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      Block copolymer-boron cluster conjugate for effective boron neutron capture therapy of solid tumors.

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          Abstract

          Boron neutron capture therapy is a promising tumor treatment method, though its wide application has been limited due to the poor tumor selectivity and intracellular delivery of10B-compounds. Here, block copolymer-boron cluster conjugate based on the clinically used sodium borocaptate (BSH) and poly(ethylene glycol)-b-poly(glutamic acid) copolymer have been developed for effectively penetrating tumor tissues and homogeneously delivering the boron clusters into cancer cells towards safe and efficient boron neutron capture therapy. The PEGylated block copolymer-boron cluster (BSH) conjugate has demonstrated significant higher cellular uptake and tumor accumulation when compared to the non-PEGylated formulations and BSH. Moreover, the enhanced delivery to tumors of the conjugates, as well as their superior intratumoral penetration, which facilitated reaching the intracellular space of most cells in tumors, allowed the effective ablation of tumors after neutron irradiation.

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          Author and article information

          Journal
          J Control Release
          Journal of controlled release : official journal of the Controlled Release Society
          Elsevier BV
          1873-4995
          0168-3659
          May 28 2017
          : 254
          Affiliations
          [1 ] Department of Radiology, Center for Medical Imaging, State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University and Collaborative Innovation Center for Biotherapy, Chengdu 610041, PR China. Electronic address: mi@scu.edu.cn.
          [2 ] Department of Nuclear Engineering and Management, Graduate School of Engineering, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033, Japan.
          [3 ] Department of Bioengineering, Graduate School of Engineering, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-8656, Japan.
          [4 ] Innovation Center of Nanomedicine (iCONM), 3-25-14 Tonomachi, Kawasaki-ku, Kawasaki 210-0821, Japan.
          [5 ] Radiation Oncology Research Laboratory, Research Reactor Institute, Kyoto University, Osaka 2 Asahiro nishi, Kumatori, Sennan, Osaka 590-0494, Japan.
          [6 ] Department of Bioengineering, Graduate School of Engineering, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-8656, Japan. Electronic address: horacio@bmw.t.u-tokyo.ac.jp.
          [7 ] Innovation Center of Nanomedicine (iCONM), 3-25-14 Tonomachi, Kawasaki-ku, Kawasaki 210-0821, Japan; Policy Alternatives Research Institute, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-8656, Japan. Electronic address: kataoka@bmw.t.u-tokyo.ac.jp.
          [8 ] Innovation Center of Nanomedicine (iCONM), 3-25-14 Tonomachi, Kawasaki-ku, Kawasaki 210-0821, Japan; Laboratory for Chemistry and Life Science, Institute of Innovative Research, Tokyo Institute of Technology, R1-11, 4259 Nagatsuta, Midori-ku, Yokohama 226-8503, Japan. Electronic address: nishiyama.n.ad@m.titech.ac.jp.
          Article
          S0168-3659(16)31087-2
          10.1016/j.jconrel.2017.03.036
          28336377
          bc79c73f-8163-4ae1-bc82-945659b7d303
          History

          Tumor penetration,Polymer-drug conjugate,Sodium borocapate,Boron neutron capture therapy,Drug delivery system

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