Please use this identifier to cite or link to this item:
Title: Selectivity of folate conjugated polymer micelles against different tumor cells
Authors: Zhao, H.
Yung, L.Y.L. 
Keywords: Doxorubicin
Drug targeting
Polymer micelle
Issue Date: 12-Feb-2008
Citation: Zhao, H., Yung, L.Y.L. (2008-02-12). Selectivity of folate conjugated polymer micelles against different tumor cells. International Journal of Pharmaceutics 349 (1-2) : 256-268. ScholarBank@NUS Repository.
Abstract: Folate or folic acid has been employed as a targeting moiety of various anticancer agents to increase their cellular uptake within target cells since folate receptors are vastly overexpressed in several human tumors. In this study, a biodegradable polymer poly(d,l-lactide-co-glycolide)-poly(ethylene glycol)-folate (PLGA-PEG-FOL) was used to form micelles for encapsulating anticancer drug doxorubicin (DOX). The drug loading content, encapsulation efficiency and in vitro release were characterized. To evaluate the targeting ability of the folate conjugated micelles, the cytotoxicity and cellular uptake of DOX-loaded micelles on three cancer cell lines with different amount of folate receptors (KB, MATB III, C6) and normal fibroblast cells (CCL-110) were compared. The cytotoxicity of PLGA-PEG-FOL micelles to cancer cells was found to be much higher than that of normal fibroblast cells, demonstrating that the folate conjugated micelles has the ability to selectively target to cancer cells. For normal cells, the cellular uptake of PLGA-PEG-FOL micelles was similar to PLGA-PEG micelles without folate conjugation, and was substantially lower than that of cancer cells. In addition, the cell cycle analysis showed that the apoptotic percentage of normal fibroblasts was substantially lower compared with the cancer cells after exposing to DOX-loaded PLGA-PEG-FOL micelles. An optimal folate amount of approximately 40-65% on the micelles was found to be able to kill cancer cells but, at the same time, to have very low effect to normal cells. © 2007 Elsevier B.V. All rights reserved.
Source Title: International Journal of Pharmaceutics
ISSN: 03785173
DOI: 10.1016/j.ijpharm.2007.07.040
Appears in Collections:Staff Publications

Show full item record
Files in This Item:
There are no files associated with this item.


checked on Mar 18, 2019


checked on Mar 18, 2019

Page view(s)

checked on Mar 9, 2019

Google ScholarTM



Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.