The invention belongs to the field of pharmacy, and particularly relates to whole process targeting polypeptide molecule targeting a brain capillary vessel endothelial cell, a tumor neovascular endothelial cell, a tumor mimic blood vessel, a tumor cell and a tumor stem cell, and a stable optimized polypeptide molecule thereof, and an application of modified compound and a drug delivery system in the diagnosis and treatment of tumors. The invention relates to the application of the whole process targeting polypeptide WVAP and a WVAP modified drug and a polymer carrier material, and the application thereof in the construction of tumor imaging and a targeted therapy delivery system, the results show that WVAP can cross a blood-brain barrier, can target tumor neovascularization and cross blood-tumor barrier, and target tumor mimicry blood vessels, the tumor cells and the cancer stem cells; the nano drug delivery system constructed by the WVAP modified polymer carrier material can effectively deliver the encapsulated drug into the brain, targets the tumor tissue, and significantly improves the antitumor efficacy.