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Mol Pharm. 2017 Nov 6;14(11):4032-4041. doi: 10.1021/acs.molpharmaceut.7b00704. Epub 2017 Oct 16.

Acid-Activatable Theranostic Unimolecular Micelles Composed of Amphiphilic Star-like Polymeric Prodrug with High Drug Loading for Enhanced Cancer Therapy.

Shi X1,2, Hou M1,2, Bai S1,2, Ma X1,2, Gao YE1,2, Xiao B1,3, Xue P1,2, Kang Y1,2, Xu Z1,2, Li CM1,2.

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Institute for Clean Energy and Advanced Materials, Faculty of Materials and Energy, Southwest University , Chongqing 400715, P. R. China.
Chongqing Engineering Research Centre for Micro-Nano Biomedical Materials and Devices , Chongqing 400715, P.R. China.
Institute for Biomedical Sciences, Center for Diagnostics and Therapeutics, Georgia State University , Atlanta, Georgia 30302, United States.


Stimuli-responsive nanomedicine with theranostic functionalities with reduced side-effects has attracted growing attention, although there are some major obstacles to overcome before clinical applications. Herein, we present an acid-activatable theranostic unimolecular micelles based on amphiphilic star-like polymeric prodrug to systematically address typical existing issues. This smart polymeric prodrug has a preferable size of about 35 nm and strong micellar stability in aqueous solution, which is beneficial to long-term blood circulation and efficient extravasation from tumoral vessels. Remarkably, the polymeric prodrug has a high drug loading rate up to 53.1 wt%, which induces considerably higher cytotoxicity against tumor cells (HeLa cells and MCF-7 cells) than normal cells (HUVEC cells) suggesting a spontaneous tumor-specific targeting capability. Moreover, the polymeric prodrug can serve as a fluorescent nanoprobe activated by the acidic microenvironment in tumor cells, which can be used as a promising platform for tumor diagnosis. The superior antitumor effect in this in vitro study demonstrates the potential of this prodrug as a promising platform for drug delivery and cancer therapy.


acid-activatable; cancer therapy; drug delivery; polymeric prodrug; unimolecular micelles

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