Rice bran oil (RBO) is an emerging cooking oil, known for its high level of bioactive compounds that play an important role in the management of different diseases. The RBO extraction methods directly impact the level of bioactives in RBO, resulting in alterations of therapeutic activities. The green extraction processes, including supercritical CO2, subcritical CO2 Soxhlet, subcritical liquefied dimethyl ether, enzyme-assisted aqueous, microwave-assisted, and ultrasound-assisted extraction, were applied to obtain RBO from rice bran. RBO exhibited potential health benefits via upregulation and downregulation of several types of molecular pathways and gene expression. In addition, the unique physicochemical properties of RBO enable its use in cosmetics, novel drug delivery systems, biosurfactant applications, and the development of moisturizing, detoxifying, and anti-aging products. Several novel formulations, such as nanoemulsions, emulgels, self-nanoemulsifying systems, and oleogels, were prepared in which RBO significantly improves solubility, bioavailability, and intestinal absorption of lipophilic drugs. Animal feed, biofuel, and food products are other applications of RBO. Considering all these aspects of RBO, this review was designed to explore the in-depth RBO extraction phenomenon, the molecular mechanism exerted by functional agents in RBO, and the emerging applications in diverse fields.