Preparation and physicochemical characteristics of the complex of edaravone with hydroxypropyl-β-cyclodextrin

The aim of this study was to prepare an inclusion complex of edaravone, a novel free radical scavenger drug, with hydroxypropyl-beta-cyclodextrin (HP-beta-CD) to improve its apparent solubility, dissolution rate and stability. The solubility of edaravone was evaluated by phase solubility method and the profile displayed a typical A(L)-type, indicating the formation of 1:1 stoichiometric inclusion complex. The inclusion complex was prepared by freeze-drying method and characterized by DTA, XRD and NMR. These results suggested that edaravone could form inclusion complex with HP-beta-CD and was deeply included in the cavity of HP-beta-CD. Additionally, the dissolution rate and stability of the inclusion complex were greatly improved compared with that of edaravone. These results strongly showed that the use of HP-beta-CD could be a promising approach to improve the physicochemical characteristics of edaravone. (C) 2010 Elsevier Ltd. All rights reserved.