<p>Ellipticine is a naturally occurring alkaloid that is derived from the plants of <i>Apocynaceae</i> family and has gained a lot of attention for its promising anticancer properties. Its therapeutic activity is linked with many mechanisms, like oxidative activation, DNA intercalation and inhibition of the topoisomerase II. Despite this potential, the clinical application of ellipticine has been limited because of its systemic toxicity, poor water solubility and the absence of targeted delivery methods. In order to address these issues, researchers have come up with nanoformulation strategies such as liposomes, nanoparticles and micelles. These systems can improve ellipticine’s solubility, stability and also minimize unwanted side effects by directing the drug straight to the tumor cells. Many studies have reported that ellipticine-loaded nanocarriers show higher cytotoxic effects against a range of cancer cell lines and may even help in overcoming the drug resistance that is seen in many other therapies. With the ongoing advancements, these nanodelivery methods are promising for improving cancer treatment outcomes. This review examines the progress, challenges and the future aspects of the ellipticine nanoformulation.</p> Graphical Abstract <p></p>