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Issue 16, 2017
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Redox/pH dual-sensitive hybrid micelles for targeting delivery and overcoming multidrug resistance of cancer

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Abstract

A redox/pH dual-sensitive graft copolymer, poly(β-amino ester)-g-D-α-tocopherol polyethylene glycol succinate (PBAE-g-TPGS), was synthesized through a Michael-type step polymerization using disulfide linkage-containing TPGS macromonomers. Pluronic F127 (F127) and folate-F127 conjugation were introduced to prepare paclitaxel (PTX)-loaded hybrid micelles to improve their biocompatibility and serum stability and also to achieve targeted delivery. The hybrid micelles exhibited in vitro redox/pH-sensitive PTX release, enhanced cellular uptake through receptor-mediated endocytosis, and strengthened anticancer activities in both the drug-sensitive human breast cancer MCF-7 and drug-resistant MCF-7/ADR cells. P-Glycoprotein inhibition by TPGS and folate-mediated targeted delivery helped overcome multidrug resistance (MDR) and increase the therapeutic efficiency of the drug, leading to good anticancer effects in the MCF-7/ADR xenograft model. Overall, the folate-modified redox/pH-sensitive hybrid micelles provided a three-step approach to enhance anticancer activities via targeted delivery, controlled release, and depressed drug efflux; thus, these micelles may be a powerful weapon against MDR cancers in the future.

Graphical abstract: Redox/pH dual-sensitive hybrid micelles for targeting delivery and overcoming multidrug resistance of cancer

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Publication details

The article was received on 17 Dec 2016, accepted on 15 Mar 2017 and first published on 21 Mar 2017


Article type: Paper
DOI: 10.1039/C6TB03282F
Citation: J. Mater. Chem. B, 2017,5, 2964-2978
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    Redox/pH dual-sensitive hybrid micelles for targeting delivery and overcoming multidrug resistance of cancer

    M. Yin, Y. Bao, X. Gao, Y. Wu, Y. Sun, X. Zhao, H. Xu, Z. Zhang and S. Tan, J. Mater. Chem. B, 2017, 5, 2964
    DOI: 10.1039/C6TB03282F

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