Issue 15, 2012

Reducible self-assembled micelles for enhanced intracellular delivery of doxorubicin

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

Article information

Article type
Paper
Submitted
18 Oct 2011
Accepted
03 Jan 2012
First published
24 Jan 2012

J. Mater. Chem., 2012,22, 7121-7129

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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