Elucidating of Fluconazole Cocrystallization With a Cutting-Edge Nutraceutical Coformer for Enhanced Formulation Strategies

This current research reports the synthesis and characterization of a cocrystal of Fluconazole (FLU), a widely used antifungal drug, with a nutraceutical coformer (NCF) that has potential health benefits as well as improving its solubility and antifungal activity.

The co-crystal was obtained by solvent evaporation in a stoichiometric ratio using three natural coformers: Ferulic acid, caffeic acid, and glycerine, and characterized by various analytical techniques, including Powder x-ray diffraction (PXRD), Differential scanning calorimetry (DSC), and Fourier transform infrared (FTIR) spectroscopy.

The cocrystals showed lower heats of fusion (ΔH) compared to pure Fluconazole, indicating the possibility of increased entropy and solubility for all cocrystals. Using the solvent evaporation method with ferulic acid, caffeic acid, and glycine showed significant enhancement of solubility, ranging from 1.06-fold to 4.80-fold, depending on the co-former and different media used.

The zone of inhibition assay showed that cocrystals of Fluconazole with nutraceuticals (FLU+CAF, FLU+GLY, and FLU+FER) exhibited higher zones of inhibition compared to pure Fluconazole and DMSO control. Solubility and dissolution studies revealed that cocrystals of Fluconazole with nutraceutical coformers could be an effective approach to enhancing the solubility and antifungal activity of Fluconazole.