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Diblock Copolymer Glyco-nanomicelles Constructed by Maltoheptaose-based Amphiphile for Reduction- and pH-mediated Intracellular Drug Delivery

Abstract

A new type of reduction- and pH-mediated glyco-polymeric micelles was synthesized for the antitumor drug doxorubicin (DOX) delivery in this study. The micelles were constructed by diblock copolymer (MH-S-S-AcMH) with disulfide linkage between hydrophilic block maltoheptaose (MH) and hydrophobic block acetalated maltoheptaose (AcMH). Experimental results showed that the amphiphilic MH-S-S-AcMH with 20 nm average size could self-assemble into micelles under physiological conditions and rapidly release the conjugated drugs DOX when exposed to weakly acidic (pH = 5) and reductive (10 mM DTT) environment. Fluorescence microscopy detection indicated that the drug carriers can be endocytosed effectively, endowing the anticancer agents flow into cells and suppress the growth of HeLa tumor cells. Compared with DOX at higher dosage and MH-S-S-AcMH micelles which are non-toxic to tumor cells, the cytotoxicity assays manifested that the DOX-loaded MH-S-S-AcMH micelles exhibited a better toxicity to HeLa tumor cells. According to these results, the copolymer mentioned above as the practically non-toxic, high stability, novel reduction- and pH-mediated glyco-polymeric micelles could be empolyed in improving drug delivery efficiency and enhancing anticancer efficacy.

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Publication details

The article was received on 17 Sep 2017, accepted on 12 Feb 2018 and first published on 15 Feb 2018


Article type: Paper
DOI: 10.1039/C7PY01601H
Citation: Polym. Chem., 2018, Accepted Manuscript
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    Diblock Copolymer Glyco-nanomicelles Constructed by Maltoheptaose-based Amphiphile for Reduction- and pH-mediated Intracellular Drug Delivery

    L. Cheng, T. Luan, D. Liu, J. Cheng, H. Li, W. Hua, L. Zhang, J. Lan, Y. Liu and G. Zhao, Polym. Chem., 2018, Accepted Manuscript , DOI: 10.1039/C7PY01601H

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