The term “nutraceutical” comprises of “nutrients” and “pharmaceuticals.” Nutraceuticals refers to a food substance, or a part of it, which possesses health benefits in terms of therapeutic or preventive effects. By the turn of the twenty-first century, the use of nutraceuticals became increasingly popular among the consumers due to awareness of rising drug costs, lack of efficacy of conventional drugs, and greater incidences of adverse effects. Nutraceuticals play an important role and offer health benefits including the prevention and treatment of diseases. In developing countries like India, a major percentage of the global population is looking at alternative medical therapy and nutraceuticals (including herbals/botanicals) with great expectation. This chapter explains the general introduction of nutraceuticals, their history, overview of the market, and their benefits in human health, focusing on how bio-based delivery systems enhance nutraceutical’s bioavailability.