Abstract: Disclosed is a targeted delivery system for a hydrophobic antitumor drug, referring to conjugates of E-selectin polypeptide ligand-polyethylene glycol-antitumor drug connected by different link bridges containing disulfide bonds. The synthesis of the conjugates, antitumor activity evaluation, the particle size and morphology characteristics of nanoparticles self-assembled by the conjugates in an aqueous solution, and the release of the antitumor drug in different conditions are comprised. The conjugates can actively target at vessels of a tumor site by the E-selectin peptide ligand, and can also self-assemble into nanoparticles in an aqueous solution, so as to be passively targeted at the tumor site by EPR effect.

Abstract: Disclosed herein is a preparation method and use of a surface double-modified human serum albumin as a tumor targeting nano drug carrier, wherein the targeting nano drug carrier includes human serum albumin (HSA), polyethylene glycol and E-selectin peptide ligand. The targeting nano drug carrier is formed by coupling the E-selectin peptide ligand and polyethylene glycol to the surface of HSA by thioether linker formed between the sulfhydryl group of E-selectin peptide ligand and activated HSA. The targeting nano drug carrier can encapsulate hydrophobic antitumor drugs and form nanoparticles with certain particle size after treatment, which can not only increase the solubility and stability of the hydrophobic antitumor drugs, but also can actively recognize and bind E-selectin which is highly expressed on activated endothelial cells at tumor site, competitively inhibit the interaction between E-selectin and tumor cells, and thus inhibit the adhesion and migration of tumor cells.

Abstract: Disclosed is a targeted delivery system for a hydrophobic antitumor drug, referring to conjugates of E-selectin polypeptide ligand-polyethylene glycol-antitumor drug connected by different link bridges containing disulfide bonds. The synthesis of the conjugates, antitumor activity evaluation, the particle size and morphology characteristics of nanoparticles self-assembled by the conjugates in an aqueous solution, and the release of the antitumor drug in different conditions are comprised. The conjugates can actively target at vessels of a tumor site by the E-selectin peptide ligand, and can also self-assemble into nanoparticles in an aqueous solution, so as to be passively targeted at the tumor site by EPR effect.