F3-PEPTIDE TARGETED LIPID-BASED NANOPARTICLES USEFUL FOR THE TREATMENT OF ANGIOGENESIS-DEPENDENT DISEASES

摘要

The present invention relates to F3 -peptide targeted lipid-based nanoparticles, adequate to encapsulate and delivery- one or more nucleic acids, comprising; a) one or more nucleic acids; b) one or more cationic lipids; c) one or more non- cationic lipids; d) one or more poly (ethylene glycol) - derivatized lipids; and e) one or more coupled targeting ligands which bind to the nucleolin receptor. The nanoparticles according to the invention have a high loading capacity, ability to protect the encapsulated nucleic acid, a size below 250 ran and a charge close to neutrality, which are adequate features for intravenous administration. The nanoparticles of the present inventon have the ability to selectively delivery a siRNA to cancer cells and/or endothelial cells from angiogenic blood vessels leading to an effective silencing of a target gene. These nanoparticles are used for the treatment of angiogenesis- dependent diseases, namely cancer, inflammation, an auto-immune disease or an ocular disorder.