Saturation Solubility and Dissolution Property Improvement of Albendazole by Salt Formation Approach

Albendazole belongs to BCS-II category whose systemic and local anthelmintic effectiveness is restricted due to its low water solubility–related dissolution properties. The present investigation was aimed to prepare salts of albendazole using various weak organic acids such as succinic acid, tartaric acid, benzoic acid, and citric acid as counterions. The solvent evaporation was used to prepare the salts. The results of differential scanning calorimetry, Fourier-transform infrared spectroscopy, and powder X-ray diffraction suggested the formation of a new crystalline solid phase due to reaction between ABZ and organic acids. The results of 1H NMR studies indicted the participation of protons attached to nitrogen atoms (N–-H +) in the salt formation process. A significantly higher amount of drug release was observed in in vitro dissolution study from all the prepared salts compared to a pure drug in 0.1 N HCl. Contrary to that, no significant improvement was observed in in vitro dissolution study performed in 6.8 pH phosphate buffer. The prepared novel salts successfully improved the saturation solubility and dissolution properties of albendazole.