title: Neo-mannosylated liposomes: synthesis and interaction with mouse Kupffer cells and resident peritoneal macrophages.
abstract: In order to target liposomes to cells expressing at their surface mannose receptors, e.g. mouse Kupffer cells and peritoneal macrophages, we have developed a new synthetic strategy which allows a chemically well defined preparation of neo-mannosylated vesicles. alpha-D-Thiomannopyranoside residues, substituted with a hydrophilic spacer arm and functionalized with a sulfhydryl group, were covalently coupled to preformed large unilamellar vesicles containing 4-(p-maleimidophenyl)butyryl phosphatidylethanolamine. Liposomes, containing 15 mol% of mannosyl residues, were specifically aggregated with concanavalin A; this aggregation could be reversed by an excess of free methyl alpha-D-mannopyranoside indicating that the surface ligands were freely accessible to the lectin. The neo-mannosylated liposomes presented in vitro an increased binding to cells possessing alpha-D-mannose specific binding sites. At 37 degrees C a specific binding, up to 9-fold compared to control vesicles, was observed. These neo-mannosylated vesicles represent attractive tools for targeting bio-active molecules to macrophage-associated diseases.
authors.affiliation: Laboratoire de Chimie Enzymatique, CNRS UA 1182, Université Louis Pasteur, Strasbourg, France.
authors.forename: C D
authors.initials: CD
authors.lastname: Muller
authors.forename: F
authors.initials: F
authors.lastname: Schuber
mesh_terms: D000818:Animals; D003208:Concanavalin A; D007202:Indicators and Reagents; D007700:Kinetics; D007728:Kupffer Cells / Q000276:immunology*; D037181:Lectins, C-Type; D008081:Liposomes / Q000138:chemical synthesis* / Q000378:metabolism; D008264:Macrophages / Q000276:immunology*; D008358:Mannose / Q000378:metabolism*; D000090323:Mannose Receptor; D037241:Mannose-Binding Lectins; D051379:Mice; D015394:Molecular Structure; D011956:Receptors, Cell Surface; D011971:Receptors, Immunologic / Q000378:metabolism*
chemical_list: D007202:Indicators and Reagents; D037181:Lectins, C-Type; D008081:Liposomes; D000090323:Mannose Receptor; D037241:Mannose-Binding Lectins; D011956:Receptors, Cell Surface; D011971:Receptors, Immunologic; D003208:Concanavalin A; D008358:Mannose