文献类型：期刊文献

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

作者：Dai, Yixing[1];Wang, Shuo[2,3,4];Shi, Weibin[2,3,4];Lang, Meidong[1,5]

机构：[1]East China Univ Sci & Technol, Sch Mat Sci & Engn, Key Lab Adv Polymer Mat, Shanghai 200237, Peoples R China;[2]Shanghai Jiao Tong Univ, Sch Med, Xinhua Hosp, Dept Gen Surg, Shanghai 200092, Peoples R China;[3]Shanghai Jiao Tong Univ, Sch Med, Xinhua Hosp, Lab Gen Surg, Shanghai 200092, Peoples R China;[4]Shanghai Jiao Tong Univ, Inst Biliary Tract Dis Res, Sch Med, Shanghai 200092, Peoples R China;[5]Shanghai Collaborat Innovat Ctr Biomfg, 130 Meilong Rd, Shanghai 200237, Peoples R China

年份：2017

卷号：176

起止页码：107

外文期刊名：CARBOHYDRATE POLYMERS

收录：;EI(收录号：20173504093324);WOS:【SCI-EXPANDED(收录号:WOS:000410970900013)】；

基金：This research was supported by the National Key Research and Development Program (2016YFC1100703).

语种：英文

外文关键词：Apatinib; Carboxymethyl; chitosan-graft-poly-(epsilon-caprolactone); Micelles; pH-responsive; Drug delivery system; Anti-angiogenesis

摘要：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.