Curcumin-nicotinamide cocrystallization with supercritical solvent (CSS): Synthesis, characterization and in vivo antinociceptive and anti-inflammatory activities

Abstract Curcumin is a bioactive polyphenol, which presents several medicinal benefits such as antinociceptive, anti-inflammatory, anti-carcinogenic, antimalarial, and antioxidant activity. Despite the benefits, the main barrier in curcumin use by pharmaceutical industry is its low solubility in water medium and hence low bioavailability. The cocrystallization process is characterized by the incidence of molecular interactions between the active pharmaceutical ingredient and coformer that enables improvements in physicochemical properties such as solubility and bioavailability. The main objective of this work is to produce a curcumin-nicotinamide cocrystal by Cocrystallization with Supercritical Solvent (CSS) technique in order to increase curcumin water dissolution rate as well as antinociceptive/anti-inflammatory activities. Curcumin-nicotinamide cocrystal dissolution rate were about 2 times greater than pure curcumin in water medium. The cocrystallization process increased curcumin antinociceptive/anti-inflammatory potency probably due to alterations in its bioavailability. These results open new possibilities of use for curcumin cocrystals in pharmaceutical industries.