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Colloids Surf B Biointerfaces. 2014 Mar 1;115:164-9. doi: 10.1016/j.colsurfb.2013.11.039. Epub 2013 Nov 27.

Nanocapsules based on mPEGylated artesunate prodrug and its cytotoxicity.

Author information

1
Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, East China Normal University, Shanghai 200062, PR China.
2
College of Chemical Engineering, Wuhan University of Technology, Wuhan 430070, PR China.
3
Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, East China Normal University, Shanghai 200062, PR China. Electronic address: jhyu@sist.ecnu.edu.cn.
4
Department of Diagnostic Imaging, Changzheng Hospital, Shanghai 200003, PR China.
5
The Commonwealth Scientific and Industrial Research Organisation, Bayview Avenue, Bag 10, Clayton South, Melbourne, Victoria 3169, Australia.

Abstract

mPEGylated artesunate prodrug was synthesized via esterification between poly(ethylene glycol) monomethyl ether (mPEG) and artesunate (ART). The product was inclined to form nanocapsules in aqueous media due to its amphiphilic nature. These nanocapsules showed narrow size distribution, with an average particle size of 88.7 nm measured by dynamic laser scattering (DLS). Their vesical morphology was further confirmed by transmission electron microscopy (TEM). We found that the release of ART from the nanocapsules was controllable, which was contributed to the easily hydrolyzed property of the ester bond. In addition, the cytotoxicity of the prodrug against L1210 and MCF7 cell lines showed an essential decrease compared with the free ART. These results present a new strategy in designing anti-tumor ART nanocapsules for targeting tumor cells.

KEYWORDS:

Artesunate; Controllable release; Nanocapsules; Passive targeting; mPEGylation

PMID:
24334269
DOI:
10.1016/j.colsurfb.2013.11.039
[Indexed for MEDLINE]

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