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Issue 8, 2016
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Construction of coumarin-based cross-linked micelles with pH responsive hydrazone bond and tumor targeting moiety

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Abstract

It is still a major challenge for targeted cancer chemotherapy to design a stable biocompatible micellar drug delivery system. To address this dilemma, novel responsive cross-linked micelles (x-micelles) based on polyurethane with photo-responsive coumarin derivatives and pH-responsive hydrazone groups were synthesized. The polymers could be self-assembled into micelles using a typical and facile way. The x-micelles were stable at physiological conditions after UV light induced cross-linking, and can be disassociated under acidic condition. The drug loading content (DLC) and the encapsulation efficiency (EE) of the obtained x-micelles (15.2% and 60.8% respectively) were higher than those of micelles (9.8% and 39.2% respectively), and the DOX release rate of x-micelles was also improved. For targeted therapy, folic acid (FA) was then conjugated to x-micelles, resulting in x-micelles–FA. Cellular viability experiments show that both x-micelles and micelles had a low cytotoxicity and good biocompatibility of up to 1000 μg mL−1, and DOX-loaded x-micelles–FA and x-micelles exhibited half-maximal inhibitory concentration (IC50) values of 1.17 and 2.40 μg mL−1, respectively, to HeLa cells, but have lower cytotoxicity to L929 cells. The pH-responsive x-micelles–FA exhibited superior extracellular stability but activated intracellular drug release. We have demonstrated that the polyurethane with UV- and pH-responsive properties as a novel platform for tumor-targeting drug delivery.

Graphical abstract: Construction of coumarin-based cross-linked micelles with pH responsive hydrazone bond and tumor targeting moiety

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Supplementary files

Article information


Submitted
24 Dec 2015
Accepted
27 Jan 2016
First published
28 Jan 2016

J. Mater. Chem. B, 2016,4, 1480-1488
Article type
Paper

Construction of coumarin-based cross-linked micelles with pH responsive hydrazone bond and tumor targeting moiety

Y. Long, W. Gu, C. Pang, J. Ma and H. Gao, J. Mater. Chem. B, 2016, 4, 1480
DOI: 10.1039/C5TB02729B

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