US4853228A
Expired / Lapsed
US
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Method of manufacturing unilamellar lipid vesicles
Assignee: IGEN Inc A DE CORP
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Filing: 1987-07-28
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Granted: 1989-08-01
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Expires: 2007-07-28
Abstract
Abstract Disclosed is a new type of unilamellar lipid vesicle made from polyoxyethylene acyl ethers or sorbitan alkyl esters. These unilamellar vesicles are made with easily obtained, relatively inexpensive materials and the vesicles are more stable then conventional unilamellar lipid vesicles. A delivery system for drugs or other molecules is also disclosed.
Inventors
- 👤 Donald F. H. Wallach
- 👤 Jean Philippot
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 20:04
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/10; A61K9/127; A61K9/1271; A61K9/1272; Y; Y10; Y10S; Y10S436/00; Y10S436/829
Claims Analysis
Total Claims: 25
Claim 1
Independent Claim
93 words
A large unilamellar vesicle comprising a surfactant selected from a group consisting of polyoxyethylene alkyl ethers having the structure R.sub.1 --O--(CH.sub.2 --CH.sub.2 --O--).sub.m --H wherein R 1 is CH 3 --(CH 2 ) n , n ranges from 11 to 15, and m ranges from 2 to 4 and sorbitan alkyl esters having the structure ##STR3## wherein R 2 is CH 3 --(CH 2 ) x and x ranges from 11 to 15 and a sterol, whereby said surfactant comprises substantially all the lipid in the structure of said large unilamellar lipid vesicle.
Claim 2
Dependent Claim
93 words
A large unilamellar vesicle comprising a surfactant selected from a group consisting of polyoxyethylene alkyl ethers having the structure R.sub.1 --O--(CH.sub.2 --CH.sub.2 --O--).sub.m --H wherein R 1 is CH 3 --(CH 2 ) n , n ranges from 11 to 15, and m ranges from 2 to 4 and sorbitan alkyl esters having the structure ##STR3## wherein R 2 is CH 3 --(CH 2 ) x and x ranges from 11 to 15 and a sterol, whereby said surfactant comprises substantially all the lipid in the structure of said large unilamellar lipid vesicle.
Claim 3
Dependent Claim
17 words
The large unilamellar vesicle of claim 1 wherein said polyoxyethylene alkyl ether comprises polyoxyethylene (2) cetyl ether.
Claim 4
Dependent Claim
17 words
The large unilamellar vesicle of claim 1 wherein said polyoxyethylene alkyl ether comprises polyoxyethylene (4) lauryl ether.
Claim 5
Dependent Claim
24 words
The large unilamellar vesicle of claim 1 wherein said sterol is selected from a group consisting of cholesterol, its chemical analogs, and its derivatives.
Claim 6
Dependent Claim
12 words
The large unilamellar vesicle of claim 4 further comprising a charge-producing amphiphile.
Claim 7
Dependent Claim
32 words
The large unilamellar vesicle of claim 5 wherein said amphiphile is a negative charge-producing material selected from a group consisting of dicetyl phosphate, cetyl sulphate, phosphatydic acid, phosphatidyl serine, and mixtures thereof.
Claim 8
Dependent Claim
30 words
The large unilamellar vesicle of claim 5 wherein said amphiphile is a positive charge-producing material selected from a group consisting of long chain amines, quaternary ammonium compounds, and mixtures thereof.
Claim 9
Dependent Claim
13 words
The large unilamellar vesicle of claim 1 further comprising a hydrophilic targeting molecule.
Claim 10
Dependent Claim
24 words
The large unilamellar vesicle of claim 8 wherein said hydrophilic targeting molecule is selected from a group consisting of immunoglobulins, lectins, and peptide hormones.
Claim 11
Dependent Claim
15 words
The large unilamellar vesicle of claim 1 wherein said sorbitan alkyl ester comprises sorbitan laurate.
Claim 12
Dependent Claim
15 words
The large unilamellar vesicle of claim 1 wherein said sorbitan alkyl ester comprises sorbitan monopalmitate.
