Self forming, thermodynamically stable liposomes and their applications

• US 20070042032A1
• Filed: 10/24/2006
• Published: 02/22/2007
• Est. Priority Date: 12/20/2000
• Status: Active Grant

• Current Assignee: BioZone Laboratories, Incorporated (Ceba-Tech Specialty Solutions, Inc.)
• Original Assignee: BioZone Laboratories, Incorporated (Ceba-Tech Specialty Solutions, Inc.)
• Inventors: Keller, Brian, Lasic, Alenka, Lasic, Dan
• Granted Patent: US 7,718,190 B2
• Time in Patent Office: Days
• US Class Current: 424/450
• CPC Class Codes: A61K 9/127 Liposomes
• 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: A61K 9/1272 with substantial amounts of non-phosphatidyl, i.e. non-acylglycerophosphate, surfactants as bilayer-forming substances, e.g. cationic lipids with cholesterol as the only non-phosphatidyl surfactant A61K9/127; lipids as modifying agent A61K47/543
• CPC Class Codes: A61K 9/1277 Processes for preparing; Proliposomes
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: Y10T 428/2984 Microcapsule with fluid core [includes liposome]

Abstract

Certain diacylglycerol-polyethyleneglycol (DAG-PEG) lipids are especially useful for forming thermodynamically stable liposomes. Such liposomes are useful for a variety of purposes, including the delivery of therapeutic agents.

Claims

1. A liposome comprising one or more lipids

where one or more of the lipids is a diacylglycerol-polyethyleneglycol (PEG), selected from the group consisting of PEG-12 glycerol dioleate (GDO), PEG-12 glycerol dimyristate (GDM), PEG-23 glycerol dipalmitate-(GDP), PEG-12 glycerol distearate (GDS), and PEG-23 GDS, where the number after “

PEG”

indicates the numbers of C₂H₄O subunits in the PEG chain.

2. The liposome of claim 1 further comprising an active compound.

3. The liposome of claim 2, where the active compound is a protein, peptide, nucleic acid, agent for treating a neoplasm, agent for treating inflammation, agent for treating an infection, agent for treating a gasterointestinal disease, agent for treating an immunological disease, agent for treating a skin diseases or an eye disease, agent use in diagnosing disease, nutrient, agent for treating a blood disease, agent for treating a metabolic disease, agent for treating a cardiovascular disease, agent for treating a renal disease, agent for treating a genitourinary disease, agent for treating a respiratory disease or agent for treating a central nervous system disease.

4. A composition for the preparation of a liposome, said composition comprising:

an active compound; and

one or more lipids selected from the group consisting of PEG-12 GDO, PEG-12 GDM, PEG-23 GDP, PEG-12 GDS and PEG-23 GDS.

5. A method of preparing a liposome comprising combining an aqueous solution and a lipid solution, wherein the lipid solution comprises one or more of the lipids selected from the group consisting of PEG-12 glycerol dioleate (GDO), PEG-12 glycerol dimyristate (GDM), PEG-23 glycerol dipalmitate (GDP), PEG-12 glycerol distearate (GDS), and PEG-23 GDS, where the number after “

PEG”

indicates the numbers of C₂H₄O subunits in the PEG chain. the diacylglycerol-PEG lipid.

6. The method of claim 5 further comprising combining an active compound with the lipid solution and the aqueous solution.