Aprepitant (APT), an antiemetic drug used for chemotherapy-induced nausea and vomiting (CINV), exhibits poor compressibility, solubility, and micromeritic properties. Crystal habit modification was studied using solvent evaporation, conventional antisolvent crystallization (APTAS), cooling crystallization (APTCC), and the advanced sonocrystallization technique (APTSN). Morphological analysis of the sonocrystallized crystals revealed small, platy crystals exhibiting an aspect ratio of 1. 35 ± 0. 04 and a span value of 1. 06. The APTSN showed improved micromeritics as compared to APTAS (1. 59 ± 0. 03) and APTCC (1. 48 ± 0. 04) (antisolvent-crystallized APT and cooling crystallized APT, respectively). All modified crystals exhibited a plate-shaped crystal habit with no agglomeration. The angle of repose, Carr’s index, and Hausner’s ratio exhibit that the APTSN showed improvement in powder properties. Solid-state characterization using differential scanning calorimetry (DSC), Powder X-ray Diffraction Spectroscopy (PXRD), and Thermogravimetric Analysis (TGA) proved no change in polymorph. Contact angle-driven wettability was as follows: APT > APTAS > APTSN > APTCC, and the results were corroborated by X-ray photon spectroscopy (XPS) and intrinsic dissolution profiles. The XPS studies revealed a decrease in the surface polar component of APTSN, resulting in reduced wettability. APTSN showed the highest tensile strength at 20 kg/cm2 among all other crystals. All the modified crystals exhibited a reduced IDR profile, resulting from a reduction in the polar component at the surface.
Pandhare et al. (2026) studied this question.