Abstract: Bioactive substances are good raw materials for functional food development due to their anti-tumor, anti-inflammatory, antioxidant and hypolipidemic activities, but most of them are easy to decompose in the process of production, processing and storage. To address this problem, food-grade delivery systems have been designed around proteins, polysaccharides and polyphenols, forming complexes that alter the functional and nutritional properties of foods. In this paper, the research progress of conjugation method, characterization and functional properties of binary and ternary food-grade complexes with different functional properties prepared from proteins, polysaccharides, polyphenols are reviewed, the main type of complexes as carriers and its application in bioactive substances transfer system are summarized, and the interaction between delivery system and human gastrointestinal tract are also summarized. The main problems to be paid attention to in preparation and analysis of complex as delivery system are emphasized and its application prospect is forecasted.