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Nutraceuticals are super-nutrients isolated and purified from foods (fruits, vegetables, legumes, spices, etc.), which generally promote health besides their authentic nutritional values and are, therefore, used to manage various diseases/disorders. Mainly, they are categorized by their source of origin, therapeutic benefits, and chemical constitution. The prior art also suggests their long history of health benefits; however, the full potential of nutraceuticals, such as curcumin, resveratrol, quercetin, and carotenoids, has still been unexplored due to their poor physiochemical properties, i.e., low aqueous solubility, poor diffusion, low gastrointestinal stability poor permeability, and low bioavailability. To enhance the efficacy of nutraceuticals, drug-delivery systems using nanotechnology (liposome, nanospheres, nanoemulsion, micelle, and nanocrystals) represent an innovative way to effectively increase their efficacy, oral bioavailability, and alleviate other barriers. Besides improving the physicochemical properties and therapeutic efficacy of nutraceuticals, developed nanoformulations also provide a targeted approach-based delivery. This chapter will give brief details of the full therapeutic potential gained with the utilization of nanotechnology in nutraceuticals.