As an essential polyunsaturated fatty acid, linoleic acid (LA) plays an important role in maintaining the integrity of cellular membranes, modulating inflammatory responses, and mediating intracellular signaling. This review explores the structure, properties, and nutritional significance of LA and its bioactive derivatives, with particular attention to sustainable production methods and their potential applications. A comprehensive review of the recent literature was conducted, emphasizing the use of green synthesis techniques, such as enzyme-catalyzed biocatalysis and microbiological transformations, in order to obtain LA-derived nutraceuticals. Analyses were conducted on the key aspects related to food industry applications, regulatory frameworks, and emerging market trends. Through green synthesis strategies, LA derivatives with antioxidant, anti-inflammatory, and antimicrobial properties have been developed. There is potential for these compounds to be incorporated into health-oriented food products. In spite of this, challenges remain regarding their stability and bioavailability. Furthermore, there are inconsistencies in international regulatory standards which prevent these compounds from being widely adopted. The development of functional and sustainable food products based on linoleic acid derivatives obtained using ecological methods offers significant potential. Research is required to optimize production processes, enhance compound stability, and clinically validate health effects. The integration of the market and the safety of consumers will be supported by addressing regulatory harmonization.