Preparation, characterization and in vivo evaluation of pharmacological activity of different crystal forms of ibuprofen

Abstract

Different polymorphic forms can affect the performance of the drug product. In addition, isomorphic crys tals show different chemical and physical properties due to the changes in the crystal habit. However, it is unclear whether the crystal habit results in different pharmacological activity. The aim of this study was to investigate whether the pharmacological effect of ibuprofen could be affected due to the variety of the crystal habit. Solvent change technique and conventional fusion method were carried out to modify the characteristics of ibuprofen. The physicochemical properties of each were investigated using powder X-ray diffraction (PXRD), Fourier transform infrared (FT-IR) spectroscopy and differential scanning calorimetry (DSC) techniques. Results of scanning electron microscopy (SEM) analysis revealed differences in the surface characteristics of the crystals obtained. Further study revealed that the samples crystallized exhibited the remarkable variation on the dissolution profiles in different dissolution medium. Moreover, in vivo antinociceptive and anti-inflammatory findings demonstrated that the crystal habit modifications resulted in the different therapeutic efficacy. Taken together, these results indicate that the modification of the crystal habit had a great influence on the in vivo pharmacological activity of ibuprofen crystals.