title: Self-assembly of BODIPY based pH-sensitive near-infrared polymeric micelles for drug controlled delivery and fluorescence imaging applications.
abstract: Responsive block copolymer micelles emerging as promising imaging and drug delivery systems show high stability and on-demand drug release activities. Herein, we developed self-assembled pH-responsive NIR emission micelles entrapped with doxorubicin (DOX) within the cores by the electrostatic interactions for fluorescence imaging and chemotherapy applications. The block copolymer, poly(methacrylic acid)-block-poly[(poly(ethylene glycol) methyl ether methacrylate)-co-boron dipyrromethene derivatives] (PMAA-b-P(PEGMA-co-BODIPY), was synthesized via reversible addition-fragmentation chain transfer (RAFT) polymerization, and the molecular weight distribution of this copolymer was narrow (Mw/Mn = 1.31). The NIR fluorescence enhancement induced by the phenol/phenolate interconversion equilibrium works as a switch in response to the intracellular pH fluctuations. DOX-loaded PMAA-b-P(PEGMA-co-BODIPY) micelles can detect the physiological pH fluctuations with a pKa near physiological conditions (∼7.52), and showed pH-responsive collapse and an obvious acid promoted anticancer drug release behavior (over 58.8-62.8% in 10 h). Real-time imaging of intracellular pH variations was performed and a significant chemotherapy effect was demonstrated against HeLa cells.
authors.affiliation: Suzhou Key Laboratory of Macromolecular Design and Precision Synthesis, Jiangsu Key Laboratory of Advanced Functional Polymer Design and Application, Department of Polymer Science and Engineering, College of Chemistry, Chemical Engineering and Materials Science, Soochow University, Suzhou 215123, China. chengzhenping@suda.edu.cn.
authors.forename: Xiaodong
authors.initials: X
authors.lastname: Liu
authors.forename: Bizheng
authors.initials: B
authors.lastname: Chen
authors.forename: Xiaojun
authors.initials: X
authors.lastname: Li
authors.forename: Lifen
authors.initials: L
authors.lastname: Zhang
authors.forename: Yujie
authors.initials: Y
authors.lastname: Xu
authors.forename: Zhuang
authors.initials: Z
authors.lastname: Liu
authors.forename: Zhenping
authors.initials: Z
authors.lastname: Cheng
authors.forename: Xiulin
authors.initials: X
authors.lastname: Zhu
mesh_terms: D001896:Boron Compounds / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D003692:Delayed-Action Preparations / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D004317:Doxorubicin / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D006367:HeLa Cells; D006801:Humans; D006863:Hydrogen-Ion Concentration; D008689:Methacrylates / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D008823:Micelles; D061848:Optical Imaging; D011092:Polyethylene Glycols / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D011109:Polymethacrylic Acids / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology
chemical_list: C095489:4,4-difluoro-4-bora-3a,4a-diaza-s-indacene; D001896:Boron Compounds; D003692:Delayed-Action Preparations; D008689:Methacrylates; D008823:Micelles; D011109:Polymethacrylic Acids; C524499:polyethylene glycol methacrylate; C030613:polymethacrylic acid; D011092:Polyethylene Glycols; D004317:Doxorubicin