AbstractFood bioactive compounds have a beneficial biological effect on human health, fending off cancer, cardiovascular disease, metabolic syndrome, and neurodegenerative disease, among other noncommunicable diseases and neurodegenerative disorders. Secondary metabolites like polyphenols, glucosinolates, carotenoids, vitamins, terpenoids, saponins, and fibers have been linked to these health benefits due to their antioxidant, antiatherogenic, anti‐inflammatory, antimicrobial, cardioprotective, and vasodilator properties. This review comprehensively illustrates the extraction of bioactive compounds in food formulations along plant wastes and provides insight into the efficient delivery systems for health‐promoting compounds. There is an insight into how to choose which bioactive to use, how to extract them in a bioavailable state, and how to include and deliver them. Grapes, garlic, sweet potato leaves, cactus pears, beetroot, amaranth, Picea abies bark waste, olive leaves, and black plum are discussed comprehensively in terms of extraction and health benefits. The novel and emerging technologies are discussed in detail, and a comprehensive review and comparison with conventional methods are presented. The significant health benefits associated with bioactive compounds are also discussed.