title: Amphiphilic Polycarbonates from Carborane-Installed Cyclic Carbonates as Potential Agents for Boron Neutron Capture Therapy.
abstract: Carboranes with rich boron content have showed significant applications in the field of boron neutron capture therapy. Biodegradable derivatives of carborane-conjugated polymers with well-defined structure and tunable loading of boron atoms are far less explored. Herein, a new family of amphiphilic carborane-conjugated polycarbonates was synthesized by ring-opening polymerization of a carborane-installed cyclic carbonate monomer. Catalyzed by TBD from a poly(ethylene glycol) macroinitiator, the polymerization proceeded to relatively high conversions (>65%), with low polydispersity in a certain range of molecular weight. The boron content was readily tuned by the feed ratio of the monomer and initiator. The resultant amphiphilic polycarbonates self-assembled in water into spherical nanoparticles of different sizes depending on the hydrophilic-to-hydrophobic ratio. It was demonstrated that larger nanoparticles (PN150) were more easily subjected to protein adsorption and captured by the liver, and smaller nanoparticles (PN50) were more likely to enter cancer cells and accumulate at the tumor site. PN50 with thermal neutron irradiation exhibited the highest therapeutic efficacy in vivo. The new synthetic method utilizing amphiphilic biodegradable boron-enriched polymers is useful for developing more-selective and -effective boron delivery systems for BNCT.
authors.affiliation: State Key Laboratory of Polymer Physics and Chemistry, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences , Changchun 130022, PR China.|University of Chinese Academy of Sciences , Beijing 100049, PR China.
authors.forename: Hejian
authors.initials: H
authors.lastname: Xiong
authors.affiliation: State Key Laboratory of Polymer Physics and Chemistry, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences , Changchun 130022, PR China.|University of Chinese Academy of Sciences , Beijing 100049, PR China.
authors.forename: Xing
authors.initials: X
authors.lastname: Wei
authors.affiliation: State Key Laboratory of Polymer Physics and Chemistry, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences , Changchun 130022, PR China.
authors.forename: Dongfang
authors.initials: D
authors.lastname: Zhou
authors.affiliation: State Key Laboratory of Polymer Physics and Chemistry, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences , Changchun 130022, PR China.
authors.forename: Yanxin
authors.initials: Y
authors.lastname: Qi
authors.affiliation: State Key Laboratory of Polymer Physics and Chemistry, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences , Changchun 130022, PR China.
authors.forename: Zhigang
authors.initials: Z
authors.lastname: Xie
authors.affiliation: Key Laboratory of Polymer Ecomaterials, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences , Changchun 130022, PR China.
authors.forename: Xuesi
authors.initials: X
authors.lastname: Chen
authors.affiliation: State Key Laboratory of Polymer Physics and Chemistry, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences , Changchun 130022, PR China.
authors.forename: Xiabin
authors.initials: X
authors.lastname: Jing
authors.affiliation: State Key Laboratory of Polymer Physics and Chemistry, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences , Changchun 130022, PR China.
authors.forename: Yubin
authors.initials: Y
authors.lastname: Huang
mesh_terms: D000818:Animals; D001692:Biological Transport; D001880:Boranes / Q000737:chemistry*; D016754:Boron Neutron Capture Therapy / Q000379:methods*; D002254:Carbonates / Q000737:chemistry*; D045744:Cell Line, Tumor; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D051379:Mice; D053758:Nanoparticles / Q000737:chemistry; D010316:Particle Size; D011076:Polycarboxylate Cement / Q000737:chemistry* / Q000378:metabolism / Q000493:pharmacokinetics / Q000627:therapeutic use*; D014018:Tissue Distribution
chemical_list: D001880:Boranes; D002254:Carbonates; D011076:Polycarboxylate Cement; C005506:polycarbonate