title: pH-Triggered Polypeptides Nanoparticles for Efficient BODIPY Imaging-Guided Near Infrared Photodynamic Therapy.
abstract: An efficient pH-responsive multifunctional polypeptide micelle for simultaneous imaging and in vitro photodynamic therapy (PDT) has been prepared. The goal here is to detect and treat cancer cells by near-infrared fluorescence (NIRF) imaging and PDT synchronously. A photosensitizer BODIPY-Br2 with efficient singlet oxygen generation was synthesized at first which owns both seductive abilities in fluorescence emission and reactive oxygen species (ROS) generation under light irradiation. Then, amphiphilic copolymer micelles pH-triggered disassembly were synthesized from N-carboxyanhydride (NCA) monomer via a ring-opening polymerization and click reaction for the loading of BODIPY-Br2 by hydrophobic interaction, and the driving force is the protonation of the diisopropylethylamine groups conjugated to the polypeptide side chains. In vitro tests performed on HepG2 cancer cells confirm that the cell suppression rate was improved by more than 40% in the presence of light in the presence of an extremely low energy density (12 J/cm(2)) with very low concentration of 5.4 μM photosensitizer. At the same time, the internalization of the nanoparticles by cells can also be traced by NIRF imaging, indicating that the NIR nanoparticles presented imaging guided photodynamic therapy properties. It provides the potential of using polypeptide as a biodegradable carrier for NIR image-guided photodynamic therapy.
authors.affiliation: CAS Key Laboratory of Soft Matter Chemistry, National Synchrotron Radiation Laboratory, iChEM, and Department of Chemical Physics, University of Science and Technology of China , Hefei 230026, P. R. China.
authors.forename: Le
authors.initials: L
authors.lastname: Liu
authors.affiliation: CAS Key Laboratory of Soft Matter Chemistry, National Synchrotron Radiation Laboratory, iChEM, and Department of Chemical Physics, University of Science and Technology of China , Hefei 230026, P. R. China.
authors.forename: Liyi
authors.initials: L
authors.lastname: Fu
authors.affiliation: CAS Key Laboratory of Soft Matter Chemistry, National Synchrotron Radiation Laboratory, iChEM, and Department of Chemical Physics, University of Science and Technology of China , Hefei 230026, P. R. China.
authors.forename: Titao
authors.initials: T
authors.lastname: Jing
authors.affiliation: CAS Key Laboratory of Soft Matter Chemistry, National Synchrotron Radiation Laboratory, iChEM, and Department of Chemical Physics, University of Science and Technology of China , Hefei 230026, P. R. China.
authors.forename: Zheng
authors.initials: Z
authors.lastname: Ruan
authors.affiliation: CAS Key Laboratory of Soft Matter Chemistry, National Synchrotron Radiation Laboratory, iChEM, and Department of Chemical Physics, University of Science and Technology of China , Hefei 230026, P. R. China.
authors.forename: Lifeng
authors.initials: L
authors.lastname: Yan
mesh_terms: D000812:Anhydrides / Q000737:chemistry; D063566:Biodegradable Plastics / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use*; D004337:Drug Carriers / Q000008:administration & dosage* / Q000737:chemistry; D005453:Fluorescence; D056945:Hep G2 Cells; D006801:Humans; D006863:Hydrogen-Ion Concentration; D007259:Infrared Rays; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry; D009369:Neoplasms / Q000188:drug therapy*; D010455:Peptides / Q000008:administration & dosage; D010778:Photochemotherapy; D017319:Photosensitizing Agents / Q000008:administration & dosage* / Q000138:chemical synthesis / Q000737:chemistry; D011108:Polymers / Q000008:administration & dosage / Q000138:chemical synthesis / Q000737:chemistry; D017382:Reactive Oxygen Species / Q000737:chemistry; D026082:Singlet Oxygen / Q000737:chemistry
chemical_list: D000812:Anhydrides; D063566:Biodegradable Plastics; D004337:Drug Carriers; D010455:Peptides; D017319:Photosensitizing Agents; D011108:Polymers; D017382:Reactive Oxygen Species; D026082:Singlet Oxygen
keywords: N-carboxyanhydride (NCA); near-infrared fluorescence (NIRF) imaging; pH-responsive; photodynamic therapy (PDT); polypeptide; singlet oxygen