Back to Journals » International Journal of Nanomedicine » Volume 7

Folate-mediated targeted and intracellular delivery of paclitaxel using a novel deoxycholic acid-O-carboxymethylated chitosan–folic acid micelles

Authors Wang, Chen Y, Zhang D, Zhang Q, Zheng D, Hao L, Liu Y, Duan C, Jia L, Liu G

Received 1 November 2011

Accepted for publication 24 November 2011

Published 18 January 2012 Volume 2012:7 Pages 325—337


Review by Single-blind

Peer reviewer comments 3

Feihu Wang1, Yuxuan Chen2, Dianrui Zhang1, Qiang Zhang3, Dandan Zheng1, Leilei Hao1, Yue Liu1, Cunxian Duan1, Lejiao Jia1, Guangpu Liu1
1Department of Pharmaceutics, College of Pharmacy, Shandong University, Jinan, People’s Republic of China; 2Department of Pharmacy, Shenzhou Hospital, Shenyang, People’s Republic of China; 3State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing, People’s Republic of China

Background: A critical disadvantage for successful chemotherapy with paclitaxel (PTX) is its nontargeting nature to cancer cells. Folic acid has been employed as a targeting ligand of various anticancer agents to increase their cellular uptake within target cells since the folate receptor is overexpressed on the surface of such tumor cells. In this study, a novel biodegradable deoxycholic acid-O-carboxymethylated chitosan–folic acid conjugate (DOMC-FA) was used to form micelles for encapsulating the anticancer drug PTX.
Methods and results: The drug-loading efficiency, encapsulation efficiency, in vitro drug release and physicochemical properties of PTX-loaded micelles were investigated in detail. In vitro cell culture studies were carried out in MCF-7 cells, a human breast carcinoma cell line, with folate receptor overexpressed on its surface. An increased level of uptake of folate-conjugated micelles compared to plain micelles in MCF-7 cells was observed, and the enhanced uptake of folate-micelles mainly on account of the effective process of folate receptor-mediated endocytosis. The MTT assay, morphological changes, and apoptosis test implied that the folate-conjugated micelles enhanced the cell death by folate-mediated active internalization, and the cytotoxicity of the FA-micellar PTX (DOMC-FA/PTX) to cancer cells was much higher than micelles without folate (DOMC/PTX) or the commercially available injectable preparation of PTX (Taxol).
Conclusion: Results indicate that the PTX-loaded DOMC-FA micelle is a successful anticancer-targeted drug-delivery system for effective cancer chemotherapy.

Keywords: paclitaxel, folate, polymeric micelles, targeted delivery

Creative Commons License This work is published and licensed by Dove Medical Press Limited. The full terms of this license are available at and incorporate the Creative Commons Attribution - Non Commercial (unported, v3.0) License. By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. For permission for commercial use of this work, please see paragraphs 4.2 and 5 of our Terms.

Download Article [PDF]  View Full Text [HTML][Machine readable]


Readers of this article also read:

Molecular targets in arthritis and recent trends in nanotherapy

Roy K, Kanwar RK, Kanwar JR

International Journal of Nanomedicine 2015, 10:5407-5420

Published Date: 26 August 2015

Is increasing the dose of Entecavir effective in partial virological responders?

Erturk A, Adnan Akdogan R, Parlak E, Cure E, Cumhur Cure M, Ozturk C

Drug Design, Development and Therapy 2014, 8:621-625

Published Date: 29 May 2014

Vincristine sulfate liposomal injection for acute lymphoblastic leukemia

Soosay Raj TA, Smith AM, Moore AS

International Journal of Nanomedicine 2013, 8:4361-4369

Published Date: 6 November 2013

Photodynamic therapy of a 2-methoxyestradiol tumor-targeting drug delivery system mediated by Asn-Gly-Arg in breast cancer

Shi J, Wang Z, Wang L, Wang H, Li L, Yu X, Zhang J, Ma R, Zhang Z

International Journal of Nanomedicine 2013, 8:1551-1562

Published Date: 19 April 2013

Controlled-release approaches towards the chemotherapy of tuberculosis

Saifullah B, Hussein MZ, Hussein Al Ali SH

International Journal of Nanomedicine 2012, 7:5451-5463

Published Date: 12 October 2012

Systematic in-vitro evaluation of the NCI/NIH Developmental Therapeutics Program Approved Oncology Drug Set for the identification of a candidate drug repertoire for MLL-rearranged leukemia

Hoeksema KA, Jayanthan A, Cooper T, Gore L, Trippett T, Boklan J, Arceci RJ, Narendran A

OncoTargets and Therapy 2011, 4:149-168

Published Date: 5 September 2011