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pH-responsive carboxymethyl chitosan-derived micelles as apatinib carriers for effective anti-angiogenesis activity: Preparation and in vitro evaluation.

Carbohydr Polym.. 2017-11; 
Dai Y, Wang S, Shi W, Lang M.
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摘要

In this study, carboxymethyl chitosan-graft-poly-(ε-caprolactone) copolymers (CMCS-g-PCL) were synthesized and used to encapsulate apatinib to prepare apatinib-loaded CMCS-g-PCL (CPA) micelles. CPA micelles' sizes were 100-150nm at pH 7.4 while aggregated to 300-350nm at pH 6.4, and the release rate at pH 6.4 was faster than pH 7.4, indicating CPA micelles have a pH-responsive activity. Furthermore, the release rate decreased with an increased grafting ratio of CMCS-g-PCL, which was shown by the results of release experiments from CPA-2 to CPA-10 micelles. A series of cell experiments demonstrated that blank micelles were non-toxic for human umbilical endothelial cells (HUVECs) below 0.125mg/ml, CPA micelles h... More

关键词

Anti-angiogenesis; Apatinib; Carboxymethyl chitosan-graft-poly-(ε-caprolactone); Drug delivery system; Micelles; pH-responsive