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Front. Pharmacol. | doi: 10.3389/fphar.2018.00118

Complete Suppression of Non-small-cell Lung Cancer by Hydrophobic Poly(ester amide) Nanoparticles with High Docetaxel Loading

Xing Chen1, Lili Zhao2, Yang Kang3,  Zhiyu He1, Fei Xiong1, Xiang Ling1* and  Jun Wu1*
  • 1School of Engineering, Sun Yat-sen University, China
  • 2Department of Endoscopy, Jiangsu Province Hospital, China
  • 3Key Laboratory of Mountain Ecological Restoration and Bioresource Utilization, Chengdu Institute of Biology (CAS), China

Non-small-cell lung cancer (NSCLC) accounts for over 85% of clinical lung cancer cases, which are the leading cause of cancer-related death. To develop new therapeutic strategy for NSCLC, a library of L-phenylalanine-based poly(ester amide) (Phe-PEA) polymers was synthesized and assembled with docetaxel (Dtxl) to form Dtxl-loaded Phe-PEA nanoparticles. The hydrophobic Phe-PEA polymers are able to form nanoparticles by nanoprecipitation method and the characterization results showed that the screened Dtxl-8P4 NPs have small particle size (~100 nm) and high Dtxl loading (~20 wt%). In vitro experiments showed that Dtxl-8P4 NPs were rapidly trafficked into cancer cells, then effectively escaped from lysosomal degradation and achieved significant tumor cell inhibition. In vivo results demonstrated Dtxl-8P4 NPs with prolonged blood circulation could efficiently deliver Dtxl to A549 tumor sites, lead to reduced cell proliferation, block metastasis and increase apoptosis, then persistent inhibition of tumor growth. Therefore, Phe-PEA NPs are abble to load high amount of hydrophobic drugs and could be a promising therapeutic approach for NSCLC and other cancer treatments.

Keywords: Cancer, DOCETAXEL, hydrophobicity, nanoparticle, Poly(ester amide)

Received: 18 Jan 2018; Accepted: 01 Feb 2018.

Edited by:

Jianxun Ding, Changchun Institute of Applied Chemistry (CAS), China

Reviewed by:

Guoming Sun, Sunogel Biotechnologies Inc, United States
Yue Pan, Soochow University, China
Weiping Wang, University of Hong Kong, Hong Kong  

Copyright: © 2018 Chen, Zhao, Kang, He, Xiong, Ling and Wu. This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.

* Correspondence:
Dr. Xiang Ling, Sun Yat-sen University, School of Engineering, Guangzhou, China,
Prof. Jun Wu, Sun Yat-sen University, School of Engineering, Guangzhou, China,