US4721612A
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Steroidal liposomes
Assignee: Elan Pharmaceuticals LLC
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Filing: 1985-04-10
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Granted: 1988-01-26
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Expires: 2005-04-10
Abstract
Abstract Methods and compositions are described for the preparation of lipid vesicles, the bilayers of which comprise a salt form of an organic acid derivative of a sterol such as the tris-salt form of a sterol hemisuccinate. The method is rapid, efficient, and does not require the use of organic solvents. The sterol hemisuccinate vesicles may be used to entrap compounds which are insoluble in aqueous solutions. Such preparations are especially useful for entrapping bioactive agents of limited solubility thus enabling administration in vivo.
Inventors
- 👤 Andrew S. Janoff
- 👤 Mircea C. Popescu
- 👤 Alan L. Weiner
- 👤 Lois E. Bolcsak
- 👤 Paul S. Tremblay
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 11:10
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/10; A61K9/127; A61K9/1271; A61K9/1272; A61K39/00; A61K2039/555; A61K2039/55511; A61K2039/55555; Y; Y10; Y10S; Y10S436/00; Y10S436/829; Y10T; Y10T428/00; Y10T428/29; Y10T428/2982; Y10T428/2984; Y10T436/00; Y10T436/11; Y10T436/117497
Claims Analysis
Total Claims: 59
Claim 1
Independent Claim
35 words
A method for administering a compound in vivo comprising, administering to a host the compound entrapped in a liposome, the bilayers of which comprise a salt form of an organic acid derivative of a sterol.
Claim 2
Independent Claim
35 words
A method for administering a compound in vivo comprising, administering to a host the compound entrapped in a liposome, the bilayers of which comprise a salt form of an organic acid derivative of a sterol.
Claim 3
Dependent Claim
13 words
The method according to claim 1 in which the liposomes comprise multilamellar vesicles.
Claim 4
Dependent Claim
13 words
The method according to claim 1 in which the liposomes comprise unilamellar vesicles.
Claim 5
Dependent Claim
24 words
The method according to claim 1 in which the bilayers comprise a tris(hydroxymethyl) aminomethane salt form of an organic acid derivative of a sterol.
Claim 6
Dependent Claim
45 words
The method according to claim 1 in which the bilayers comprise a salt form of a carboxylic acid derivative of a sterol, a salt form of a dicarboxylic acid derivative of a sterol, or a salt form of a polycarboxylic acid derivative of a sterol.
Claim 7
Dependent Claim
16 words
The method according to claim 5 in which the carboxylic acid comprises an aliphatic carboxylic acid.
Claim 8
Dependent Claim
18 words
The method according to claim 6 in which the aliphatic carboxylic acid contains up to five carbon atoms.
Claim 9
Dependent Claim
16 words
The method according to claim 5 in which the dicarboxylic acid comprises an aliphatic dicarboxylic acid.
Claim 10
Dependent Claim
18 words
The method according to claim 8 in which the aliphatic dicarboxylic acid contains up to seven carbon atoms.
Claim 11
Dependent Claim
14 words
The method according to claim 9 in which the aliphatic dicarboxylic acid is succinate.
Claim 12
Dependent Claim
22 words
The method according to claim 1 in which the bilayers comprise a salt form of an hydroxy acid derivative of a sterol.
Claim 13
Dependent Claim
16 words
The method according to claim 11 in which the hydroxy acid comprises an a hydroxy acid.
Claim 14
Dependent Claim
34 words
The method according to claim 1 in which the bilayers comprise a salt form of an amino acid derivative of a sterol or a salt form of a polyamino acid derivative of a sterol.
Claim 15
Dependent Claim
22 words
The method according to claim 1 in which the bilayers comprise a salt form of an organic acid derivative of a cholesterol.
Claim 16
Dependent Claim
13 words
The method according to claim 14 in which the liposomes comprise multilamellar vesicles.
Claim 17
Dependent Claim
13 words
The method according to claim 14 in which the liposomes comprise unilamellar vesicles.
Claim 18
Dependent Claim
23 words
The method according to claim 1 in which the bilayers comprise a salt form of an organic acid derivative of a vitamin D.
Claim 19
Dependent Claim
22 words
The method according to claim 1 in which the bilayers comprise a salt form of an organic acid derivative of a phytosterol.
Claim 20
Dependent Claim
23 words
The method according to claim 1 in which the bilayers comprise a salt form of an organic acid derivative of a steroid hormone.
Claim 21
Dependent Claim
21 words
The method according to claim 1 in which the bilayers comprise the tris(hydroxymethyl)aminomethane salt form of a hemisuccinate derivative of cholesterol.
Claim 22
Dependent Claim
13 words
The method according to claim 20 in which the liposomes comprise multilamellar vesicles.
Claim 23
Dependent Claim
13 words
The method according to claim 20 in which the liposomes comprise unilamellar vesicles.
Claim 24
Dependent Claim
27 words
The method according to claim 1 or 20 in which the bioactive agent is selected from the group consisting of: dyes, radiolabels, radio-opaque compounds, and fluorescent compounds.
Claim 25
Dependent Claim
16 words
The method according to claim 1 or 20 in which the compound comprises a bioactive agent.
