期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 19, 期 13, 页码 4057-4066出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2011.05.016
关键词
Folate receptor; PLGA nanoparticles; Endometrial carcinoma; Drug targeting; Paclitaxel
资金
- Guangzhou Municipal Science and Technology [2007Z3-E0601]
- Guangdong province Science and Technology Program [2007B030502014]
- National Natural Science Foundation of China [30772332]
Folate (FOL) mediated poly-lactide-co-glycolide-polyethylene glycol nanoparticles (FOL-PEG-PLGA NPs) bearing paclitaxel (PTX) were prepared for the effective delivery of drug to endometrial carcinoma. The average size, zeta potential and encapsulation efficiency of FOL-targeted NPs were found to be around 220 nm, -30.43 mV and 95.6%. Cellular uptake was observed. The accumulation of FOL-targeted NPs depends on dual effects of passive and active targeting. The FOL-targeted PTX NPs showed a greater cytotoxicity against HEC-1A cancer cells in vitro and in vivo, which might be induced by apoptosis. H&E staining did not showed apparent tissue damage to liver and kidney of the mice after injecting NPs intravenously. These results suggest that the novel FOL-PEG-PLGA NPs could be a potential delivery system with excellent therapeutic efficacy for targeting the drugs to cancer cells. (C) 2011 Elsevier Ltd. All rights reserved.
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