastname: Kang
mesh_terms: D000903:Antibiotics, Antineoplastic / Q000008:administration & dosage* / Q000493:pharmacokinetics; D003692:Delayed-Action Preparations / Q000737:chemistry*; D004317:Doxorubicin / Q000008:administration & dosage* / Q000493:pharmacokinetics; D006367:HeLa Cells; D006801:Humans; D006863:Hydrogen-Ion Concentration; D008768:Methylmethacrylates / Q000737:chemistry*; D008823:Micelles; D011092:Polyethylene Glycols / Q000737:chemistry*
chemical_list: D000903:Antibiotics, Antineoplastic; D003692:Delayed-Action Preparations; D008768:Methylmethacrylates; D008823:Micelles; D011092:Polyethylene Glycols; D004317:Doxorubicin; C009931:poly(ethylmethacrylate)
keywords: Block copolymer; Cancer therapy; Controlled release; Micelles; pH-responsive