Ternary conjugate of antitumor drug, and synthesis and application

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. The results show that the conjugates have significant antitumor activity but are less toxic to normal cells, can inhibit the adhesion between tumor cells and vascular endothelial cells, have the potential of anti-tumor metastasis, and have a broad prospect in development and application of antitumor drugs.