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H2O2-responsive polymeric micelle with a benzil moiety for efficient DOX delivery and AIE Imaging


Nano drug delivery is a promising domain in biomedical theranostic and has aroused more and more attention in recent years. We report here an amphiphilic polymer TPG1, bearing H2O2-sensitive benzil and AIE fluorephore tetraphenylethene (TPE) unit, which was able to self-assemble into spherical nanosized micelles in aqueous solution. Doxorubicin (DOX) can be encapsulated into the TPG1 micelles efficiently with the loading capability up to 59% by weight. The benzil moiety could be cleaved via Baeyer-Villiger type reaction in the presence of H2O2, leading to the decomposition of TPG1 micelles and release of DOX. In vitro studies indicated that DOX-loaded TPG1 micelles can be internalized by cancer cells, followed by unloading encapsulated DOX under the stimulation of H2O2. The drug release process can be monitored by the AIE fluorescence from the degradation products containing TPE moiety. MTT assays against HeLa and HepG2 cancer cells demonstrated that DOX-loaded micelles showed a good anticancer efficacy. The polymer TPG1 and corresponding decomposed products showed great biocompatibility. Our data suggest that TPG1 have the potential to be employed for the controlled drug delivery system.

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Publication details

The article was received on 14 Apr 2019, accepted on 08 May 2019 and first published on 09 May 2019

Article type: Paper
DOI: 10.1039/C9OB00859D
Org. Biomol. Chem., 2019, Accepted Manuscript

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    H2O2-responsive polymeric micelle with a benzil moiety for efficient DOX delivery and AIE Imaging

    Y. Dai, X. Sun, W. Sun, J. Yang, R. Liu, Y. Luo, T. Zhang, Y. Tian, Z. Lu and L. He, Org. Biomol. Chem., 2019, Accepted Manuscript , DOI: 10.1039/C9OB00859D

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