Back to Journals » International Journal of Nanomedicine » Volume 9 » Issue 1

Self-assembled micelles of novel amphiphilic copolymer cholesterol-coupled F68 containing cabazitaxel as a drug delivery system

Authors Song Y, Tian Q, Huang Z, Fan D, She Z, Liu X, Cheng X, Yu B, Deng Y

Received 23 January 2014

Accepted for publication 23 February 2014

Published 12 May 2014 Volume 2014:9(1) Pages 2307—2317

DOI https://doi.org/10.2147/IJN.S61220

Checked for plagiarism Yes

Review by Single-blind

Peer reviewer comments 3

Yanzhi Song,1 Qingjing Tian,1 Zhenjun Huang,1 Di Fan,1 Zhennan She,1 Xinrong Liu,1 Xiaobo Cheng,1 Bin Yu,2 Yihui Deng1

1College of Pharmacy, Shenyang Pharmaceutical University, 2Liaoning Medical Device Test Institute, Shenyang, People’s Republic of China

Abstract: Despite being one of the most promising amphiphilic block copolymers, use of Pluronic F68 in drug delivery is limited due to its high critical micelle concentration (CMC). In this study, we developed a novel F68 derivative, cholesterol-coupled F68 (F68-CHMC). This new derivative has a CMC of 10 µg/mL, which is 400-fold lower than that of F68. The drug-loading capacity of F68-CHMC was investigated by encapsulating cabazitaxel, a novel antitumor drug. Drug-loaded micelles were fabricated by a self-assembly method with simple dilution. The optimum particle size of the micelles was 17.5±2.1 nm, with an entrapment efficiency of 98.1% and a drug loading efficiency of 3.16%. In vitro release studies demonstrated that cabazitaxel-loaded F68-CHMC micelles had delayed and sustained-release properties. A cytotoxicity assay of S180 cells showed that blank F68-CHMC was noncytotoxic with a cell viability of nearly 100%, even at a concentration of 1,000 µg/mL. The IC50 revealed that cabazitaxel-loaded F68-CHMC micelles were more cytotoxic than Tween 80-based cabazitaxel solution and free cabazitaxel. In vivo antitumor activity against S180 cells also indicated better tumor inhibition by the micelles (79.2%) than by Tween 80 solution (56.2%, P<0.05). Based on these results, we conclude that the F68-CHMC copolymer may be a potential nanocarrier to improve the solubility and biological activity of cabazitaxel and other hydrophobic drugs.

Keywords: Pluronic F68, cholesterol, synthesis, cabazitaxel, micelles, cancer therapy

Creative Commons License This work is published and licensed by Dove Medical Press Limited. The full terms of this license are available at https://www.dovepress.com/terms.php 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]

 

Other articles by this author:

Accelerated blood clearance phenomenon upon cross-administration of PEGylated nanocarriers in beagle dogs

Wang CL, Cheng XB, Su YQ, Pei Y, Song YZ, Jiao J, Huang ZJ, Ma YF, Dong YM, Yao Y, Fan JJ, Ta H, Liu XR, Xu H, Deng YH

International Journal of Nanomedicine 2015, 10:3533-3545

Published Date: 14 May 2015

Tolerance-like innate immunity and spleen injury: a novel discovery via the weekly administrations and consecutive injections of PEGylated emulsions

Wang L, Wang C, Jiao J, Su Y, Cheng X, Huang Z, Liu X, Deng Y

International Journal of Nanomedicine 2014, 9:3645-3657

Published Date: 4 August 2014

The application of EDTA in drug delivery systems: doxorubicin liposomes loaded via NH4EDTA gradient

Song YZ, Huang ZJ, Song Y, Tian QJ, Liu XR, She ZN, Jiao J, Lu E, Deng YH

International Journal of Nanomedicine 2014, 9:3611-3621

Published Date: 1 August 2014

Effect of particle size on solubility, dissolution rate, and oral bioavailability: evaluation using coenzyme Q10 as naked nanocrystals

Sun J, Wang F, Sui Y, She Z, Zhai W, Wang C, Deng Y

International Journal of Nanomedicine 2012, 7:5733-5744

Published Date: 12 November 2012

Repeated injection of PEGylated solid lipid nanoparticles induces accelerated blood clearance in mice and beagles

Zhao Y, Wang L, Yan M, Ma Y, Zang G, She Z, Deng Y

International Journal of Nanomedicine 2012, 7:2891-2900

Published Date: 12 June 2012

Readers of this article also read:

Green synthesis of water-soluble nontoxic polymeric nanocomposites containing silver nanoparticles

Prozorova GF, Pozdnyakov AS, Kuznetsova NP, Korzhova SA, Emel’yanov AI, Ermakova TG, Fadeeva TV, Sosedova LM

International Journal of Nanomedicine 2014, 9:1883-1889

Published Date: 16 April 2014

Methacrylic-based nanogels for the pH-sensitive delivery of 5-Fluorouracil in the colon

Ashwanikumar N, Kumar NA, Nair SA, Kumar GS

International Journal of Nanomedicine 2012, 7:5769-5779

Published Date: 15 November 2012

A novel preparation method for silicone oil nanoemulsions and its application for coating hair with silicone

Hu Z, Liao M, Chen Y, Cai Y, Meng L, Liu Y, Lv N, Liu Z, Yuan W

International Journal of Nanomedicine 2012, 7:5719-5724

Published Date: 12 November 2012

Cross-linked acrylic hydrogel for the controlled delivery of hydrophobic drugs in cancer therapy

Deepa G, Thulasidasan AK, Anto RJ, Pillai JJ, Kumar GS

International Journal of Nanomedicine 2012, 7:4077-4088

Published Date: 27 July 2012

Servant leadership: a case study of a Canadian health care innovator

Vanderpyl TH

Journal of Healthcare Leadership 2012, 4:9-16

Published Date: 16 February 2012

Corrigendum: Softec HD hydrophilic acrylic intraocular lens: biocompatibility and precision

Espandar L, Sikder S, Moshirfar M

Clinical Ophthalmology 2011, 5:159-160

Published Date: 6 February 2011

Crystallization after intravitreal ganciclovir injection

Pitipol Choopong, Nattaporn Tesavibul, Nattawut Rodanant

Clinical Ophthalmology 2010, 4:709-711

Published Date: 14 July 2010