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Fabrication of paclitaxel hybrid nanomicelles to treat resistant breast cancer via oral administration

Authors Dian LH, Hu YJ, Lin JY, Zhang JY, Yan Y, Cui YN, Su ZB, Lu WL

Received 27 August 2017

Accepted for publication 6 December 2017

Published 2 February 2018 Volume 2018:13 Pages 719—731


Checked for plagiarism Yes

Review by Single anonymous peer review

Peer reviewer comments 2

Editor who approved publication: Dr Lei Yang

Ling-Hui Dian,1,2,* Ying-Jie Hu,1,* Jia-Ye Lin,1 Jing-Ying Zhang,1 Yan Yan,1 Yi-Nuo Cui,1 Zhan-Bo Su,1 Wan-Liang Lu1

1State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing, 2School of Pharmaceutical Sciences, Guangdong Medical University, Dongguan, China

*These authors contributed equally to this work

Aim: Oral chemotherapy using anticancer drugs would improve the clinical practice and the life quality of patients. The aim of the present study was to develop paclitaxel hybrid nanomicelles for oral administration to treat resistant breast cancer.
Methods: Evaluations were performed on human breast cancer MCF-7 cells, drug-resistant breast cancer MCF-7/Adr cells, and in MCF-7/Adr-xenografted BALB/c nude mice. The nanomicelles were composed of the polymer soluplus, d-α-tocopheryl polyethyleneglycol 1000 succinate (TPGS1000), and dequalinium (DQA). The constructed paclitaxel hybrid nanomicelles were ~65 nm in size.
Results: The nanomicelles improved cellular uptake and anticancer efficacy in the resistant breast cancer cells and induced mitochondria-mediated apoptosis. The mechanism of the apoptosis-inducing effect was related to the co-localization of the nanomicelles with mitochondria; the activation of pro-apoptotic protein Bax, cytochrome C, and apoptotic enzymes caspase 9 and 3; and the inhibition of anti-apoptotic proteins Bcl-2 and Mcl-1. Oral administration of paclitaxel hybrid nanomicelles had the same anticancer efficacy as the intravenous injection of taxol in resistant breast cancer-bearing mice. The oral suitability of this formulation was associated with the nanostructure and the actions of TPGS1000 and DQA.
Conclusion: The fabricated paclitaxel hybrid nanomicelles could provide a promising oral formulation to treat drug-resistant breast cancer.

Keywords: paclitaxel, nanomicelles, oral, drug-resistant breast cancer, mice

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