Improved lipid formulation

Details Improved lipid formulation Improved lipid formulation

A - Human Necessities

61

K

A61K 9/127 (2006.01) A61K 48/00 (2006.01)

Patent

CA 2751342

The invention features an improved lipid formulation comprising a cationic lipid of formula (A), a neutral lipid, a sterol and a PEG or PEG-modified lipid, where R1 and R2 are independently alkyl, alkenyl or alkynyl, each can be optionally substituted, and R3 and R4 are independently lower alkyl or R3 and R4 can be taken together to form an optionally subsituted heterocyclic ring. In one embodiment, R1 and R2 are independently selected from oleoyl, pamitoyl, steroyl, linoleyl and R3 and R4 are methyl. Also disclosed are targeting lipids, and specific lipid formulations comprising such targeting lipids.

La présente invention concerne une préparation lipidique améliorée comprenant un lipide cationique de formule (A), un lipide neutre, un stérol et un lipide PEG ou modifié par PEG, où R1 et R2 sont indépendamment un groupe alkyle, alcényle ou alcynyle, chacun pouvant être facultativement substitué, et R3 et R4 sont indépendamment un groupe alkyle inférieur ou R3 et R4 peuvent être pris ensemble pour former un anneau hétérocyclique facultativement substitué. Dans un mode de réalisation, R1 et R2 sont indépendamment choisis parmi un groupe oléoyl, palmitoyl, stéaroyl, linoleyl et R3 et R4 sont un groupe méthyle. L'invention concerne également des lipides ciblants et des préparations lipidiques spécifiques comprenant de tels lipides ciblants.

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