Claim 26
Dependent Claim
24 words
The method according to claim 24 in which the bioactive agent is selected from the group consisting of: antibacterial, antifungal, antiviral, and antiparasitic compounds.
Claim 27
Dependent Claim
14 words
The method according to claim 24 in which the bioactive agent compound is tylosin.
Claim 28
Dependent Claim
14 words
The method according to claim 24 in which the bioactive agent compound is miconazole.
Claim 29
Dependent Claim
17 words
The method according to claim 24 in which the bioactive agent comprises a cell receptor binding compound.
Claim 30
Dependent Claim
26 words
The method according to claim 24 in which the bioactive agent is selected from the group consisting of: hormones, neurotransmitters, tumoricidal compounds, growth factors, and toxins.
Claim 31
Dependent Claim
13 words
The method according to claim 29 in which the bioactive agent comprises insulin.
Claim 32
Dependent Claim
14 words
The method according to claim 24 in which the bioactive agent comprises growth hormone.
Claim 33
Dependent Claim
15 words
The method according to claim 31 in which the growth hormone comprises bovine growth hormone.
Claim 34
Dependent Claim
15 words
The method according to claim 31 in which the growth hormone comprises human growth hormone.
Claim 35
Dependent Claim
23 words
The method according to claim 24 in which the bioactive agent is selected from the group consisting of: peptides, proteins, glycoproteins, and lipoproteins.
Claim 36
Dependent Claim
14 words
The method according to claim 34 in which the bioactive agent is an immunoglobulin.
Claim 37
Dependent Claim
15 words
The method according to claim 24 in which the bioactive agent comprises an immunomodulating compound.
Claim 38
Dependent Claim
20 words
The method according to claim 24 in which the compound is selected from the group consisting of catalysts and enzymes.
Claim 39
Dependent Claim
14 words
The method according to claim 24 in which the bioactive agent is arsenazo III.
Claim 40
Dependent Claim
25 words
The method according to claim 24 in which the bioactive agent is selected from the group consisting of: anti-inflammatory, antiglaucomic, mydriatic, analgesic and anesthetic compounds.
Claim 41
Dependent Claim
13 words
The method according to claim 24 in which the bioactive agent comprises indomethacin.
Claim 42
Dependent Claim
14 words
The method according to claim 24 in which the bioactive agent comprises a narcotic.
Claim 43
Dependent Claim
17 words
The method according to claim 24 in which the bioactive agent comprises a psychoactive or anxiolytic agent.
Claim 44
Dependent Claim
13 words
The method according to claim 42 in which the bioactive agent comprises diazepam.
Claim 45
Dependent Claim
14 words
The method according to claim 24 in which the bioactive agent comprises a vitamin.
Claim 46
Dependent Claim
12 words
The method according to claim 44 in which the vitamin comprises α-tocopherol.
Claim 47
Dependent Claim
22 words
The method according to claim 24 in which the bioactive agent is selected from the group consisting of: monosaccharides, disaccharides, and polysaccharides.
Claim 48
Dependent Claim
17 words
The method according to claim 24 in which the route of administration is intravenous, intraparitoneal, or intramuscular.
Claim 49
Dependent Claim
18 words
Steroidal liposomes comprising completely closed bilayers comprising a salt form of an organic acid derivative of a sterol.
Claim 50
Dependent Claim
18 words
Steroidal liposomes comprising completely closed bilayers comprising a salt form of an organic acid derivative of a sterol.
Claim 51
Dependent Claim
13 words
Steroidal liposomes according to claim 48 in which the liposomes comprise multilamellar vesicles.
Claim 52
Dependent Claim
13 words
Steroidal liposomes according to claim 48 in which the liposomes comprise unilamellar vesicles.
Claim 53
Dependent Claim
23 words
Steroidal liposomes according to claim 48 in which the bilayers comprise a tris(hydroxymethyl)aminomethane salt form of an organic acid derivative of a sterol.
Claim 54
Dependent Claim
26 words
Steroidal liposomes according to claim 48 in which the bilayers comprise a 2-amino-2-methyl-1,3-propanediol, 2-aminoethanol or bis-tris-propane salt form of an organic acid derivative of a sterol.
Claim 55
Dependent Claim
17 words
Steroidal liposomes according to claim 48 in which the salt is derived from an ionizable bioactive agent.
Claim 56
Dependent Claim
14 words
Steroidal liposomes according to claim 53 in which the ionizable bioactive agent is miconazole.
Claim 57
Dependent Claim
44 words
Steroidal liposomes according to claim 48 in which the bilayers comprise a salt form of a carboxylic acid derivative of a sterol, a salt form of a dicarboxylic acid of a sterol, or a salt form of a polycarboxylic acid derivative of a sterol.
Claim 58
Dependent Claim
21 words
Steroidal liposomes according to claim 48 in which the bilayers comprise a salt form of an organic acid derivative of cholesterol.
Claim 59
Dependent Claim
21 words
Steroidal liposomes according to claim 48 in which the bilayers comprise a tris(hydroxymethyl)aminomethane salt form of a hemisuccinate derivative of cholesterol.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1991-01-25 | 1991-07-27 | 1992-01-26 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1995-01-25 | 1995-07-27 | 1996-01-26 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1999-01-25 | 1999-07-27 | 2000-01-26 | $7700.00 | Window Closed / Lapsed |