EP0092453A2
Expired / Lapsed
EP
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Stable plurilamellar vesicles
Assignee: Elan Pharmaceuticals LLC
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Filing: 1983-03-29
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Granted: —
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Expires: 2003-03-29
Abstract
Abstract A new and substantially improved type of lipid vesicle, called stable plurilamellar vesicles (SPLVs), are described, as well as the process for making the same. SPLVs are stable during storage and can be used in vivo for the sustained release of compounds and in the treatment of disease.
Inventors
- 👤 Robert Parker Lenk
- 👤 Andrew Stuart Janoff
- 👤 Michael Wayne Fountain
- 👤 Marc Jeffrey Ostro
- 👤 Micrea Constantine Popescu
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-06 09:57
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/10; A61K9/127
Claims Analysis
Total Claims: 55
Claim 1
Independent Claim
3 words
Stable plurilamellar vesicles.
Claim 2
Dependent Claim
3 words
Stable plurilamellar vesicles.
Claim 3
Dependent Claim
10 words
Stable plurilamellar vesicles substantially free of MLVs, SUVs, and REVs.
Claim 4
Dependent Claim
10 words
Stable plurilamellar vesicles substantially free of MLVs, SUVs, and REVs.
Claim 5
Dependent Claim
25 words
Stable plurilamellar vesicles according to claim 1, having a lower buoyant density and a volume about one-third larger than MLVs, made from the same components.
Claim 6
Dependent Claim
25 words
Stable plurilamellar vesicles according to claim 1, which are more stable to auto-oxidation during storage in buffer than are MLVs, made from the same components.
Claim 7
Dependent Claim
25 words
Stable plurilamellar vesicles according to claim 1, which are more stable in body fluids than are MLVs, SUVs, and REVs made from the same components.
Claim 8
Dependent Claim
15 words
Stable plurilamellar vesicles according to claim 1, which release entrapped compounds when exposed to urea.
Claim 9
Dependent Claim
17 words
Stable plurilamellar vesicles according to claim 1, which, when administered in vivo, slowly release any entrapped compounds.
Claim 10
Dependent Claim
27 words
Stable plurilamellar vesicles according to claim 1, which, when administered to cells in culture, the contents of the vesicles are distributed throughout the cytosol of the cells.
Claim 11
Dependent Claim
32 words
Stable plurilamellar vesicles according to claim 1, which; when administered to cells in vivo, both the lipid and aqueous components of the vesicles are retained in the tissues and by the cells.
Claim 12
Dependent Claim
18 words
Stable plurilamellar vesicles according to claim 1, wherein the major lipid component of the vesicles is a phosphatidylcholine.
Claim 13
Dependent Claim
16 words
Stable plurilamellar vesicles according to claim 1, wherein an anti-oxidant is a component of the vesicle.
Claim 14
Dependent Claim
13 words
Stable plurilamellar vesicles according to claim 10 wherein said anti-oxidant is butylated hydroxytoluene.
Claim 15
Dependent Claim
15 words
Stable plurilamellar vesicles according to claim 1, wherein a protein is entrapped within the vesicle.
Claim 16
Dependent Claim
30 words
Stable plurilamellar vesicles according to claim 1, wherein a compound selected from the group consisting of: antibacterial compounds, antifungal compounds, antiparasitic compounds, and antiviral compounds is entrapped within the vesicle.
Claim 17
Dependent Claim
30 words
Stable plurilamellar vesicles according to claim 1, wherein a compound selected from the group consisting of: tumoricidal compounds, toxins, cell receptor binding molecules, and immunoglobulins is entrapped within the vesicle.
Claim 18
Dependent Claim
30 words
Stable plurilamellar vesicles according to claim 1, wherein a compound selected from the group consisting of: anti-inflammatory compounds, anti-glaucoma compounds, mydriatic compounds, and local anesthetics is entrapped within the vesicle.
Claim 19
Dependent Claim
30 words
Stable plurilamellar vesicles according to claim 1, wherein a compound selected from the group consisting of: enzymes, hormones, neurotransmitters, immunomodulators, nucleotides, and cyclic adenosine monophosphate is entrapped within the vesicle.
Claim 20
Dependent Claim
29 words
Stable plurilamellar vesicles according to claim 1, wherein a compound selected from the group consisting of: dyes, fluorescent compounds, radioactive compounds, and radio-opaque compounds is entrapped within the vesicle.
Claim 21
Independent Claim
77 words
A method for preparing stable plurilamellar vesicles, comprising: (a) forming a dispersion of at least one amphipathic lipid in an organic solvent; (b) combining the dispersion with a sufficient amount of an aqueous phase to form a biphasic mixture in which the aqueous phase can be completely emulsified; and (c) emulsifying the aqueous phase and evaporating the organic solvent of the biphasic mixtures, wherein the stable plurilamellar vesicles produced are substantially free of MLVs, SUVs, and REVs.
