Synthesis, solid state characterization and antifungal activity of ketoconazole cocrystals

Abstract

Co-crystallization is a promising technique for improving the biopharmaceutical properties of active pharmaceutical ingredients. The objective of present study was to prepare co-crystals to improve physicochemical properties of BCS class II drug, ketoconazole (KTZ). KTZ co-crystals were prepared with various coformers including oxalic acid, fumaric acid and nicotinamide by solvent crystallization method. The prepared co-crystals were evaluated regarding their thermal properties, crystalline nature, appearance, mean particle size, intrinsic dissolution rate and antifungal potential. The prepared co-crystals demonstrated improved solubility and dissolution rate. Moreover, co-crystals showed good antifungal potential against Candida albicans (MCC 1094). The prepared cocrystals were found to be stable over the period of 6 months verified from stability studies. Therefore, the present study showed that co-crystals may be a potential approach for a BCS class II drug, KTZ.