Screening of coformers for quercetin cocrystals through mechanochemical methods

• Autor(a) principal: De Souza, Fayene Zeferino Ribeiro [UNESP]
• Data de Publicação: 2022
• Outros Autores: De Almeida, Amanda Cosmo [UNESP], Ferreira, Patrícia Osorio [UNESP], Fernandes, Richard Perosa [UNESP], Caires, Flávio Junior [UNESP]
• Tipo de documento: Artigo
• Idioma: eng
• Título da fonte: Repositório Institucional da UNESP
• Texto Completo: http://dx.doi.org/10.26850/1678-4618eqj.v47.1.2022.p64-75; http://hdl.handle.net/11449/223320
• topic: Cocrystallization; Flavonoid; Mechanochemistry; Nutraceutical; Thermal analysis

Quercetin (QUE) is a nutraceutical compound that exhibits pharmacological properties such as antioxidant, cardioprotective, anti-ulcer, and anti-inflammatory effects. Although QUE is well-known for its benefits, its efficacy is limited due to low solubility. Thus, cocrystallization acts as an interesting approach to improve the solubility - among other properties - of this compound. In this work, cocrystallization screening was applied through neat grinding (NG) and liquid-assisted grinding (LAG), in which QUE and four cocrystal formers (benzamide, picolinamide, isonicotinamide, and pyrazinoic acid) were tested. The precursors and QUE-coformer systems were characterized using thermoanalytical techniques (TG-DTA), X-ray powder diffraction (XRPD), and Fourier transform infrared (FTIR) spectroscopy. The results showed the formation of QUE cocrystals with picolinamide and isonicotinamide coformers in a 1:1 stoichiometric ratio. Furthermore, although coformers are isomers, spectroscopic and thermal data suggest that the supramolecular synthons involved in cocrystallization are different.