Arg-Gly-Asp (RGD) Sequence Containing Cyclic Peptide and Its Active Targeting Liposomes

摘要

The present invention relates to the field of pharmaceutics and clinical pharmacy, involving the preparation method and application of a cyclic peptide containing Argnine-Glycine-Aspartate sequence and its active targeting liposomes. The cyclic peptide described here meets the requirement for ligand in that it forms ring by amide linkage with stable sterical structure, it shows low propensity to degrade, and it carries an active hydrosulfide group which is easy to modify carriers. The artificially synthesized peptide, which has a small molecular weight and low propensity to cause immune response, can be used as the ligand to bind with the integrin on the surface of HSC. The active targeting liposome established with the cyclic peptide realized cell-targeted therapy of experimental hepatic fibrosis via receptor-mediated pathway. The invention can target RGD cyclic peptide-labeled interferon-loaded liposomes to the fibrotic liver and its good efficacy in the treatment of hepatic fibrosis has been proven by experiments in rats in vitro and in vivo.