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Nanomedicine has revolutionized the pharmaceutical and biological sciences industry by providing new frontiers and targets on the diagnosis and treatment of diseases. One promising development is the integration of natural products with nanoformulations, is emerging as a novel strategy in antitumor therapy. This combination has opened up new avenues for primary intervention and treatment due to targeted delivery of therapeutic agents against cancer. Researchers are trying to enhance and establish the safety and efficacy of naturally occurring bioactive compounds characterised by their anticancer potential. Polyphenols and other phytochemicals, along with functional foods, have high potency in circumventing tumors by the effective inhibition of the expansion of cancerous cells and induction of apoptosis. Incorporation of such natural products natural products through nanotechnology is therefore meant to enhance therapeutic efficacy with an improved safety profile. The aim will be to formulate these bioactive compounds as nanoformulations to achieve higher tumor site concentration, which would result in maximum anticancer effects and perhaps reduce the possible side effects associated with conventional therapies. This calls for collaboration among researchers and clinicians in establishing evidence-based guidelines and standardized protocols that ensure safety and efficacy in the use of such therapies.