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This invention discloses a vitamin A-functionalized polyphenol-phospholipid complex, its preparation method, and its applications, belonging to the field of pharmaceutical formulation and nanodelivery technology. The phospholipid complex comprises a polyphenol drug, a phospholipid material, and a vitamin A phospholipid ligand. The vitamin A phospholipid ligand is formed by vitamin A or its derivatives and a phospholipid derivative containing amino or other reactive groups. The phospholipid complex forms a phospholipid composite structure through non-covalent interactions between the polyphenol drug and the phospholipid material, and the vitamin A phospholipid ligand is inserted into or assembled into the surface or interior of the phospholipid composite structure. Animal experiments show that this phospholipid complex can reduce serum transaminase levels and alleviate the degree of liver fibrosis, and has good blood compatibility and tissue safety. This invention provides an industrially achievable targeted nano-formulation solution for early intervention in liver fibrosis, with promising application prospects.