Claim 22
Independent Claim
77 words
A method for preparing stable plurilamellar vesicles, comprising: (a) forming a dispersion of at least one amphipathic lipid in an organic solvent; (b) combining the dispersion with a sufficient amount of an aqueous phase to form a biphasic mixture in which the aqueous phase can be completely emulsified; and (c) emulsifying the aqueous phase and evaporating the organic solvent of the biphasic mixtures, wherein the stable plurilamellar vesicles produced are substantially free of MLVs, SUVs, and REVs.
Claim 23
Dependent Claim
25 words
The method according to claim 19, wherein the ratio of volume of solvent to volume of aqueous phase is from about 3:1 to about 100:1.
Claim 24
Dependent Claim
22 words
The method according to claim 19, wherein the temperature at which the method is performed is from about 4°C to about 60°C.
Claim 25
Independent Claim
29 words
The method according to cla·m 19, wherein the temperature at which the method is performed is less than the phase transition temperature of at least one of said lipids.
Claim 26
Independent Claim
29 words
The method according to cla·m 19, wherein the temperature at which the method is performed is less than the phase transition temperature of at least one of said lipids.
Claim 27
Dependent Claim
16 words
The method according to claim 19, wherein the solvent is fluorocarbon or diethylether, or mixtures thereof.
Claim 28
Dependent Claim
12 words
The method according to claim 23 wherein the solvent contains an anti-oxidant.
Claim 29
Dependent Claim
12 words
The method according to claim 24, wherein said anti-oxidant is butylated hydroxytoluene.
Claim 30
Dependent Claim
14 words
The method according to claim 19, wherein the emulsification is performed before the evaporation.
Claim 31
Dependent Claim
15 words
The method according to claim 19, wherein the emulsification is performed simultaneously with the evaporation.
Claim 32
Dependent Claim
21 words
The method according to claim 19, wherein a material to be entrapped in the vesicles is added with the aqueous phase.
Claim 33
Dependent Claim
19 words
The method according to claim 28, wherein at least 20 percent of said material is entrapped in the vesicles.
Claim 34
Dependent Claim
12 words
The method according to claim 28, wherein said material is a protein.
Claim 35
Dependent Claim
28 words
A composition for delivery of a compound to cells in vivo, comprising stable plurilamellar vesicles according to one of claims 1 to 17 containing said compound entrapped therein.
Claim 36
Dependent Claim
17 words
The composition according to claim 31, suitable to be administered topically, intraperitoneally, intravenously, intramuscularly, subcutaneously or intraauricularly.
Claim 37
Dependent Claim
30 words
A composition for treatment of infections in animals or plants, comprising stable plurilamellar vesicles according to one of claims 1 to 17 containing a compound effective for treating said infection.
Claim 38
Dependent Claim
13 words
The composition according to claim 33, wherein said infection is an intracellular infection.
Claim 39
Dependent Claim
14 words
The composition according to claim 34 wherein said infection is caused by a parasite.
Claim 40
Dependent Claim
14 words
The composition according to claim 35, wherein said infection is caused by Brucella spp.
Claim 41
Dependent Claim
11 words
The composition according to claim 36, suitable to be administered intraperitoneally.
Claim 42
Dependent Claim
11 words
The composition according to claim 33, wherein said infection is extracellular.
Claim 43
Dependent Claim
13 words
The composition according to claim 38, wherein said infection is caused by Bacteria.
Claim 44
Dependent Claim
14 words
The composition according to claim 39, wherein said infection is caused by Staphylococcus aureus.
Claim 45
Dependent Claim
11 words
The composition according to claim 40, suitable to be administered intraperitoneally.
Claim 46
Dependent Claim
13 words
The composition according to claim 33, wherein said infection is an ocular infection.
Claim 47
Dependent Claim
15 words
The composition according to claim 42, wherein said infection is caused by a Moraxella spp.
Claim 48
Dependent Claim
11 words
The composition according to claim 43, suitable to be administrated topically.
Claim 49
Dependent Claim
14 words
The composition according to claim 33, wherein said infection is caused by a virus.
Claim 50
Dependent Claim
15 words
The composition according to claim 45, wherein said infection is caused by lymphocytic choriomeningitis virus.
Claim 51
Dependent Claim
11 words
The composition according to claim 46, suitable to be administrated intraperitoneally.
Claim 52
Dependent Claim
36 words
A composition for treatment of afflictions in animals or plants requiring sustained release of a compound effective for treating said affliction, comprising stable plurilamellar vesicles according to one of claims 1 to 17 containing said compound.
Claim 53
Dependent Claim
13 words
The composition according to claim 48, wherein said affliction is an ocular affliction.
Claim 54
Dependent Claim
11 words
A composition according to claim 49, wherein said affliction is glaucoma.
Claim 55
Dependent Claim
11 words
The composition according to claim 50, suitable to be administrated topically.
References Cited (Backward Citations)
No citation records indexed.
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