Resveratrol, a polyphenolic compound, has gained attention for its therapeutic potential, particularly in cancer treatment. However, its anticancer efficacy is limited by low water solubility, dose-limiting toxicity, low bioavailability, and rapid hepatic metabolism. To overcome these challenges, various nanoparticles, including organic and inorganic nanoparticles, liposomes, polymeric nanoparticles, dendrimers, solid lipid nanoparticles, gold nanoparticles, zinc oxide nanoparticles, zeolitic imidazolate frameworks, carbon nanotubes, and mesoporous nanoparticles, have been employed to enhance resveratrol's water solubility, bioavailability, and efficacy against different types of cancer. Resveratrol-loaded nanoparticle or resveratrol-conjugated nanoparticle administration exhibits superior anticancer potency compared to free resveratrol. This review highlights the latest developments in nanoparticle-based delivery systems for resveratrol, focusing on the potential to overcome limitations associated with the compound's bioavailability and therapeutic effectiveness. The review covers the structure and physical properties of resveratrol, its metabolism, mechanism of action against cancer, and the application of nanoparticles to improve the therapeutic potential of resveratrol for cancer treatment. Various strategies, such as triggered drug release and stimuli-responsive approaches, have been used to enhance the therapeutic efficacy and precise control of resveratrol. The review also discusses the use of organic nanoparticles (liposomes, polymeric nanoparticles), inorganic nanoparticles (gold nanoparticles, zinc oxide nanoparticles, zeolitic imidazolate frameworks, mesoporous silica nanoparticles), and carbon nanotubes in delivering resveratrol for cancer therapy.Resveratrol, a polyphenolic compound, has gained attention for its therapeutic potential, particularly in cancer treatment. However, its anticancer efficacy is limited by low water solubility, dose-limiting toxicity, low bioavailability, and rapid hepatic metabolism. To overcome these challenges, various nanoparticles, including organic and inorganic nanoparticles, liposomes, polymeric nanoparticles, dendrimers, solid lipid nanoparticles, gold nanoparticles, zinc oxide nanoparticles, zeolitic imidazolate frameworks, carbon nanotubes, and mesoporous nanoparticles, have been employed to enhance resveratrol's water solubility, bioavailability, and efficacy against different types of cancer. Resveratrol-loaded nanoparticle or resveratrol-conjugated nanoparticle administration exhibits superior anticancer potency compared to free resveratrol. This review highlights the latest developments in nanoparticle-based delivery systems for resveratrol, focusing on the potential to overcome limitations associated with the compound's bioavailability and therapeutic effectiveness. The review covers the structure and physical properties of resveratrol, its metabolism, mechanism of action against cancer, and the application of nanoparticles to improve the therapeutic potential of resveratrol for cancer treatment. Various strategies, such as triggered drug release and stimuli-responsive approaches, have been used to enhance the therapeutic efficacy and precise control of resveratrol. The review also discusses the use of organic nanoparticles (liposomes, polymeric nanoparticles), inorganic nanoparticles (gold nanoparticles, zinc oxide nanoparticles, zeolitic imidazolate frameworks, mesoporous silica nanoparticles), and carbon nanotubes in delivering resveratrol for cancer therapy.