<p>Nanocrystal formulation is a powerful approach that escalates the dissolution rate of drugs with poor water solubility. By enhancing their saturation solubility, this method considerably improves the bioavailability of these drugs. In the past ten years, numerous anticancer drug nanocrystals have been examined through preclinical studies and clinical trials. The review provides a concise overview of the different approaches employed to fabricate and characterize these nanocrystals. The different fabrication methods such as antisolvent precipitation, supercritical fluid technology, and microfluidic techniques are discussed in the review. Additionally, this review also focuses on the application of nanocrystal formulations to improve the saturation solubility of anticancer drugs, which is linked to enhanced bioavailability and increased anticancer effectiveness. This review aims to provide an all-inclusive understanding of nanocrystal formulation as an effective strategy for escalating pharmacokinetics and pharmacodynamics of anticancer drugs.</p> Graphical Abstract <p></p>