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Claims for Patent: 5,741,516

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Claims for Patent: 5,741,516

Title: Sphingosomes for enhanced drug delivery
Abstract:Liposomal formulations having extended circulation time in vivo and increased drug retention are comprised of sphingomyelin and cholesterol and have an acidic intraliposomal pH. The formulations have enhanced stability and thus are used in methods which provide improved drug delivery and more effective treatment. The delivery of ciprofloxacin, and alkaloid drugs, particularly swainsonine, vincristine and vinblastine, is significantly improved.
Inventor(s): Webb; Murray S. (Vancouver, CA), Bally; Marcel B. (Bowen Island, CA), Mayer; Lawrence D. (N. Vancouver, CA), Miller; James J. (Vancouver, CA), Tardi; Paul G. (Richmond, CA)
Assignee: Inex Pharmaceuticals Corporation (Vancouver, CA)
Application Number:08/572,555
Patent Claims: 1. A liposomal composition for delivery of a therapeutic compound to a mammalian host which comprises a liposome having one or more membranes which comprise sphingomyelin and cholesterol, a liposomal interior having a pH less than that of the liposomal exterior, and a therapeutic compound contained in said liposome for delivery to the host.

2. The liposomal composition of claim 1, wherein the sphingomyelin and cholesterol are present at a molar ratio from 75/25 mol%/mol% sphingomyelin/cholesterol to 30/50 mol%/mol% sphingomyelin/cholesterol.

3. The liposomal composition of claim 2, wherein the sphingomyelin and cholesterol are present at a molar ratio from 70/30 mol%/mol% sphingomyelin/cholesterol to 40/45 mol%/mol% sphingomyelin/cholesterol.

4. The liposomal composition of claim 3, wherein the sphingomyelin and cholesterol are present at a ratio of approximately 55/45 mol%/mol% sphingomyelin/cholesterol.

5. The liposomal composition of claim 1, wherein the lipophilic therapeutic compound is an alkaloid.

6. The liposomal composition of claim 5 wherein the alkaloid is selected from vincristine, vinblastine, swainsonine or etoposide or prodrugs thereof.

7. The liposomal composition of claim 6, wherein the alkaloid is vincristine.

8. The liposomal composition of claim 6, wherein the alkaloid is swainsonine.

9. The liposomal composition of claim 6, wherein vincristine is present at a drug to lipid ratio of approximately 0.01/1.0 to 0.2/1.0 (wt/wt) and swainsonine is present at a drug to lipid ratio of 0.01/1.0 to 0.5/1.0 (mol/mol) .

10. The liposomal composition of claim 1, further comprising at least one lipid selected from a phosphatidylcholine, phosphatidylethanolamine, phosphatidylserine, phosphatidylglycerol, phosphatidic acid, cardiolipin, phosphatidylinositol, ceramide, cerebroside and ganglioside.

11. The liposomal composition of claim 1, wherein the liposomes are unilamellar.

12. The liposomal composition of claim 1, wherein the liposomes have mean diameters of about 0.05 microns to 0.45 microns.

13. The liposomal composition of claim 1, wherein the liposomes have mean diameters of about 0.05 microns to 0.2 microns.

14. The liposomal composition of claim 1 wherein the interior of said liposome is pH 2 to pH 5.

15. The liposomal composition of claim 1, wherein the interior comprises a citrate buffer at about pH 4.0.

16. A method for delivering an alkaloid therapeutic compound to a tumor susceptible to inhibition by said compound, comprising:

administering to a host containing said tumor, a liposomal composition according to claim 1 which comprises said compound or a pharmaceutically acceptable salt thereof.

17. The method of claim 16, wherein the cholesterol is present in the liposomal composition at a total molar proportion of 30% to 50%.

18. The method of claim 17, wherein the sphingomyelin and cholesterol are present at a ratio of about 55/45, mol%/mol%, respectively.

19. The method of claim 16, wherein the alkaloid compound is vincristine or swainsonine.

20. The method of claim 19, wherein the alkaloid compound is vincristine.

21. The method of claim 19, wherein the alkaloid compound is swainsonine.

22. The method of claim 19, wherein vincristine is present in the liposomal composition at a drug to lipid ratio of approximately 0.01/1.0 to 0.2/1.0 (wt/wt) and swainsonine is present at a drug to lipid ratio of 0.01/1.0 to 0.5/1.0 (mol/mol).

23. The method of claim 16, wherein the liposomal composition containing said alkaloid compound is administered repeatedly to the host to maintain a concentration of said compound sufficient to inhibit the tumor but less than an amount which causes unacceptable toxicity to the host.

24. The method of claim 16, wherein the liposomal composition containing said alkaloid compound is administered intravenously.

25. The method of claim 16, wherein the liposomal composition containing said alkaloid compound is administered parenterally.

26. The method of claim 16, wherein the liposomal composition containing said alkaloid is administered orally.

27. The method of claim 16, wherein the liposomes of the liposomal composition administered to the host are unilamellar.

28. The method of claim 27, wherein the unilamellar liposomes of said composition have a mean diameter of 0.05 microns to 0.45 microns.

29. The method of claim 28, wherein the unilamellar liposomes of said composition have a mean diameter of 0.05 microns to 0.2 microns.

30. A method for delivering an alkaloid immunomodulating compound, comprising:

administering to a host a liposomal composition according to claim 1 comprising said immunomodulator or a pharmaceutically acceptable salt thereof.

31. The method of claim 30, wherein the compound is swainsonine.

32. The method of claim 31, wherein swainsonine is delivered parenterally or orally.

33. The method of claim 32, wherein swainsonine is delivered intravenously or orally.

34. The method of claim 31, wherein swainsonine is present in the liposomal composition at a drug to lipid ratio of approximately 0.01/1.0 to 0.5/1.0 (mol/mol).

35. The method of claim 1, wherein the therapeutic compound is ciprofloxacin or derivative thereof.
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