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Curcumin-loaded redox response of self-assembled micelles for enhanced antitumor and anti-inflammation efficacy

Authors Zhao S, Ma L, Cao C, Yu Q, Chen L, Liu J

Received 26 September 2016

Accepted for publication 27 January 2017

Published 29 March 2017 Volume 2017:12 Pages 2489—2504


Checked for plagiarism Yes

Review by Single anonymous peer review

Peer reviewer comments 2

Editor who approved publication: Dr Lei Yang

Shuang Zhao,1,* Litao Ma,1,* Chengwen Cao,1 Qianqian Yu,1 Lanmei Chen,1,2 Jie Liu1

1Department of Chemistry, Jinan University, Guangzhou, 2Department of Chemistry, School of Pharmacy, Guangdong Medical University, Zhanjiang, People’s Republic of China

*These authors contributed equally to this work

Abstract: At present, it has become evident that inflammation plays a critical role in tumor growth; meanwhile, chemotherapeutic agents using nanocarriers have been suggested as a promising strategy in cancer treatment. In this study, novel redox-responsive micelles were prepared from monomethoxy-poly(ethylene glycol)-chitosan-S-S-hexadecyl (C16-SS-CS-mPEG). These micelles were able to carry and deliver drugs into tumor cells. To serve as a control, monomethoxy-poly(ethylene glycol)-chitosan-C-C-hexadecyl (C16-CC-CS-mPEG) was developed in a similar fashion to that used to yield C16-CC-CS-mPEG without a redox-responsive disulfide bond. The cellular uptake mechanisms of both micelles were determined. The efficient intracellular drug release from micelles in MCF-7 cells was further confirmed. Results indicated that curcumin (Cur) could rapidly form C16-SS-CS-mPEG@Cur micelles when exposed to reducing agents and efficaciously enhance intracellular accumulation. The cytotoxicity assay demonstrated that C16-SS-CS-mPEG@Cur exhibited satisfactory cytotoxicity against MCF-7 cells. Anti-inflammation assay results indicated that C16-SS-CS-mPEG@Cur treatment significantly downregulated tumor necrosis factor (TNF-α) expression and showed good anti-inflammatory effects in tumor microenvironment. Most importantly, antitumor effects in vivo showed satisfactory therapeutic effects with C16-SS-CS-mPEG@Cur. Hence, C16-SS-CS-mPEG@Cur micelles can be useful in tumor therapy.

Keywords: micelles, curcumin, anti-inflammatory effect, anti-tumor effect, tumor

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