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Last Updated: October 23, 2021

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Claims for Patent: 8,058,069


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Summary for Patent: 8,058,069
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, B.C., CA)
Application Number:12/424,367
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 8,058,069
Patent Claims: 1. A nucleic acid-lipid particle comprising: (a) a nucleic acid; (b) a cationic lipid comprising from 50 mol % to 65 mol % of the total lipid present in the particle; (c) a non-cationic lipid comprising a mixture of a phospholipid and cholesterol or a derivative thereof, wherein the phospholipid comprises from 4 mol % to 10 mol % of the total lipid present in the particle and the cholesterol or derivative thereof comprises from 30 mol % to 40 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 a small interfering RNA (siRNA).

3. The nucleic acid-lipid particle of claim 2, wherein the siRNA comprises from about 15 to about 60 nucleotides.

4. The nucleic acid-lipid particle of claim 2, wherein the siRNA comprises at least one modified nucleotide.

5. The nucleic acid-lipid particle of claim 2, wherein the siRNA comprises at least one 2'-O-methyl (2'OMe) nucleotide.

6. The nucleic acid-lipid particle of claim 2, wherein said siRNA is about 19 to about 25 base pairs in length.

7. The nucleic acid-lipid particle of claim 2, wherein said siRNA comprises 3' overhangs.

8. The nucleic acid-lipid particle of claim 1, wherein the cationic lipid comprises from 52 mol % to 62 mol % of the total lipid present in the particle.

9. The nucleic acid-lipid particle of claim 1, wherein the phospholipid comprises dipalmitoylphosphatidylcholine (DPPC), distearoylphosphatidylcholine (DSPC), or a mixture thereof.

10. The nucleic acid-lipid particle of claim 1, wherein the conjugated lipid that inhibits aggregation of particles comprises a polyethyleneglycol (PEG)-lipid conjugate.

11. The nucleic acid-lipid particle of claim 10, wherein the PEG-lipid conjugate comprises a PEG-diacylglycerol (PEG-DAG) conjugate, a PEG-dialkyloxypropyl (PEG-DAA) conjugate, or a mixture thereof.

12. The nucleic acid-lipid particle of claim 11, wherein the PEG-DAA conjugate comprises a PEG-dimyristyloxypropyl (PEG-DMA) conjugate, a PEG-distearyloxypropyl (PEG-DSA) conjugate, or a mixture thereof.

13. The nucleic acid-lipid particle of claim 12, wherein the PEG has an average molecular weight of about 2,000 daltons.

14. The nucleic acid-lipid particle of claim 10, wherein the nucleic acid-lipid particle comprises about 57.1 mol % cationic lipid, about 7.1 mol % phospholipid, about 34.3 mol % cholesterol or a derivative thereof, and about 1.4 mol % PEG-lipid conjugate.

15. 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.

16. The nucleic acid-lipid particle of claim 1, wherein the nucleic acid in the nucleic acid-lipid particle is not substantially degraded after incubation of the particle in serum at 37.degree. C. for 30 minutes.

17. The nucleic acid-lipid particle of claim 1, wherein the nucleic acid is fully encapsulated in the nucleic acid-lipid particle.

18. The nucleic acid-lipid particle of claim 1, wherein the nucleic acid-lipid particle has a lipid:nucleic acid mass ratio of from about 5 to about 15.

19. The nucleic acid-lipid particle of claim 1, wherein the nucleic acid-lipid particle has a median diameter of from about 40 nm to about 150 nm.

20. The nucleic acid-lipid particle of claim 1, wherein the phospholipid comprises from 5 mol % to 9 mol % of the total lipid present in the particle.

21. The nucleic acid-lipid particle of claim 1, wherein the cholesterol or derivative thereof comprises from 32 mol % to 36 mol % of the total lipid present in the particle.

22. A pharmaceutical composition comprising a nucleic acid-lipid particle of claim 1 and a pharmaceutically acceptable carrier.

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