<p>Intravenous routes of drug delivery are widely used in clinical practice due to the advantages of fast onset of action and avoidance of first-pass effect. Still, it is difficult to develop poorly water-soluble drugs for intravenous administration. In recent years, the application of nanocrystal technology has become more and more widespread, mainly involving reducing the particle size to the nanoparticle size range and improving its physicochemical properties to enhance the bioavailability of drugs. Intravenous nanocrystals (INCs) can show unique advantages in the vasculature, with their high drug loading capacity, low toxicity, and overcoming low solubility, which makes them a new solution in tumor therapy. In addition, INCs are mainly suspended in aqueous/oil phase media, which makes them easy to inject. Therefore, INCs may serve as a novel strategy to address poor water solubility, low bioavailability, and associated toxicity. This review contains the compositional development of INCs, and preparation methods, and provides some insights into their application in oncology.</p> Graphical Abstract <p></p>