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A ROS-Responsive Polymeric Micelle with π-Conjugated Thioketal Moiety for Enhanced Drug Loading and Efficient Drug Delivery

Abstract

As the implications of reactive oxygen species (ROS) are elucidated in many diseases, ROS-responsive nanoparticles are attracting great interest of researchers. In this work, a ROS sensitive thioketal (TK) moiety with π-conjugated structure was introduced in biodegradable methoxy poly(ethylene glycol)-thioketal-poly(-caprolactone)mPEG-TK-PCL micelles as a linker, which was designed to speed up the drug release and thus enhance the therapeutic efficacy. The micelle showed a high drug loading content of xx% and excellent stability in physiological conditions because of the evocation of π-π stacking and hydrophobic interactions with the anticancer drug doxorubicin (DOX). The polymeric micelle presented a better drug carrier capacity and higher in vitro anticancer efficacy to cancer cells. The in vivo study showed that DOX-loaded mPEG-TK-PCL micelles displayed lower toxicity to normal cells and remarkably enhanced antitumor efficacy. This research provides a way of designing potential drug carriers for efficient cancer chemotherapy.

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Publication details

The article was received on 10 Aug 2017, accepted on 09 Oct 2017 and first published on 09 Oct 2017


Article type: Paper
DOI: 10.1039/C7OB01975K
Citation: Org. Biomol. Chem., 2017, Accepted Manuscript
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    A ROS-Responsive Polymeric Micelle with π-Conjugated Thioketal Moiety for Enhanced Drug Loading and Efficient Drug Delivery

    C. Sun, Y. Liang, N. Hao, L. Xu, F. Cheng, T. Su, J. Cao, Y. Pu, W. Gao and B. He, Org. Biomol. Chem., 2017, Accepted Manuscript , DOI: 10.1039/C7OB01975K

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