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Cationic lipo-thiophosphoramidates for gene delivery: synthesis, physico-chemical characterization and gene transfection activity – comparison with lipo-phosphoramidates

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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https://hal.univ-brest.fr/hal-01577011
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Submitted on : Thursday, August 24, 2017 - 3:52:57 PM
Last modification on : Thursday, November 29, 2018 - 4:09:16 PM

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Aurore Fraix, Tristan Montier, Nathalie Carmoy, Damien Loizeau, Laure Burel-Deschamps, et al.. Cationic lipo-thiophosphoramidates for gene delivery: synthesis, physico-chemical characterization and gene transfection activity – comparison with lipo-phosphoramidates. Organic and Biomolecular Chemistry, Royal Society of Chemistry, 2011, 9 (7), ⟨10.1039/C0OB00981D⟩. ⟨hal-01577011⟩

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