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Activated Charge-Reversal Polymeric Nano-System: The Promising Strategy in Drug Delivery for Cancer Therapy

School of Pharmacy and Bioengineering, Chengdu University, Chengdu 610106, China
State Key Laboratory of Silicate Materials for Architectures, Wuhan University of Technology, Wuhan 430070, China
School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China
State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao 999078, China
Department of Microbiology & Immunology, MCV Campus School of Medicine, Virginia Commonwealth University, Richmond, VA 23284, USA
Authors to whom correspondence should be addressed.
Academic Editor: Christine Wandrey
Polymers 2016, 8(4), 99;
Received: 29 January 2016 / Revised: 10 March 2016 / Accepted: 14 March 2016 / Published: 5 April 2016
(This article belongs to the Collection Polyelectrolytes)
Various polymeric nanoparticles (NPs) with optimal size, tumor-targeting functionalization, or microenvironment sensitive characteristics have been designed to solve several limitations of conventional chemotherapy. Nano-sized polymeric drug carrier systems have remarkably great advantages in drug delivery and cancer therapy, which are still plagued with severe deficiencies, especially insufficient cellular uptake. Recently, surface charge of medical NPs has been demonstrated to play an important role in cellular uptake. NPs with positive charge show higher affinity to anionic cell membranes such that with more efficient cellular internalization, but otherwise cause severe aggregation and fast clearance in circulation. Thus, surface charge-reversal NPs, specifically activated at the tumor site, have shown to elegantly resolve the enhanced cellular uptake in cancer cells vs. non-specific protein adsorption dilemma. Herein, this review mainly focuses on the effect of tumor-site activated surface charge reversal NPs on tumor treatment, including the activated mechanisms and various applications in suppressing cancer cells, killing cancer stem cell and overcoming multidrug resistance, with the emphasis on recent research in these fields. With the comprehensive and in-depth understanding of the activated surface charge reversal NPs, this approach might arouse great interest of scientific research on enhanced efficient polymeric nano-carriers in cancer therapy. View Full-Text
Keywords: polymeric nano-carriers; polyelectrolytes; drug delivery; surface charge; cellular uptake polymeric nano-carriers; polyelectrolytes; drug delivery; surface charge; cellular uptake
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MDPI and ACS Style

Hu, Y.; Gong, X.; Zhang, J.; Chen, F.; Fu, C.; Li, P.; Zou, L.; Zhao, G. Activated Charge-Reversal Polymeric Nano-System: The Promising Strategy in Drug Delivery for Cancer Therapy. Polymers 2016, 8, 99.

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