Abstract: Capsicum alkaloids, with various biological activities such as anti-cancer, anti-inflammatory, antibacterial, relieving pain, weight loss, anti-oxidation, protect the gastrointestinal tract, are the material basis and the main biologically active ingredients of capscium. However, the high stimulation, poor solubility, poor stability, liver first pass effect and other problems make its bioavailability low. In this review, recent advances in the mechanism of the versatile bioactivities of capsicum alkaloids and in the development of technologies for enhancing capsicum alkaloids bioavailability such as the use of liposome, microsphere, emulsion, hydroxypropyl -β- cyclodextrin, prodrug self-assembly technology are systematically summarized. It provides theoretical basis and technical support for the application of capsicum alkaloids in the future.