The objectives of this study were to develop rivaroxaban (RXB) nanocrystals by combination of wet ball milling and high-pressure homogenization, and to increase the solubility and dissolution rate of RXB. A new nanocrystal formulation was developed, and used to reduce particle size of RXB which is a Biopharmaceutics Classification System Class 2 drug. Particle size of RXB in nanosuspension formulation (551 nm) and nanocrystal formulation (1018 nm) was reduced significantly (p < 0.05) as compared to the particle size of RXB bulk. Dissolution rate of RXB nanocrystals (85% within 15 min) was much faster than that of RXB bulk (12% within 45 min). Also, permeability across Caco-2 cells was enhanced for RXB nanocrystals (10.18 x 10(-5) cm/s) in comparison to the RXB bulk (7.25 x 10(-5) cm/s; p < 0.05). Based on the results, it can be concluded that nanocrystal technology can be employed to improve the solubility and dissolution rate of RXB (hence permeability) with preserving its chemical structure.