Amorphous Mixtures of Albendazole with Carboxylic Acids By Cogrinding Technique: Solid State Characterizations and In Vitro Efficacy Study

Abstract

Purpose: To improve the physicochemical properties of poorly aqueous soluble albendazole by formulating its amorphous mixtures by different techniques. Methods: cogrind amorphous mixtures were successfully formulated with different carboxylic acids like citric acid, benzoic acid, salicylic acid and succinic acid in equimolar ratios by grinding and solvent drop grinding technique without formation of cocrystals. The physicochemical properties of pure albendazole and corresponding cogrind mixtures were assessed in terms of melting point, drug content, saturation solubility and dissolution studies, Infrared spectroscopy (IR), X-ray powder diffractometry (XRPD) and Differential scanning colorimetry (DSC). Results: The results indicated a marked improvement in flow properties and saturation solubility of amorphous mixtures. Further, in case of dissolution experiments, the amorphous mixtures showed a significant enhancement in the dissolution profiles as compared to pure albendazole. In-vitro anthelmintic as well as in In vitro antifungal activity was also improved. It could be concluded that better improvement of physicochemical properties of albendazole could be possible with salicylic acid and citric acid using cogrinding technique. Conclusion: It is possible to formulate amorphous mixtures of albendazole with different carboxylic acids without forming cocrystals still strong agreement to form cocrystals by solubility parameters, structural features. D.O.I. - 10.25258/ijddt.9.4.1