Folate-equipped pegylated archaeal lipid derivatives: synthesis and transfection properties |
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Authors: | Lainé Céline Mornet Emmanuel Lemiègre Loïc Montier Tristan Cammas-Marion Sandrine Neveu Cécile Carmoy Nathalie Lehn Pierre Benvegnu Thierry |
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Institution: | Ecole Nationale Supérieure de Chimie de Rennes, UMR CNRS 6226, Equipe Chimie Organique et Supramoléculaire, Av. Général Leclerc, 35700 Rennes, France. |
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Abstract: | We have previously shown that synthetic archaeal lipid analogues are useful vectors for drug/gene delivery. We report herein the synthesis and gene transfer properties of a series of novel di- and tetraether-type archaeal derivatives with a poly(ethylene glycol) (PEG) chain and further equipped with a folic acid (FA) group. The synthetic strategy and the purification by dialysis ensured complete removal of free FA. The lipids were mixed with a conventional glycine betaine-based cationic lipid and the resulting formulations were tested in transfection assays after complexation with plasmid DNA. All four novel co-lipids afforded efficient in vitro gene transfection. Moreover, the FA-equipped derivatives permitted ligand/receptor-based targeted transfection; their activity was inhibited when free FA was added to the transfection medium. These novel archaeal derivatives equipped with FA-PEG moieties may thus be of great interest for targeted in vivo transfection. |
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Keywords: | archael lipids cell targeting folic acid gene delivery |
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