Issue 7, 2018

A reactive oxygen species–responsive prodrug micelle with efficient cellular uptake and excellent bioavailability

Abstract

Stimuli-responsive polymeric drug delivery systems are of great interest in anticancer research. Here, a reactive oxygen species (ROS)–responsive prodrug was prepared by thioketal linkage of poly(ethylene glycol) (PEG) and the anticancer drug doxorubicin (DOX). The ROS–responsive property of the prodrug was confirmed by dynamic light scattering and 1H NMR. The prodrug was then used as a drug carrier to further load DOX, to form a DOX-loaded prodrug micelle, which showed dual ROS and pH-responsive release behaviors. The prodrug micelle exhibited rapid intracellular uptake. Interestingly, the in vitro anticancer activity of the ROS–responsive prodrug micelle was better than that of the DOX-loaded prodrug micelle because of its faster cellular uptake and better bioavailability. However, both the ROS–responsive prodrug and drug-loaded prodrug micelles showed better anticancer efficacy than a non-responsive DOX-loaded poly(ethylene glycol)-block-polycaprolactone (PEG2k-PCL5k) micelle. Consistent results were obtained in in vivo animal experiments as the antitumor efficacy of the prodrug micelle was superior to that of the DOX-loaded prodrug micelle. Both micelles showed negligible systemic toxicity in vivo.

Graphical abstract: A reactive oxygen species–responsive prodrug micelle with efficient cellular uptake and excellent bioavailability

Supplementary files

Article information

Article type
Paper
Submitted
15 Sep 2017
Accepted
22 Jan 2018
First published
23 Jan 2018

J. Mater. Chem. B, 2018,6, 1076-1084

A reactive oxygen species–responsive prodrug micelle with efficient cellular uptake and excellent bioavailability

L. Xu, Y. Yang, M. Zhao, W. Gao, H. Zhang, S. Li, B. He and Y. Pu, J. Mater. Chem. B, 2018, 6, 1076 DOI: 10.1039/C7TB02479G

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