Cationic oil-in-water emulsions
AssigneeGlaxosmithkline Biologicals SA
InventorsLuis Brito, Andrew Geall, Derek O'Hagan, Manmohan Singh
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Abstract
This invention generally relates to cationic oil-in-water emulsions that can be used to deliver negatively charged molecules, such as an RNA molecule. The emulsion particles comprise an oil core and a cationic lipid. The cationic lipid can interact with the negatively charged molecule thereby anchoring the molecule to the emulsion particles. The cationic emulsions described herein are particularly suitable for delivering nucleic acid molecules (such as an RNA molecule encoding an antigen) to cells and formulating nucleic acid-based vaccines.
Claims32
A composition comprising an RNA molecule complexed with a particle of a cationic oil-in-water emulsion,
- wherein the particle comprises (a) an oil core that is in liquid phase at 25° C., and (b) a cationic lipid, such that the overall net charge of the emulsion particle prior to RNA complexation is positive, and
- wherein said RNA encodes a protein antigen and said RNA is anchored to the surface of said particle by non-covalent interactions;
- wherein, when administered in an effective amount to a mammal, the composition elicits antibody titers to the antigen equal to or greater than the RNA administered to the mammal not complexed with the particle, further wherein the RNA does not include modified nucleobases, other than an optional 5′ cap.
A composition comprising an RNA molecule complexed with a particle of a cationic oil-in-water emulsion,
- wherein the particle comprises (a) an oil core that is in liquid phase at 25° C., and (b) a cationic lipid, such that the overall net charge of the emulsion particle prior to RNA complexation is positive, and
- wherein said RNA molecule encodes a protein antigen and said RNA is anchored to the surface of said particle by non-covalent interactions,
- wherein, when administered in an effective amount to a mammal, the composition elicits antibody titers to the antigen equal to or greater than the RNA administered to the mammal:
- i) not complexed with the particle and ii) at a 10-fold higher concentration, relative to the complexed RNA, further wherein the RNA does not include modified nucleobases, other than an optional 5′ cap.
A composition comprising an RNA molecule complexed with a particle of a cationic oil-in-water emulsion,
- wherein the particle comprises:
- (a) 0.2-10% (v/v) squalene core that is in liquid phase at 25° C., (b) 0.5-5.0 mg/ml of a cationic lipid, such that the overall net charge of the emulsion particle prior to RNA complexation is positive, (c) 0.01-2.5% (v/v) of a non-ionic surfactant and
- wherein said RNA molecule encodes a protein antigen and said RNA is anchored to the surface of said particle by non-covalent interactions;
- wherein, when administered in an effective amount to a mammal, the composition elicits antibody titers to the antigen equal to or greater than the RNA administered to the mammal not complexed with the particle, further wherein the RNA does not include modified nucleobases, other than an optional 5′ cap.
Dependencies are inferred from the claim text.