The promise of artesunate’s (ART) role in anticancer properties steers a focus on drug repurposing. Potential nanocargo heterostructures, with each component having a specific role, are required for effective drug delivery. Here, we have developed a nanoformulation based on nanodiamonds studded with iron oxide that exhibits exceptional biocompatibility and effective cellular delivery of ART. The current drug delivery formulation has proven improved efficiency of the drug in generating higher reactive oxygen species (ROS), resulting in DNA damage and subsequent cellular apoptosis.