Characterization and evaluation of synthetic riluzole with β-cyclodextrin and 2,6-di-O-methyl-β-cyclodextrin inclusion complexes

Abstract

β-Cyclodextrin (β-CD) and 2,6-di-O-methyl-β-cyclodextrin (DM-β-CD) inclusion complexes with riluzole (RLZ) were prepared to improve water solubility and broaden potential pharmaceutical applications. CDs/RLZ inclusion complexes were confirmed via phase solubility studies, FT-IR spectroscopy, PXRD, DSC, 1H NMR, and SEM. Phase solubility studies indicated that β-CD and DM-β-CD can form 1:1 inclusion complexes with RLZ, and the stability constants were 663.17 and 1609.07M−1, respectively. Water solubility and dissolution rate of RLZ were significantly improved in complex forms, implying that the inclusion complexes may develop pharmaceutical applications. Preliminary in vitro cytotoxicity assay also showed that RLZ hepatotoxicity was not increased in the inclusion complexes.