Compounds and methods for enhancing delivery of free...

C - Chemistry – Metallurgy – 12 – Q

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C12Q 1/68 (2006.01) A61K 48/00 (2006.01) C07H 21/04 (2006.01) C12N 15/00 (2006.01) C12N 15/85 (2006.01) C12N 15/87 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2341017

The discovery of simple, nontoxic, and pharmaceutically defined methods for genetic modification of cells and tissues would enable development of a variety of molecular medicines. "Free", "direct", or "naked" polynucleotide administration is a simple, apparently safe, and pharmaceutically defined polynucleotide delivery method. Murine, macaque, and clinical human experiments have demonstrated transfection of various tissues, such as respiratory tissues, after direct application of "free" polynucleotide. However, direct DNA transfection is relatively inefficient in comparison to many transduction systems. The invention herein is directed to transfection enhancing agents which augment the transfection activity of "free" polynucleotide, thereby facilitating the development of simple and safe alternatives to tissue transfection, more particularly respiratory tissue transfection. The experiments described herein indicate that nucleases, both extra-and intra-cellular, present in many biological fluids, such as respiratory fluid, accelerate clearance of biologically active plasmid from the tissue, and that co-administration of a nuclease inhibitor together with free polynucleotide results in marked enhancement of expression of the polynucleotide of interest. These findings support the disclosed invention of an improved polynucleotide delivery system, a "free" plasmid-based transfection technology.

La découverte de procédés pharmaceutiquement définis, non toxiques et simples pour modifier génétiquement des cellules et des tissus permet de développer des variétés de médecines moléculaires. L'administration d'un polynucléotide libre, direct ou nu est un procédé d'apport de polynucléotide pharmaceutiquement défini, simple, et apparemment sûr. Des essais cliniques effectués sur des souris, des macaques et des hommes ont montré une transaction de différents tissus, tels que des tissus respiratoires, après l'application directe d'un polynucléotide libre. Toutefois, une transfection directe d'ADN est relativement inefficace en comparaison de beaucoup de systèmes de transfection. Cette invention concerne des agents d'amélioration de transfection qui augmentent l'activité de transfection d'un polynucléotide libre, ce qui facilite le développement d'alternatives simples et sûres à la transaction de tissu, et plus particulièrement à la transaction de tissu respiratoire. Les expériences décrites dans les spécifications montrent que des nucléases, à la fois extra- et intracellulaires, présents dans de nombreux fluides biologiques, tel qu'un fluide respiratoire, accélèrent le dégagement de plasmide biologiquement actif à partir du tissu, et que la co-administration d'un inhibiteur de nucléase avec un polynucleotide libre a pour effet une amélioration marquée de l'expression du polynucléotide considéré. Ces découvertes justifient l'invention d'un système d'apport de polynucléotide amélioré, et d'une technologie de transfection à base de plamide libre.

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