Cytofectin dimers and methods of use thereof

Details Cytofectin dimers and methods of use thereof Cytofectin dimers and methods of use thereof

C - Chemistry, Metallurgy

07

C

C07C 275/14 (2006.01) A61K 9/127 (2006.01) A61K 39/00 (2006.01) A61K 39/39 (2006.01) C07C 217/42 (2006.01) C07C 237/08 (2006.01) C12N 15/88 (2006.01)

Patent

CA 2375727

A composition is provided comprising a novel cationic lipid compound having hydrophobic tails and two quaternary ammonium headgroups bridged by a linker. The composition is useful as a cytofectin for facilitating delivery and transfection of biologically active agents, particularly anionic bioactive agents such as DNA, into cells. The composition is useful also as an adjuvant for enhancing the humoral immune response of a vertebrate to an immunogen, especially an immunogen encoded by a polynucleotide-based vaccine. In certain preferred embodiments, the cationic lipid compound is a dimer containing quaternary ammonium headgroups bridged by a linker having DNA and/or cell receptor binding affinity, such as a polypeptide or polyamine. Also disclosed is an immunogenic composition comprising an immunogen and the composition of the present invention.

On décrit une composition qui contient un nouveau composé lipidique cationique ayant des queues hydrophobes et deux groupes de tête ammonium quaternaire pontés par un agent de liaison. La composition est utile en tant que cytofectine pour faciliter l'apport et la transfection d'agents biologiquement actifs, plus particulièrement d'agents bioactifs anioniques tels que de l'ADN dans des cellules. La composition est également utile en tant qu'adjuvant servant à stimuler la réponse immune humorale d'un vertébré à un immunogène, plus spécialement un immunogène codé par un vaccin à base de polynucléotide. Dans certaines formes de réalisation préférées, le composé lipidique cationique est un dimère contenant des groupes de tête ammonium pontés par un agent de liaison ayant une affinité de liaison avec le récepteur cellulaire et/ou l'ADN, tel qu'un polypeptide ou une polyamine. On décrit également une composition immunogène contenant un immunogène et la composition selon la présente invention.

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