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Issue 42, 2017
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Reversible core-crosslinked nanocarriers with pH-modulated targeting and redox-controlled drug release for overcoming drug resistance

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Abstract

Herein, a pH and redox dual-sensitive core-crosslinked targeting nanocarrier was prepared and used for co-delivery of doxorubicin (DOX) and tariquidar (TQR). The nanocarrier not only had excellent stability but also prevented the leakage of the drug in the normal physiological environment efficiently. Meanwhile, the targeting function of nanocarriers could also be suppressed in the normal physiological environment, protecting nanocarriers from being captured by RAW264.7 cells. Under mild acidic conditions, the targeting function was regained, leading to an effective tumor cell uptake of the nanocarrier. Furthermore, reduction-responsive drug release would occur in the cytoplasm due to the collapse of the reduction-sensitive crosslinked structure in the nanocarrier. By means of ligand–receptor mediated endocytosis and TQR-mediated glycoprotein (P-gp) inhibition, the IC50 value of DOX to MCF-7/ADR cells reduced from more than 100 μg mL−1 to 8.55 μg mL−1, exhibiting great potential in overcoming drug resistance.

Graphical abstract: Reversible core-crosslinked nanocarriers with pH-modulated targeting and redox-controlled drug release for overcoming drug resistance

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Publication details

The article was received on 05 Jun 2017, accepted on 29 Sep 2017 and first published on 02 Oct 2017


Article type: Paper
DOI: 10.1039/C7TB01504F
Citation: J. Mater. Chem. B, 2017,5, 8399-8407
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    Reversible core-crosslinked nanocarriers with pH-modulated targeting and redox-controlled drug release for overcoming drug resistance

    Dan Zhao, S. Ma, X. Yi, S. Cheng, R. Zhuo and F. Li, J. Mater. Chem. B, 2017, 5, 8399
    DOI: 10.1039/C7TB01504F

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