Solid inclusion inclusion complexes of oleanolic acid with amino -appended beta-cyclodextrins (ACDs).: Preparation, characterization, water solubility. and anticancer activity
机构：[1]Faculty of Life Science and Technology, Kunming University of Science and Technology, Kunming 650500, China[2]Faculty of Medicine, Kunming University of Science and Technology, Kunming 650500, China[3]Research Centre for Pharmaceutical Care and Quality Management, First People's Hospital of Yunnan Province, Kunming 650500, China云南省第一人民医院[4]Current address: Department of Pharmacy, School of Ocean, Hainan University, Haikou 570228, China.
Oleanolic acid (OA) is a pentacydic triterpenoid acid of natural abundance in plants which possesses important biological activities. However, its medicinal applications were severely impeded by the poor water solubility and resultan low bioavailability and potency. In this work, studies on solid inclusion complexes of OA with a series of amino-appended beta-cyclodextrins (ACDs) were conducted in order to address this issue. These complexes were prepared by suspension method and were well characterized by NMR, SEM, XRD, TG, DSC and Zeta potential measurement. The 2:1 inclusion mode of ACDs/OA complexes was elucidated by elaborate 2D NMR (ROESY). Besides, water solubility of OA was dramatically promoted by inclusion complexation with ACDs. Moreover, in vitro anticancer activities of OA against human cancer cell lines HepG2, HT29 and HCT116 were significantly enhanced after formation of inclusion complexes, while the apoptotic response results indicated their induction of apoptosis of cancer cells. This could provide a novel approach to development of novel pharmaceutical formulations of OA. (C) 2016 Elsevier B.V. All rights reserved.
基金：
This work was financially supported by National Natural Science
Foundation of China (NNSFC, Nos. 21362016 & 81260501) and the
Ministry of Education of P.R. China (No. 201410674009).
