期刊
CARBOHYDRATE POLYMERS
卷 176, 期 -, 页码 107-116出版社
ELSEVIER SCI LTD
DOI: 10.1016/j.carbpol.2017.08.011
关键词
Apatinib; Carboxymethyl; chitosan-graft-poly-(epsilon-caprolactone); Micelles; pH-responsive; Drug delivery system; Anti-angiogenesis
资金
- National Key Research and Development Program [2016YFC1100703]
In this study, carboxymethyl chitosan-graft-poly-(epsilon-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 100-150 nm at pH 7.4 while aggregated to 300-350 nm 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 0.125 mu g/ml, CPA micelles had significant inhibiting effect on HUVECs as IC50 was near 3.125 tig/ml, and the drug effect could be adjusted by altering grafting ratio of CMCS-g-PCL. These results suggest that CPA micelles may be used as an effective drug delivery system for anti-angiogenesis cancer therapy. (C) 2017 Elsevier Ltd. All rights reserved.
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