The invention relates to a double-receptor targeting drug delivery system realizing the synergistic effect of phototherapy and chemotherapy, as well as preparation and applications of the double-receptor targeting drug delivery system. The system is a compound containing hyaluronic acid, polylactic acid, polypeptide, and chlorambucil / chlorin e6, wherein the molecular weight of polylactic acid is 8000Da, specifically, the compound comprises the following components in parts by weight: 100-2000 parts of hyaluronic acid, 1500-10000 parts of polylactic acid, 21-450 parts of N,N'-dicyclohexylcarbodiimide, 12-240 parts of N-hydroxy succinimide, 1-30 parts of polypeptide, 20-400 parts of 1-(3-(Dimethylaminopropyl)-3-ethylcarbodiimide, 100-1000 parts of chlorambucil, and 50-600 parts of chlorin e6. The double-receptor targeting drug delivery system has the beneficial effects that (1) the synergistic effect of phototherapy and chemotherapy is realized; (2) the multiple targeting properties are realized; (3) the good blood stability is realized; (4) the system has small toxicity and high safety.