Inclusion of lycorine with natural cyclodextrins (α-, β- and γ-CD): Experimental and in vitro evaluation

• Published in: Journal of molecular structure 2017-02, Vol.1130, p.669-676
• Main Authors: Liu, Dan-Dan, Guo, Ya-Fei, Zhang, Jian-Qiang, Yang, Zhi-Kuan, Li, Xiang, Yang, Bo, Yang, Rui
• Format: Article
• Language: English
• Subjects: Anticancer; Binding behavior; Cyclodextrin; Lycorine
• ISSN: 0022-2860; 1872-8014
• DOI: 10.1016/j.molstruc.2016.11.018

The primary goal of this research was to investigate the effect of spatial compatibility in the inclusion complex formation of cyclodextrins with different cavity size on physicochemical and anticancer properties. For this purpose, the binding behaviors of the complex formations of α-, β- and γ-cyclodextrins with lycorine were observed by the use of UV, MS, XRD, DSC, TG, 1H, and 2D NMR spectroscopy and elemental analysis. The results displayed that the binding behavior was contrary to the size of the CDs, and the value of binding constant of lycorine/γ-CD was the smallest, while the value of binding constant of lycorine/α-CD was the greatest. In vitro study demonstrated that the lycorine-α-CD and lycorine-β-CD are valuable approaches to enhance lycorine bioavailability. The results deduced that using CDs with moderate cavities (such as α-CD or β-CD) as a cyclodextrin-based delivery system to form the lycorine-type inclusion complex could be more applicable, and further helps to improve the properties of lycorine-type therapeutic agent. •Inclusion complexes of lycorine with three natural cyclodextrins were synthesized.•The binding behavior had determined by experimental.•The trend of binding ability was as follows: α-CD>β-CD>γ-CD.•The inclusion complexes still maintain good antitumor activities in vitro.•α-CD or β-CD is more applicable to form the lycorin-type inclusion complex.