Lipophosphoramidates as lipidic part of lipospermines for gene delivery |
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Authors: | Lamarche François Mével Mathieu Montier Tristan Burel-Deschamps Laure Giamarchi Philippe Tripier Raphaël Delépine Pascal Le Gall Tony Cartier Dominique Lehn Pierre Jaffrès Paul-Alain Clément Jean-Claude |
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Institution: | UMR CNRS 6521, Université de Bretagne Occidentale, UFR Sciences, 6, Avenue Le Gorgeu, CS 93837, F-29238 Brest cedex 3, France. |
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Abstract: | The DNA compacting properties of polyamines (especially spermine) are well-known, hence the use of spermine as the cationic part in several synthetic DNA carriers. Here, we describe the synthesis of modified spermines, with a "lipophosphoramidate" as the lipidic part, and their use for efficient in vitro transfection. Physicochemical measurements (particle size, zeta potentials, pKa determination) and gel retardation assays were also performed. Theoretical membrane-disrupting ability was established by FRET. Taken together, our results indicate that lipophosphoramidates constitute an interesting alternative to "classical" lipidic parts of cationic lipids used as DNA carriers. |
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