Liposomal compositions, and methods of using liposomal compositions to treat dislipidemias

• US 6,773,719 B2
• Filed: 08/07/2001
• Issued: 08/10/2004
• Est. Priority Date: 03/04/1994
• Status: Expired due to Fees

• Current Assignee: Pfizer Inc., University of British Columbia
• Original Assignee: Esperion LUV Development, Inc. (Pfizer Inc.), University of British Columbia
• Inventors: Williams, Kevin Jon, Rodrigueza, Wendi V., Hope, Michael J.
• Primary Examiner(s): Kishore, Gollamudi S.
• Application Number:
  US09/924,222
• Publication Number:
  US 20020110587A1
• Time in Patent Office: 1,099 Days
• Field of Search: 424/450, 428/402.2, 514/824
• US Class Current: 424/450
• CPC Class Codes: A61K 31/685 one of the hydroxy compounds having nitrogen atoms, e.g. phosphatidylserine, lecithin
• CPC Class Codes: A61K 9/0019 Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner non-active ingredients are additionally classified in A61K47/00
• CPC Class Codes: A61K 9/127 Liposomes
• CPC Class Codes: Y10T 428/2984 Microcapsule with fluid core [includes liposome]

Abstract

The present invention provides a liposomal composition for treating dislipidemias in human subjects, a method of using a liposomal composition, and devices and modes of operation of the devices and of the compositions, and kits related thereto. The invention provides for the reverse transport of cholesterol from peripheral tissues to the liver in a warm blood mammal while controlling plasma atherogenic lipoprotein concentrations, including LDL concentrations. A method described above and mode of operation of the devices includes the stop of administering an effective amount of a multiplicity of acceptors comprised of phospholipids substantially free of sterol. A method described above optionally includes the stop of periodically assaying atherogenic lipoprotein concentrations with an assay during the treatment period to assess atherogenic lipoprotein concentrations and obtain an atherogenic lipoprotein profile.

Claims

1. A method for treating a vascular disease or condition selected from the group consisting of atherosclerosis, hypercholesterolemia and hypoalphalipoproteinemia in a human, comprising administering to a human in need thereof a pharmaceutically acceptable and a therapeutically effective amount of unilamellar phospholipid liposomes having empty aqueous cores and having a Gaussian distribution wherein at least about 68% of the liposomes have a mean diameter of 125±

30 nm.

3. The method of claim 1 or 2 in which the therapeutically effective amount is about 10 mg to about 1600 mg per kg body weight.

4. The method of claim 1 or 2 in which the therapeutically effective amount is about 300 mg per kg body weight.

5. The method of claim 1 or 2 in which the therapeutically effective amount is about 0.1 to 1.5 gm/kg.

6. The method of claim 1 or 2 in which the therapeutically effective amount is about 0.28 to 0.42 gm/kg.

7. The method of claim 1 or 2 in which the liposomes are administered once.

8. The method of claim 1 or 2 in which the liposomes are administered more than once.

9. The method of claim 1 or 2 in which the liposomes are administered in repeated doses.

10. The method of claim 1 or 2 in which said liposomes are administered weekly.

11. The method of claim 1 or 2 in which said liposomes are administered once per week for 4 to 16 weeks.

12. The method of claim 1 or 2 in which said liposomes are administered once per week for 10 weeks.

2. A method for treating a vascular disease or condition selected from the group consisting of atherosclerosis, hypercholesterolemia and hypoalphalipoproteinemia in a human, comprising administering to a human in need thereof a pharmaceutically acceptable and a therapeutically effective amount of unilamellar phospholipid liposomes having empty aqueous cores and having a Gaussian distribution wherein at least about 68% of the liposomes have a mean diameter between 100-150 nm.