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Issue 15, 2012
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Reducible self-assembled micelles for enhanced intracellular delivery of doxorubicin

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Abstract

This study developed novel reducible micelles that are approximately 100 nm in diameter and consist of poly(β-amino ester)-graft-poly(ethylene glycol) amphiphilic copolymers (PAE) with phenylbutylamine functional side groups. Our report is unique in the following ways: (1) the reductively degradable micelles provide a safe and efficient doxorubicin intracellular delivery, (2) the synthesis procedure is a simple and mild pathway with a well-defined structure, and (3) the aromatic phenylbutylamine side groups increase hydrophobicity and strengthen the interaction with doxorubicin (DOX) to improve the drug-loading capability. In vitro, micelles exhibit faster release of DOX upon the action of dithiothreitol (DTT). Drug-laden micelles present higher cell inhibition efficiency in comparison to free doxorubicin, while the blank micelles show very low cytotoxicity. The copolymeric micelles show a rapid internalization and efficient cytoplasmic doxorubicin release in both human hepatocellular carcinoma HepG2 and human breast adenocarcinoma MCF-7 cell lines observed by confocal laser scanning microscopy (CLSM). The micelle is promising for enhanced intracellular drug delivery in tumour cells.

Graphical abstract: Reducible self-assembled micelles for enhanced intracellular delivery of doxorubicin

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Publication details

The article was received on 18 Oct 2011, accepted on 03 Jan 2012 and first published on 24 Jan 2012


Article type: Paper
DOI: 10.1039/C2JM15277K
J. Mater. Chem., 2012,22, 7121-7129

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    Reducible self-assembled micelles for enhanced intracellular delivery of doxorubicin

    J. Chen, F. Zehtabi, J. Ouyang, J. Kong, W. Zhong and M. M. Q. Xing, J. Mater. Chem., 2012, 22, 7121
    DOI: 10.1039/C2JM15277K

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