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Well-Defined, Reversible Boronate Crosslinked Nanocarriers for Targeted Drug Delivery in Response to Acidic pH Values and cis-Diols

Authors

  • Dr. Yuanpei Li,

    1. Department of Biochemistry and Molecular Medicine, UC Davis Cancer Center, University of California, Davis, 2700 Stockton Blvd., Sacramento, CA 95817 (USA)
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    • These authors contributed equally to this work.

  • Dr. Wenwu Xiao,

    1. Department of Biochemistry and Molecular Medicine, UC Davis Cancer Center, University of California, Davis, 2700 Stockton Blvd., Sacramento, CA 95817 (USA)
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    • These authors contributed equally to this work.

  • Dr. Kai Xiao,

    1. Department of Biochemistry and Molecular Medicine, UC Davis Cancer Center, University of California, Davis, 2700 Stockton Blvd., Sacramento, CA 95817 (USA)
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  • Dr. Lorenzo Berti,

    1. Department of Biochemistry and Molecular Medicine, UC Davis Cancer Center, University of California, Davis, 2700 Stockton Blvd., Sacramento, CA 95817 (USA)
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  • Prof. Juntao Luo,

    Corresponding author
    1. Department of Pharmacology, SUNY Upstate Cancer Research Institute, SUNY Upstate Medical University, Syracuse, NY 13210 (USA)
    • Department of Pharmacology, SUNY Upstate Cancer Research Institute, SUNY Upstate Medical University, Syracuse, NY 13210 (USA)
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  • Harry P. Tseng,

    1. Department of Biochemistry and Molecular Medicine, UC Davis Cancer Center, University of California, Davis, 2700 Stockton Blvd., Sacramento, CA 95817 (USA)
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  • Gabriel Fung,

    1. Department of Biochemistry and Molecular Medicine, UC Davis Cancer Center, University of California, Davis, 2700 Stockton Blvd., Sacramento, CA 95817 (USA)
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  • Prof. Kit S. Lam

    Corresponding author
    1. Department of Biochemistry and Molecular Medicine, UC Davis Cancer Center, University of California, Davis, 2700 Stockton Blvd., Sacramento, CA 95817 (USA)
    • Department of Biochemistry and Molecular Medicine, UC Davis Cancer Center, University of California, Davis, 2700 Stockton Blvd., Sacramento, CA 95817 (USA)
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  • This work was funded by NIH/NCI (R01CA115483 and R01CA140449), NIH/NIBIB (R01EB012569), and DoD BCRP Postdoctoral Award (W81XWH-10-1-0817).

Abstract

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Demand and deliver: Micelles reversibly crosslinked by boronate esters (see scheme) show in vitro and in vivo stability, and thus minimize premature drug release under physiological conditions. After reaching the tumor sites, drug (stars in scheme) release is activated by cleavage of the boronate esters by the acidic conditions around the tumor or in the target cells, or by the administration of mannitol.

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