Claims for Patent: 9,364,435

Summary for Patent: 9,364,435

Title:	Lipid formulations for nucleic acid delivery
Abstract:	The present invention provides novel, stable lipid particles comprising one or more active agents or therapeutic agents, methods of making the lipid particles, and methods of delivering and/or administering the lipid particles. More particularly, the present invention provides stable nucleic acid-lipid particles (SNALP) comprising a nucleic acid (such as one or more interfering RNA), methods of making the SNALP, and methods of delivering and/or administering the SNALP.
Inventor(s):	Yaworski; Edward (Maple Ridge, CA), Lam; Kieu (Surrey, CA), Jeffs; Lloyd (Delta, CA), Palmer; Lorne (Vancouver, CA), MacLachlan; Ian (Mission, CA)
Assignee:	PROTIVA BIOTHERAPEUTICS, INC. (Burnaby, BC, CA)
Application Number:	14/462,441
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 9,364,435
Patent Claims:	1. A nucleic acid-lipid particle comprising: (a) a nucleic acid; (b) a cationic lipid comprising from 50 mol % to 85 mol % of the total lipid present in the particle; (c) a non-cationic lipid comprising from 13 mol % to 49.5 mol % of the total lipid present in the particle; and (d) a conjugated lipid that inhibits aggregation of particles comprising from 0.5 mol % to 2 mol % of the total lipid present in the particle. 2. The nucleic acid-lipid particle of claim 1, wherein the nucleic acid comprises an interfering RNA, mRNA, an antisense oligonucleotide, a ribozyme, a plasmid, an immunostimulatory oligonucleotide, or mixtures thereof. 3. The nucleic acid-lipid particle of claim 2, wherein the interfering RNA comprises a small interfering RNA (siRNA), an asymmetrical interfering RNA (aiRNA), a microRNA (miRNA), or mixtures thereof. 4. The nucleic acid-lipid particle of claim 1, wherein the cationic lipid comprises from 50 mol % to 65 mol % of the total lipid present in the particle. 5. The nucleic acid-lipid particle of claim 1, wherein the non-cationic lipid comprises a mixture of a phospholipid and cholesterol or a derivative thereof. 6. The nucleic acid-lipid particle of claim 5, wherein the phospholipid comprises dipalmitoylphosphatidylcholine (DPPC), distearoylphosphatidylcholine (DSPC), or a mixture thereof. 7. The nucleic acid-lipid particle of claim 5, wherein the phospholipid comprises from 3 mol % to 15 mol % of the total lipid present in the particle. 8. The nucleic acid-lipid particle of claim 5, wherein the cholesterol or derivative thereof comprises from 30 mol % to 40 mol % of the total lipid present in the particle. 9. The nucleic acid-lipid particle of claim 1, wherein the conjugated lipid that inhibits aggregation of particles comprises a polyethyleneglycol (PEG)-lipid conjugate. 10. The nucleic acid-lipid particle of claim 9, wherein the PEG-lipid conjugate comprises a PEG-diacylglycerol (PEG-DAG) conjugate, a PEG-dialkyloxypropyl (PEG-DAA) conjugate, or a mixture thereof. 11. The nucleic acid-lipid particle of claim 10, wherein the PEG-DAA conjugate comprises a PEG-dimyristyloxypropyl (PEG-DMA) conjugate, a PEG-distearyloxypropyl (PEG-DSA) conjugate, or a mixture thereof. 12. The nucleic acid-lipid particle of claim 1, wherein the conjugated lipid that inhibits aggregation of particles comprises from 1 mol % to 2 mol % of the total lipid present in the particle. 13. The nucleic acid-lipid particle of claim 1, wherein the nucleic acid is fully encapsulated in the nucleic acid-lipid particle. 14. A pharmaceutical composition comprising a nucleic acid-lipid particle of claim 1 and a pharmaceutically acceptable carrier. 15. A method for introducing a nucleic acid into a cell, the method comprising: contacting the cell with a nucleic acid-lipid particle of claim 1. 16. A method for the in vivo delivery of a nucleic acid, the method comprising: administering to a mammalian subject a nucleic acid-lipid particle of claim 1. 17. A method for treating a disease or disorder in a mammalian subject in need thereof, the method comprising: administering to the mammalian subject a therapeutically effective amount of a nucleic acid-lipid particle of claim 1. 18. The method of claim 17, wherein the disease or disorder is a viral infection. 19. The method of claim 17, wherein the disease or disorder is a liver disease or disorder. 20. The method of claim 17, wherein the disease or disorder is cancer.