Claim 13
Dependent Claim
122 words
A delivery system for a hydrophilic material, said system consisting of a large unilamellar vesicle having a lipid bilayer surrounding a subtantially aqueous interior, said lipid bilayer comprising a nonphospholipid surfactant, a sterol, a targeting molecule, and a charge-producing amphiphile, said surfactant being selected from a group consisting of polyoxyethylene alkyl ethers having the structure R.sub.1 --O--(CH.sub.2 --CH.sub.2 --O--).sub.m --H wherein R 1 is CH 3 --(CH 2 ) n , n ranges from 11 to 15, and m ranges from 2 to 4, and sorbitan alkyl esters having the structure ##STR4## wherein R 2 is CH 3 --(CH 2 ) x and x ranges from 11 to 15 said surfactant comprising substantially all the lipid in the structure of said vesicle.
Claim 14
Dependent Claim
122 words
A delivery system for a hydrophilic material, said system consisting of a large unilamellar vesicle having a lipid bilayer surrounding a subtantially aqueous interior, said lipid bilayer comprising a nonphospholipid surfactant, a sterol, a targeting molecule, and a charge-producing amphiphile, said surfactant being selected from a group consisting of polyoxyethylene alkyl ethers having the structure R.sub.1 --O--(CH.sub.2 --CH.sub.2 --O--).sub.m --H wherein R 1 is CH 3 --(CH 2 ) n , n ranges from 11 to 15, and m ranges from 2 to 4, and sorbitan alkyl esters having the structure ##STR4## wherein R 2 is CH 3 --(CH 2 ) x and x ranges from 11 to 15 said surfactant comprising substantially all the lipid in the structure of said vesicle.
Claim 15
Dependent Claim
15 words
The delivery system of claim 12 wherein said polyoxyethylene alkyl ether comprises polyoxyethylene 2-cetyl ether.
Claim 16
Dependent Claim
16 words
The delivery system of claim 12 wherein said polyoxyethylene alkyl ether comprises polyoxyethylene (4) lauryl ether.
Claim 17
Dependent Claim
14 words
The delivery system of claim 12 wherein said sorbitan alkyl ester comprises sorbitan laurate.
Claim 18
Dependent Claim
14 words
The delivery system of claim 12 wherein said sorbitan alkyl ester comprises sorbitan monopalmitate.
Claim 19
Dependent Claim
14 words
The delivery system of claim 12 wherein said sterol comprises cholesterol or its derivatives.
Claim 20
Dependent Claim
31 words
The delivery system of claim 12 wherein said amphiphile is a negative charge-producing material selected from a group consisting of dicetyl phosphate, cetyl sulphate, phosphatydic acid, phosphatidyl serine, and mixtures thereof.
Claim 21
Dependent Claim
29 words
The delivery system of claim 12 wherein said amphiphile is a positive charge-producing material selected from a group consisting of long chain amines, quaternary ammonium compounds, and mixtures thereof.
Claim 22
Dependent Claim
15 words
The delivery system of claim 12 wherein said target molecule comprises a hydrophilic targeting molecule.
Claim 23
Dependent Claim
23 words
The delivery system of claim 20 wherein said hydrophilic targeting molecule is selected from a group consisting of immunoglobulins, lectins, and peptide hormones.
Claim 24
Dependent Claim
61 words
The delivery system of claim 12 wherein said hydrophilic material is enclosed within said lipid bilayer, said lipid bilayer comprising: approximately 46-48 parts of said surfactant; approximately 46-48 parts of a sterol selected from the group consisting of cholesterol, its chemical analogs, and its derivatives; approximately 4-8 parts of a charge-producing amphiphile; and less than one part of a targeting molecule.
Claim 25
Dependent Claim
33 words
The delivery system of claim 22 wherein said hydrophilic material is selected from the group consisting of nucleic acids, immunological adjuvants, enzymes, hormones, lymphokines, blood proteins, pesticides, contrast dyes, and radioactive marker molecules.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
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| 3.5 Years (Year 4) | 1992-07-31 | 1993-01-30 | 1993-08-01 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-07-31 | 1997-01-30 | 1997-08-01 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-07-31 | 2001-01-30 | 2001-08-01 | $7700.00 | Window Closed / Lapsed |