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Issue 7, 2011
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Cationic lipo-thiophosphoramidates for gene delivery: synthesis, physico-chemical characterization and gene transfection activity – comparison with lipo-phosphoramidates

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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.

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

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Publication details

The article was received on 03 Nov 2010, accepted on 16 Dec 2010 and first published on 17 Dec 2010


Article type: Paper
DOI: 10.1039/C0OB00981D
Org. Biomol. Chem., 2011,9, 2422-2432

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

    A. Fraix, T. Montier, N. Carmoy, D. Loizeau, L. Burel-Deschamps, T. Le Gall, P. Giamarchi, H. Couthon-Gourvès, J. Haelters, P. Lehn and P. Jaffrès, Org. Biomol. Chem., 2011, 9, 2422
    DOI: 10.1039/C0OB00981D

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