A New Ferulic Acid–Nicotinamide Cocrystal With Improved Solubility and Dissolution Performance

• Published in: Journal of pharmaceutical sciences 2020-03, Vol.109 (3), p.1330-1337
• Main Authors: Chaves Júnior, José Venâncio, dos Santos, Jonh Anderson Borges, Lins, Taynara Batista, de Araújo Batista, Rayanne Sales, de Lima Neto, Severino Antônio, de Santana Oliveira, Artur, Nogueira, Fernando Henrique Andrade, Gomes, Ana Paula Barreto, de Sousa, Damião Pergentino, de Souza, Fábio Santos, Aragão, Cícero Flávio Soares
• Format: Article
• Language: English
• Subjects: cocrystal; dissolution profile; ferulic acid; solubility
• ISSN: 0022-3549; 1520-6017
• DOI: 10.1016/j.xphs.2019.12.002

Among the various strategies for increasing aqueous solubility of pharmaceutical substances, cocrystals have been emerging as a promising alternative. The ferulic acid (FEA) is a molecule with limited aqueous solubility, but with an interesting pharmacological activity, highlighting its antitumor potential. This study presents the characterization and physicochemical properties of a new cocrystal based on FEA and nicotinamide (NIC). The FEA-NIC cocrystal was obtained by solvent evaporation technique and physicochemically characterized by differential scanning calorimetry, powder X-ray diffraction, Fourier transform infrared spectroscopy, solid-state nuclear magnetic resonance and scanning electron microscopy. The content determination and dissolution profile in different media were analyzed by high-performance liquid chromatography. The results obtained with the characterization techniques indicated the obtainment of an anhydrous cocrystal of FEA and NIC at a 1:1 molar ratio. The method was reproducible and obtained a high yield, of approximately 99%. In addition, a 70% increase in the FEA solubility in the cocrystal and a better dissolution performance than the physical mixture in pH 6.8 were achieved.