Solid-state characterization of ibuprofen-isonicotinamide cocrystals prepared by electrospraying and solvent evaporation

Electrospraying (ELS) was used to prepare micronized ibuprofen-isonicotinamide cocrystal (IBU-INA-ELS) and its properties were compared with the solvent evaporated cocrystal (IBU-INA-SE). Solid-state characterization of crystalline phase, production yield, particle size, powder flow, wettability, solution mediated phase transformation (SMPT), and dissolution rate were measured. The ELS produced phase pure particles of IBU-INA with a size of 1.46 μm and yield of 72.3%. This cocrystal improved the intrinsic dissolution rate and powder dissolution rate of IBU by 3.6- and 1.7-fold, respectively. Our experiments showed that the dissolution of IBU-INA was affected by particle size, solubility, SMPT and wettability. ELS produced micronized cocrystals for improving dissolution of ibuprofen with a high yield in a single step and mild conditions. The intestinal absorption of ibuprofen is limited by low dissolution rate in the gastrointestinal fluids. This drug needs applied in an appropriate method to enhance its dissolution. One way to improve dissolution of ibuprofen is preparing micronized cocrystal of this drug and a water soluble compound, isonicotinamide. In this study, we prepared and characterized micronized particles of ibuprofen-isonicotinamide cocrystal by electrospraying, a single step and continuous method without need for any added material. Our experiments showed that the prepared micronized cocrystal could improve the dissolution of ibuprofen but the cocrystal is rapidly precipitated as ibuprofen crystals in contact with dissolution medium. This precipitation hampered the expected increase in dissolution. Therefore, solution mediated phase transformation should be considered in formulating micronized cocrystals. Micronized ibuprofen-isonicotinamide cocrystals with improved dissolution prepared by electrospraying. However, phase conversion strongly affected its dissolution. #Cocrystal #Dissolution #Ibuprofen