Lipid compositions
View Patent ↗Disclosed herein are lipid compositions comprising a cationic lipid of formula (I), a neutral lipid, a sterol and a PEG or PEG-modified lipid, wherein formula (I) is (F). Also disclosed are methods of producing the cationic lipid of formula (I).
1. A composition comprising (a) a sterol; (b) a neutral lipid; (c) a PEG or a PEG-modified lipid; and (d) a compound of formula (V), or a salt thereof
2. The composition of claim 1 , wherein the compound of formula V is an inorganic or organic salt thereof.
3. The composition of claim 2 , wherein the compound of formula V is an organic acid thereof.
4. The composition of claim 1 , wherein the sterol is cholesterol.
5. The composition of claim 1 , wherein the PEG-modified lipid is PEG-DMG.
6. The composition of claim 1 , wherein the neutral lipid is DSPC.
7. The composition of claim 1 , wherein the composition comprises about 25-75% of the compound of formula V, about 5-50% of the sterol, about 0.5-20% of the PEG or PEG-modified lipid and about 0.1-15% of the neutral lipid.
8. The composition of claim 1 , wherein the composition comprises about 35-65% of the compound of formula V, about 15-45% of the sterol, about 0.5-10% of the PEG or PEG-modified lipid and about 3-15% of the neutral lipid.
9. The composition of claim 1 , wherein the composition comprises about 40-65% of the compound of formula V, about 25-40% of the sterol, about 0.5-5% of the PEG or PEG-modified lipid, and about 5-10% of the neutral lipid.
10. The composition of claim 1 , wherein the composition comprises about 50% of the compound of formula V, about 38.5% of the sterol, about 1.5% of the PEG or PEG-modified lipid, and about 10% of the neutral lipid.
11. The composition of claim 4 , wherein the composition comprises about 50% of the compound of formula (VI), about 38.5% of the sterol, about 1.5% of the PEG or PEG-modified lipid, and about 10% of the neutral lipid.
12. The lipid formulation of claim 1 , further comprising a targeting lipid comprising N-acetyl galactosamine as a targeting moiety.
13. The formulation of claim 12 , wherein said targeting lipid is present in the composition in a molar amount of from about 0.001% to about 5%.
14. The formulation of claim 12 , wherein said targeting lipid is present in the composition in a molar amount of from about 0.005% to about 1.5%.
15. The formulation of claim 12 , wherein said targeting lipid is selected from:
16. The composition of claim 1 , wherein the composition is an association complex.
17. The composition of claim 1 , wherein the composition is a liposome.
18. The composition of claim 1 , further comprising a nucleic acid agent.
19. The composition of claim 1 , further comprising single stranded RNA agent.
20. The composition of claim 1 , further comprising a double stranded RNA agent.
21. The composition of claim 18 , wherein the ratio of lipid:nucleic acid is about 3 to about 15.
22. The composition of claim 1 , further comprising at least one apolipoprotein.