Investigation of inclusion complex of Epothilone A with cyclodextrins

The inclusion complexation of Epothilone A with native cyclodextrin (beta- or gamma-CD) and its derivative hydroxypropyl-beta-cyclodextrin (HP beta CD) were prepared. Their behavior, characterization, and binding ability were investigated in both solution and the solid state by means of UV-vis, NMR, XRD, DSC and SEM. The results show that the water solubility and solution stability obviously increased in the inclusion complex with cyclodextrins. Meanwhile, the inclusion complexes still retained anticancer activity against A549 and MCF-7 cells, similar to free Epothilone A. This satisfactory water solubility, high solution stability, and high anticancer activity of the Epothilone A/CD complexes will be potentially useful as an anticancer therapy. (C) 2013 Elsevier Ltd. All rights reserved.