Host-guest inclusion system of artesunate with β-cyclodextrin and its derivatives: Characterization and antitumor activity

被引:15
作者
Xie, Hudie [1 ]
Yang, Bo [1 ]
Wang, Fen [1 ]
Zhao, Yulin [2 ]
机构
[1] Kunming Univ Sci & Technol, Fac Life Sci & Technol, Kunming 650500, Peoples R China
[2] Kunming Univ Sci & Technol, Fac Chem Engn, Kunming 650500, Peoples R China
基金
中国国家自然科学基金;
关键词
Artesunate; beta-Cyclodextrin; Inclusion complex; Solubilization; Thermal stability; DRUG; DIHYDROARTEMISININ; COMPLEXATION; SOLUBILITY; PROGRESS;
D O I
10.1016/j.molstruc.2014.12.087
中图分类号
O64 [物理化学(理论化学)、化学物理学];
学科分类号
070304 ; 081704 ;
摘要
Inclusion complexes between artesunate (ATS) and three cyclodextrins, namely beta-cyclodextrin (beta-CD), hydroxypropyl-beta-cyclodextrin (HP-beta-CD) and sulfobutyl ether-beta-cyclodextrin (SBE-beta-CD), were prepared by a suspension method. The complexes in both liquid and solid were characterized by phase-solubility diagram, nuclear magnetic resonance (NMR), powder X-ray diffraction (XRD) and thermoanalysis. The results suggested that artesunate was partly encapsulated within the cyclodextrin cavity to form a 1:1 stoichiometry host-guest compound. Especially in the SBE-beta-CD complex, displayed the greatest stability constant. Significant enhancement of water solubility and thermal stability of ATS in present of beta-CDs was shown. The calculated IC50 values indicated that the antitumor activities of inclusion complexes were better than that of ATS. Satisfactory aqueous solubility, along with high thermal stability of inclusion complexes will be potentially useful for their application on the formulation design of natural medicine. (C) 2015 Elsevier B.V. All rights reserved.
引用
收藏
页码:90 / 96
页数:7
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