文献类型：期刊文献

英文题名：Folate receptor targeted bufalin/β-cyclodextrin supramolecular inclusion complex for enhanced solubility and anti-tumor efficiency of bufalin

作者：Zou Aihua[1,2];Zhao Xiaotong[1,2];Handge, Ulrich A.[5];Garamus, Vasil M.[6];Willumeit-Roemer, Regine[6];Peihao, Yin[3,4]

机构：[1]East China Univ Sci & Technol, State Key Lab Bioreactor Engn, Shanghai Key Lab Funct Mat Chem, Shanghai 200237, Peoples R China;[2]East China Univ Sci & Technol, Sch Chem & Mol Engn, Inst Appl Chem, Shanghai 200237, Peoples R China;[3]Shanghai Univ Tradit Chinese Med, Putuo Hosp, Dept Clin Oncol, Shanghai, Peoples R China;[4]Shanghai Univ Tradit Chinese Med, Intervent Canc Inst Integrat Med, Shanghai, Peoples R China;[5]Helmholtz Zentrum Geesthacht, Ctr Mat & Coastal Res, Polymer Res Inst, D-21502 Geesthacht, Germany;[6]Helmholtz Zentrum Geesthacht, Ctr Mat & Coastal Res, Inst Mat Reearch, D-21502 Geesthacht, Germany

年份：2017

卷号：78

起止页码：609

外文期刊名：MATERIALS SCIENCE & ENGINEERING C-MATERIALS FOR BIOLOGICAL APPLICATIONS

收录：;EI(收录号：20171703606433);WOS:【SCI-EXPANDED(收录号:WOS:000404944700072)】；

基金：Mrs. Ivonne Ternes is acknowledged for the DSC measurements. Thanks to Shengke Li for his suggestions. We gratefully acknowledge the support of this work by Shanghai Natural Science Foundation (Grant No. 15ZR1409900), the National Natural Science Foundation of China (Grant No. 31200617) and Knowledge Innovation Program of CAS (Grant No. 2013KIP103).

语种：英文

外文关键词：Bufalin; beta-cydodextrin; Inclusion complex; Folic acid; Drug delivery

摘要：Bufalin (BF), a traditional Chinese medicine, exhibited inhibitory activities against a broad spectrum of tumor cells. The present study elaborates that bufalin was successfully encapsulated into the cavity of beta-cyclodextrin (beta-CD), which was determined by Fourier transform infrared spectroscopy (FT-IR), proton nuclear magnetic resonance spectroscopy (H-1 NMR), differential scanning calorimetry (DSC) and scanning electron microscopy (SEM). The best reaction mole ratio of BF/beta-CD was 1:5. The solubilities of bufalin in water and phosphate buffer solution (pH = 7.4) were increased up to 24 and 34 times after encapsulated into the cavity of S-CD respectively. The inclusion efficiency (IE) and drug loading (DL) of bufalin in the inclusion complex were (94.22 +/- 0.85)% and (14.11 +/- 0.20)%, respectively. Then beta-CD conjugated with folic acid (FA) were further prepared and employed to improve the anti-tumor efficacy of inclusion complex. The in vitro dissolution and solubility study showed better values of inclusion complex and FA targeted inclusion complex than that of pure BF. Cytotoxicity experiments by using HCT116 cell line revealed that the antitumor efficiency of bufalin were enhanced more than two folds in the presence of beta-CD and folate conjugated beta-CD (FA-PEI-beta-CD), which demonstrated the potential application of beta-CD (FA-9EI-beta-CD) as delivery vehicles of bufalin for antitumor therapy. (C) 2017 Elsevier B.V. All rights reserved.