Cationic lipo-thiophosphoramidates for gene delivery: synthesis, physico-chemical characterization and gene transfection activity--comparison with lipo-phosphoramidates |
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Authors: | Fraix Aurore Montier Tristan Carmoy Nathalie Loizeau Damien Burel-Deschamps Laure Le Gall Tony Giamarchi Philippe Couthon-Gourvès Hélène Haelters Jean-Pierre Lehn Pierre Jaffrès Paul-Alain |
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Institution: | Université Européenne de Bretagne, Université de Brest, CEMCA, CNRS UMR 6521, IFR 148 ScInBIoS, 6 Avenue Le Gorgeu, 29238 Brest, France. |
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Abstract: | The synthesis of cationic lipo-thiophosphoramidates, a new family of cationic lipids designed for gene delivery, is reported herein. This new class of lipids is less polar than its oxygenated equivalent the lipo-phosphoramidates. Fluorescence anisotropy and FRET were used to determine the fluidity and fusogenicity of the lipo-phosphoramidates 3a-b and lipo-thiophosphoramidates 7a-b. The determination of both the size and the zeta potential of the nano-objects (liposomes and lipoplexes) and the determination of the DNA binding ability of the liposomes have completed the physico-chemical characterizations of the cationic lipids studied. Finally, the cationic lipids 3a-b and 7a-c have been evaluated as synthetic vectors for gene transfection into a variety of mammalian cell lines. The lipo-thiophosphoramidate 7a proved to be an efficient and low toxicity synthetic vector even when used at low lipid to DNA charge ratios. |
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