EVALUATION OF THE FORMATION OF FERULIC ACID COCRYSTALS WITH DIFFERENT COFORMERS
cocrystal, ferulic acid, solubility, dissolution profile.
Co-crystals are crystalline structures generated from the union of two or more substances, where they have been shown to improve technological and physico-chemical parameters, for example aqueous solubility, which represents a limiting factor in the absorption of drugs. A molecule that is being studied for its antioxidant potential is ferulic acid (FEA), highlighting its antitumor results, however the low aqueous solubility of this molecule appears as an obstacle to its clinical study. The objective of this work is to develop and characterize physically FEA cocrystals with improved aqueous solubility. The cocrystals were prepared by rotaevaporation under reduced pression technique, using ethanol as the solvent. Initially, eight coformers were screened by differential scanning calorimetry (DSC), x-ray diffraction (XRD) and Fourier transform infrared spectroscopy (FTIR). The FEA and nicotinamide cocrystal (FEA: NIC) presented the best aqueous solubility and the latter studies of development and validation of high and ultra high performance liquid chromatography methodologies, experimental design, thermogravimetry (TG), hydrogen resonance magnetic (¹H-NMR) and dissolution profile were carried out. Good reproducibility was observed in the cocrystallization process of FEA:NIC, and in the experimental design the formation occurred only in the 1: 1 molar ratio. The TG showed little physical interaction, the ¹H-NMR confirmed that there were no chemical interactions between the molecules and the cocrystal presented a better dissolution profile than the isolated raw materials. Knowing the importance of increasing the bioavailability of molecules of low aqueous solubility, AFE:NIC is a viable alternative for further study.