Nanotechnology-based drug delivery systems have the potential to enhance the efficacy of poorly soluble systemic drugs. Curcumin, a yellow pigment isolated from turmeric, possesses a wide range of pharmacological activities, including anticancer effects. The anticancer potential of curcumin is mediated through the inhibition and modulation of several intracellular signaling pathways, as confirmed in various in vitro and in vivo cancer studies. However, clinical application of dietary curcumin for the treatment of cancer and other chronic diseases have been hindered by poor bioavailability, due to low systemic solubility as well as rapid metabolism and elimination from the body. Different techniques for sustained and efficient curcumin delivery, including nanoparticles, liposomes, micelles, phospholipids, and curcumin-encapsulated polymer nanoparticles are the focus of this study. Previous studies have shown that nanocurcumin has improved anticancer effects as compared to normal curcumin formulations. Among nanoformulations, few composite nanosystems have the simultaneous properties of therapeutic activity and multifunctional nanoparticles as enhanced image contrast agents. We also address the challenges to the development of nanocurcumin delivery platforms by enhancing a steady aqueous dispersion state. Further studies are needed using preclinical and clinical cancer models to recommend nanocurcumin as a drug of choice for cancer therapy.