Lipid nanoparticles
AssigneeseTheRNA immunotherapies NV, Vrije Unversiteit Brussel
InventorsStefaan De Koker, Sanne Bevers, Peter Tomme
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Abstract
The present invention relates to the field of lipid nanoparticles (LPN); more specifically comprising an ionisable lipid, a phospholipid, a sterol, a PEG lipid and one or more nucleic acids. The LNP's of the present invention are characterized in having a minimal average diameter of about 140 nm, thereby inducing a more potent immune response. The present invention provides use of the LNPs for immunogenic delivery of nucleic acid molecules, specifically mRNA; thereby making them highly suitable for use in vaccines, such as for the treatment of cancer or infectious diseases. Finally, methods are provided for preparing such LNP's.
Claims16
A mixture of lipid nanoparticles, the lipid nanoparticles in the mixture comprising:
- from about 35 mol % to about 65 mol % of an ionizable lipid;
- from about 5 mol % to about 15 mol % of a phospholipid selected from the group consisting of DOPE, DOPC, and mixtures thereof;
- from about 15 mol % to about 50 mol % of a sterol;
- from about 0.5 mol % to about 2 mol % of a PEG lipid;
- and
- one or more mRNA molecules,
- wherein the lipid nanoparticles of the mixture have average diameters of from about 160 nm to about 230 nm to target the spleen in preference over the liver at a ratio of about 8 to 1 when administered intravenously;
- and
- wherein the ionisable lipid is a compound of formula (I):
- wherein:
- RCOO is alpha-D-Tocopherolsuccinoyl;
- and
- X is
A mixture of lipid nanoparticles, the lipid nanoparticles in the mixture comprising:
- from about 35 mol % to about 65 mol % of an ionizable lipid;
- from about 5 mol % to about 15 mol % DOPC;
- from about 15 mol % to about 50 mol % of a sterol;
- from about 0.5 mol % to about 2 mol % of a PEG-modified diacylglycerol;
- and
- one or more mRNA molecules,
- wherein the lipid nanoparticles of the mixture have average diameters of about 230 nm to target the spleen in preference over the liver at a ratio of about 8 to 1 when administered intravenously;
- and
- wherein the ionizable lipid is a compound of formula (I):
- with RCCO being α-D-Tocopherolsuccinoyl:
- and
- X being
A mixture of lipid nanoparticles, the lipid nanoparticles in the mixture comprising:
- from about 35 mol % to about 65 mol % of an ionizable lipid;
- from about 5 mol % to about 15 mol % DOPE;
- from about 15 mol % to about 50 mol % of a sterol;
- from about 0.5 mol % to about 2 mol % of a PEG-modified diacylglycerol;
- and
- one or more mRNA molecules,
- wherein the lipid nanoparticles of the mixture have average diameters of about 160 nm to target the spleen in preference over the liver when administered intravenously;
- and
- wherein the ionizable lipid is a compound of formula (I):
- with RCCO being alpha-D-Tocopherolsuccinoyl;
- and
- X being
Dependencies are inferred from the claim text.