The Citrus grandis, commonly known as pomelo, is a widely distributed fruit and is the largest fruit among citrus species in the Rutaceae family. Citrus peels are the primary agro-food byproducts of citrus processing industries, generating significant solid waste, which is reported to be over 15 million tons per year. The peel of Citrus grandis accounts for 30% of the total fruit weight and contains phytochemicals such as aroma-active volatiles, flavonoids, pectins, carotenoids, phenolic acids, polysaccharides, and coumarins. Naringin, also known as naringenin-7-O-glycoside, is a natural flavonoid that is responsible for the bitter taste of Citrus grandis fruit. Naringin is a potential therapeutic agent because of its antibacterial, anti-inflammatory, and antioxidant properties and has various pharmacological applications, such as the treatment of several illnesses, including heart disease, obesity, and diabetes. The recovery of naringin from peels of Citrus grandis is a key step toward the sustainability of agriculture and its use in various industries. Extraction of naringin from citrus peel should be done in a way that is both safe and efficient, without compromising any of its biological properties that support human health. A wide range of methods, including microwave, auto-hydrolysis, Soxhlet, water infusion, maceration, ultrasound, supercritical fluid, and solid microphase extraction, are employed in the extraction of naringin. The most innovative technology available, though, is supercritical carbon dioxide (SC-CO2) extraction, which has many benefits over traditional extraction techniques, including extract quality, environmental sustainability, and enhanced kinetics. This chapter highlights various bioactive compounds and health advantages of naringin and its extraction from Citrus grandis peel using several conventional and nonconventional processes, with a particular emphasis on the supercritical CO2 extraction approach.