Paul-Alain Jaffrès et al. from the Université de Brest report the synthesis of cationic lipo-phosphoramidates and lipo-thiophosphoramidates possessing the capacity to compact and transfect plasmid DNA. They investigated the effect of different functional groups on the physico-chemical properties of the lipids and found that they could fine tune the fluidity and fusogenicity of the liposomes. The best of the thiophosphoramidates synthesised provided highly efficient transfection—even at low charge levels, in contrast to the older phosphoramidates—demonstrating that a minor modification of the chemical structure of the cationic lipids may have a direct impact on their gene transfection ability.
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Cationic lipo-thiophosphoramidates for gene delivery: synthesis, physico-chemical characterization and gene transfection activity – comparison with lipo-phosphoramidates
Aurore Fraix, Tristan Montier, Nathalie Carmoy, Damien Loizeau, Laure Burel-Deschamps, Tony Le Gall, Philippe Giamarchi, Hélène Couthon-Gourvès, Jean-Pierre Haelters, Pierre Lehn and Paul-Alain Jaffrès
Org. Biomol. Chem., 2011, Advance Article
DOI: 10.1039/C0OB00981D
