Liposomes containing modified cholesterol for organ targeting

• US 4,544,545 A
• Filed: 06/20/1983
• Issued: 10/01/1985
• Est. Priority Date: 06/20/1983
• Status: Expired due to Fees

• Current Assignee: Trustees of University of Massachusetts
• Original Assignee: Trustees University of Massachusetts
• Inventors: Davis, Michael A., Ryan, Patrick J., Melchior, Donald L.
• Primary Examiner(s): Nucker, Christine M.
• Application Number:
  US06/505,696
• Time in Patent Office: 834 Days
• Field of Search: 424/1.1, 424/9, 424/16, 424/7.1, 424/85, 424/88, 424/94, 252/315.3
• US Class Current: 424/1.21
• CPC Class Codes: A61K 9/1271 Non-conventional liposomes, e.g. PEGylated liposomes, liposomes coated with polymers liposome as conjugate A61K47/6911
• CPC Class Codes: Y10S 424/812 Liposome comprising an antibody, antibody fragment, antigen, or other specific or nonspecific immunoeffector

Abstract

Phospholipid liposomes are provided having an outer layer including a cholesterol derivative such as a cholesterol ester and an aqueous medium confined by the layer which includes a tracer agent, a cytoxic agent or a therapeutic agent. The liposomes are adapted for specific organ targeting.

Claims

1. In a liposome formed by the incapsulation of an active agent by at least one lipid containing bilayer, the improvement comprising a ligand modified cholesterol compound in the lipid of said bilayer, said ligand being positioned at the 3 carbon position of said cholesterol, said ligand modified cholesterol compound rendering the liposome more specific for accumulation at a pre-selected organ in vivo.

2. The liposomes of claim 1 wherein said modified cholesterol is cholesterol butyrate.

3. The liposomes of claim 1 wherein said modified cholesterol is cholesterol phenylacetate.

4. The liposomes of any one of claims 1, 2 or 3 wherein said lipid bilayer includes a radioactive cation.

5. The liposomes of any one of claims 1, 2 or 3 wherein said lipid bilayer includes a fluorescent dye.

6. The liposomes of any one of claims 1, 2 or 3 wherein said lipid bilayer includes gaseous material.

7. The liposomes of any one of claims 1, 2 or 3 wherein said lipid bilayer includes a drug.

8. The liposomes of any one of claims 1, 2 or 3 wherein said lipid bilayer includes an enzyme.

9. The liposomes of any one of claims 1, 2 or 3 wherein said lipid bilayer includes metallic ions.

10. The liposomes of any one of claims 1, 2 or 3 wherein said lipid bilayer includes a magnetic compound.

11. The liposomes of any one of claims 1, 2 or 3 wherein said lipid bilayer includes genetic material.

12. The liposomes of any one of claims 1, 2 or 3 wherein said lipid bilayer includes an antigen or antibody.