title: "Smart" delivery of antisense oligonucleotides by anionic pH-sensitive liposomes.
abstract: Antisense oligonucleotides are molecules that are able to inhibit gene expression being, therefore, potentially active for the treatment of viral infections cancer or inflammatory diseases. However, because of their poor stability in biological medium and their weak intracellular penetration, "smart" delivery systems such as anionic pH-sensitive liposomes were designed. Most known liposome formulations contain a specific phospholipid, phosphatidylethanolamine (PE), which undergoes a transition from lamellar to inverted micelles structures at low pH and allow fusion of liposomal and endosomal membranes and by consequence destabilization of the endosomes. Therefore, liposomes made of PE are able to release their contents in response to acidic pH within the endosomal system while remaining stable in plasma thus improving the cytoplasmic delivery of oligonucleotides after endocytosis. This review illustrates the advantages of this approach for the delivery of antisense oligonucleotides.
authors.affiliation: School of Pharmacy, University of Paris-Sud, UMR CNRS 8612, 5 Rue Jean Baptiste Clément, 92296 Châtenay-Malabry, France. elias.fattal@cep.u-psud.fr
authors.forename: Elias
authors.initials: E
authors.lastname: Fattal
authors.forename: Patrick
authors.initials: P
authors.lastname: Couvreur
authors.forename: Catherine
authors.initials: C
authors.lastname: Dubernet
mesh_terms: D000818:Animals; D000838:Anions; D003593:Cytoplasm / Q000378:metabolism; D016503:Drug Delivery Systems; D004355:Drug Stability; D004705:Endocytosis / Q000187:drug effects / Q000502:physiology; D006863:Hydrogen-Ion Concentration; D008081:Liposomes / Q000737:chemistry*; D016376:Oligonucleotides, Antisense / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D010714:Phosphatidylethanolamines / Q000737:chemistry
chemical_list: D000838:Anions; D008081:Liposomes; D016376:Oligonucleotides, Antisense; D010714:Phosphatidylethanolamines; C483858:phosphatidylethanolamine