期刊
INTERNATIONAL JOURNAL OF PHARMACEUTICS
卷 443, 期 1-2, 页码 110-119出版社
ELSEVIER
DOI: 10.1016/j.ijpharm.2012.12.042
关键词
Controlled release; Indomethacin; Cyclodextrin-conjugates; Micelle; Cytotoxicity
资金
- National Natural Science Foundation of China [51073102]
- Fok Ying Tung Education Foundation [122034]
- Program for New Century Excellent Talents in University [NCET-10-0592]
- Program for Changjiang Scholars and Innovative Research Team in University [IRT1163]
- Foundations of Sichuan Province [2012JQ0009]
- Fundamental Research Funds for the Central Universities [2010SCU22001, 2011SCU04A04]
- Natural Science Foundation of Jiangsu Province [BK2010248, BK2011340]
Cyclodextrin-conjugated poly(lactic acid)-b-poly(ethylene glycol) (beta-CD-PLA-mPEG), a well-defined amphiphilic copolymer, was synthesized by controlled ring-open copolymerization and click coupling reaction, in order to obtain a biocompatible drug delivery system with controlled release profiles. The beta-CD-PLA-mPEG copolymer could self-assemble in aqueous solution to form micelles with a mean particle size of 173.4 nm, which will decrease to 159.2 nm after loaded with a kind of hydrophobic drug (indomethacin, IND). The IND-loaded beta-CD-PLA-mPEG micelles show spherical shape within the nano-size scale under TEM imaging. Compared with that formed by PLA-mPEG, the micelles formed by beta-CD-PLA-mPEG copolymer present higher drug loading efficiency and controlled release profile of IND, especially in the control of its initial burst release. Meanwhile, beta-CD-PLA-mPEG copolymer exhibits low toxicity to cells. The micelles formed by beta-CD-PLA-mPEG copolymer could be a promising controlled release system for various hydrophobic drugs. (c) 2013 Elsevier B.V. All rights reserved.
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