ENHANCEMENT OF THE PHYSICOCHEMICAL PROPERTIES OF POORLY SOLUBLE CABAZITAXEL BY CO-CRYSTALLIZATION TECHNIQUE - IN VITRO STUDIES

Abstract

To overcome the poor solubility and low bioavailability of Cabazitaxel, co-crystallization technique was attempted. Cabazitaxel co-crystals were prepared with selected co-former citric acid by liquid assisted-grinding method. Characterization was carried out through Fourier Transform infra-red spectroscopy, differential scanning colorimetry and X-ray diffraction. The Fourier-transform infrared spectroscopy results showed that a hydrogen bond was formed between Cabazitaxel and citric acid to yield a co-crystal. Melting point determination and solubility study was carried out to confirm the changes occurred in free drug after co-crystallization with the co-former. The prepared co-crystals were further transformed into immediate release tablets with Croscarmellose sodium as superdisintegrant and menthol as subliming agent.  Micrometric properties, pre-compression and post-compression properties were evaluated. Full factorial CCD design was used to optimize the formulation parameters. The optimized batch has shown promising results as per desirability. The optimized batch was kept under stressed conditions and found stable.