LIPID NANOPARTICLES Russian patent published in 2025 - IPC A61K9/00 A61K47/14 A61K47/24 A61K38/00 

Abstract RU 2837542 C1

FIELD: biotechnology.

SUBSTANCE: what is described is an mRNA vaccine containing one or more lipid nanoparticles (LNP), which contain: from 50 to 65 mol.% of an ionisable lipid; from 6 to 15 mol.% of phospholipid; sterol; PEG-lipid and one or more mRNA molecules, according to the invention, said PEG-lipid is a C18-PEG2000 lipid, said LNP contains less than 1 mol.% of said PEG-lipid, preferably 0.5 to 0.9 mol.% of said PEG -lipid. Disclosed is a lipid nanoparticle (LNP) for use in vaccination by means of mRNA, wherein said LNP contains: from 50 to 65 mol.% of an ionisable lipid; from 6 to 15 mol.% of phospholipid; sterol; PEG-lipid and one or more mRNA molecules, according to the invention, said PEG-lipid is a C18-PEG2000 lipid, said LNP contains less than 1 mol.% of said PEG-lipid, preferably 0.5 to 0.9 mol.% of said PEG-lipid. Also disclosed is a lipid nanoparticle (LNP) for use in a pharmaceutical composition comprising: 50 to 65 mol.% of an ionisable lipid; from 6 to 15 mol.% of phospholipid; sterol; PEG-lipid and one or more nucleic acid molecules, according to the invention, said PEG-lipid is a C18-PEG2000 lipid and said LNP contains less than about 1 mol.% of said PEG-lipid, preferably from 0.5 to 0.9 mol.% of said PEG-lipid. Disclosed is the use of a pharmaceutical composition in medicine, for example in the treatment of cancer or infectious diseases, wherein said composition comprises one or more said lipid nanoparticles and a pharmaceutically acceptable carrier, and wherein said nanoparticles are selected from a group comprising mRNA coding an immunomodulatory polypeptide and/or mRNA coding an antigen. Also disclosed is the use of a lipid nanoparticle in medicine, for example in treating cancer or infectious diseases.

EFFECT: authors of the invention unexpectedly found that PEG-lipids, which are present in low amounts, id est less than about 1 mol.%, in LNP, provide formation of nanoparticles, which are especially suitable for immunogenic delivery of mRNA with systemic introduction of LNP, and in addition, said effects are more pronounced in longer chain PEG lipids, such as diC18-PEG lipids.

17 cl, 6 dwg, 4 tbl, 6 ex

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RU 2 837 542 C1

Authors

De Koker, Stefan

Bevers, Sanne

Skhiffelers, Rajmond, Mikhel

Koejmans, Sander, Aleksander, Antonius

Dates

2025-04-01Published

2021-01-21Filed