There is compelling evidence that drug molecules isolated from natural sources are hindered by low
systemic bioavailability, poor absorption, and rapid elimination from the human body. Novel approaches are
urgently needed that could enhance the retention time as well as the efficacy of natural products in the body.
Among the various adopted approaches to meet this ever-increasing demand, nanoformulations show the most
fascinating way of improving the bioavailability of dietary phytochemicals through modifying their pharmacokinetics
and pharmacodynamics. Curcumin, a yellowish pigment isolated from dried ground rhizomes of turmeric,
exhibits tremendous pharmacological effects, including anticancer activities. Several in vitro and in vivo
studies have shown that curcumin mediates anticancer effects through the modulation (upregulation and/or
downregulations) of several intracellular signaling pathways both at protein and mRNA levels. Scientists have
introduced multiple modern techniques and novel dosage forms for enhancing the delivery, bioavailability, and
efficacy of curcumin in the treatment of various malignancies. These novel dosage forms include nanoparticles,
liposomes, micelles, phospholipids, and curcumin-encapsulated polymer nanoparticles. Nanocurcumin has
shown improved anticancer effects compared to conventional curcumin formulations. This review discusses the
underlying molecular mechanism of various nanoformulations of curcumin for the treatment of different cancers.
We hope that this study will make a road map for preclinical and clinical investigations of cancer and recommend
nano curcumin as a drug of choice for cancer therapy.