Dietary polyphenols, primarily categorized into flavonoids (flavanols, flavones, flavan-3-ols, anthocyanidins, flavanones, and isoflavones) and nonflavonoids (stilbenes and phenolic acids) are reported to have health-promoting effects, such as antioxidant, anti-inflammatory, antitumor, antibacterial, antiviral, and cardioprotective properties. However, their applications in functional food and medications are limited due to their low bioavailability and insufficient systemic delivery. Nano-delivery system conveyances frameworks astoundingly influence the take-up properties of the stacked atoms because the molecule small shape, size, and surface properties of the nanoparticles apply a vital role in the improvement of the systemic delivery of polyphenols This includes nano-emulsion, nano-encapsulation, polymer nanoparticles (NPs), nano-liposomes, solid liquid nanoparticles, cyclodextrins, and polyphenol-loaded hydrogels. Nano-technology is a rapidly developing area that guarantees the improvement of materials with novel measurements, new properties, and more extensive scope for utilization. This review reports the different therapeutic applications of dietary polyphenols, their biological activities, and different nano-delivery systems successfully developed for overcoming the delivery challenges. These applications also seek to improve their bioavailability, reduce toxicity, and enhance dietary polyphenol uptake across the gastrointestinal tract.