Patent US5032457A successfully refreshed from Google Patents.
US5032457A
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Paucilamellar lipid vesicles using charge-localized, single chain, nonphospholipid surfactants
Assignee: Novavax Inc
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Filing: 1989-09-21
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Granted: 1991-07-16
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Expires: 2009-09-21
Abstract
Abstract Disclosed are paucilamellar lipid vesicles made of single chain nonphospholipid anionic or zwitterionic surfactants and a method of their manufacture. The preferred vesicle forming materials are single chain sarcosinamides having 12-20 carbon chains and single chain betaines. The vesicles are formed rapidly and can be used to encapsulate aqueous or oily solutions.
Inventors
- 👤 Donald F. H. Wallach
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-07 23:19
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/10; A61K9/127; A61K9/1271; A61K9/1272; A61K9/1277; C; C11; C11D; C11D17/00; C11D17/0008; C11D17/0017; C11D17/0021; C11D17/0026; Y; Y10; Y10S; Y10S436/00; Y10S436/829; Y10T; Y10T428/00; Y10T428/29; Y10T428/2982; Y10T428/2984
Claims Analysis
Total Claims: 36
Claim 1
Independent Claim
106 words
A method of preparing aqueous-filled, paucilamellar lipid vesicles consisting essentially of the steps of: A. Providing a solventless nonaqueous lipophilic phase comprising a single chain charge-localized nonphospholipid surfactant selected from the group consisting of betaines and anionic sarcosinamides and any lipid-soluble materials to be incorporated in said lipid vesicle; B. Providing an aqueous phase formed of an aqueous solvent and any aqueous soluble materials to be encapsulated; and C. Combining said nonaqueous lipophilic phase with a substantial excess of said aqueous phase in a single step under shear mixing conditions; whereby said aqueous-filled paucilamellar lipid vesicles are formed without the formation of a separable lamellar phase.
Claim 2
Independent Claim
106 words
A method of preparing aqueous-filled, paucilamellar lipid vesicles consisting essentially of the steps of: A. Providing a solventless nonaqueous lipophilic phase comprising a single chain charge-localized nonphospholipid surfactant selected from the group consisting of betaines and anionic sarcosinamides and any lipid-soluble materials to be incorporated in said lipid vesicle; B. Providing an aqueous phase formed of an aqueous solvent and any aqueous soluble materials to be encapsulated; and C. Combining said nonaqueous lipophilic phase with a substantial excess of said aqueous phase in a single step under shear mixing conditions; whereby said aqueous-filled paucilamellar lipid vesicles are formed without the formation of a separable lamellar phase.
Claim 3
Dependent Claim
25 words
The method of claim 1 wherein said betaine comprises a betaine having the structure: ##STR5## where R 2 is a long chain fatty acid ester.
Claim 4
Dependent Claim
15 words
The method of claim 2 wherein R 2 is propyl oleate, having the structure ##STR6##
Claim 5
Dependent Claim
33 words
The method of claim 1 wherein said sarcosinamide comprises a sarcosinamide having the structure ##STR7## where ##STR8## is the carbonyl derivative of a long chain fatty acid having 12 to 20 carbon atoms.
Claim 6
Dependent Claim
26 words
The method of claim 4 where R 1 is selected from the group consisting of lauric acid, fatty acids having 14-20 carbon atoms, and mixtures thereof.
Claim 7
Dependent Claim
13 words
The method of claim 1 wherein said lipophilic phase further comprises a sterol.
Claim 8
Dependent Claim
10 words
The method of claim 6 wherein said sterol comprises cholesterol.
Claim 9
Dependent Claim
14 words
The method of claim 1 wherein said lipophilic phase further comprises a charge-producing amphiphile.
Claim 10
Independent Claim
165 words
The method of preparing oil-filled paucilamellar lipid vesicles having a water-immiscible oily material in their amorphous central cavities consisting essentially of the steps of: A. Providing a nonaqueous lipophilic phase comprising a charge-localized single chain nonphospholipid surfactant selected from the group consisting of betaines and anionic sarcosinamides and any lipid-soluble materials to be incorporated in said lipid vesicles; B. Providing an aqueous phase formed of an aqueous solvent and any aqueous soluble materials to be incorporated in said lipid vesicles; and C. Providing an oil phase of a water-immiscible oily material and any oil-dispersible material to be incorporated in said lipid vesicles; D. Blending said lipid phase and said oil phase to form a lipid-oil phase; E. Combining said lipid-oil phase with a substantial excess of said aqueous phase in a single step under shear mixing conditions; whereby said single chain charge-localized nonphospholipid paucilamellar lipid vesicles having a water-immiscible oily material in their central cavities are formed without the formation of a separable lamellar phase.
Claim 11
Independent Claim
165 words
The method of preparing oil-filled paucilamellar lipid vesicles having a water-immiscible oily material in their amorphous central cavities consisting essentially of the steps of: A. Providing a nonaqueous lipophilic phase comprising a charge-localized single chain nonphospholipid surfactant selected from the group consisting of betaines and anionic sarcosinamides and any lipid-soluble materials to be incorporated in said lipid vesicles; B. Providing an aqueous phase formed of an aqueous solvent and any aqueous soluble materials to be incorporated in said lipid vesicles; and C. Providing an oil phase of a water-immiscible oily material and any oil-dispersible material to be incorporated in said lipid vesicles; D. Blending said lipid phase and said oil phase to form a lipid-oil phase; E. Combining said lipid-oil phase with a substantial excess of said aqueous phase in a single step under shear mixing conditions; whereby said single chain charge-localized nonphospholipid paucilamellar lipid vesicles having a water-immiscible oily material in their central cavities are formed without the formation of a separable lamellar phase.
Claim 12
Dependent Claim
25 words
The method of claim 9 wherein said betaine comprises a betaine having the structure: ##STR9## where R 2 is a long chain fatty acid ester.
Claim 13
Dependent Claim
15 words
The method of claim 10 wherein R 2 is propyl oleate, having the structure ##STR10##
Claim 14
Dependent Claim
33 words
The method of claim 9 wherein said sarcosinamide comprises a sarcosinamide having the structure ##STR11## where ##STR12## is the carbonyl derivative of a long chain fatty acid having 12 to 20 carbon atoms.
Claim 15
Dependent Claim
26 words
The method of claim 12 where R 1 is selected from the group consisting of lauric acid, fatty acids having 14-20 carbon atoms, and mixtures thereof.
Claim 16
Dependent Claim
13 words
The method of claim 9 wherein said lipophilic phase further comprises a sterol.
Claim 17
Dependent Claim
10 words
The method of claim 14 wherein said sterol comprises cholesterol.
Claim 18
Dependent Claim
14 words
The method of claim 9 wherein said lipophilic phase further comprises a charge-producing amphiphile.
Claim 19
Dependent Claim
56 words
Aqueous-filled paucilamellar lipid vesicles consisting of 2-10 lipid bilayers in the form of substantially spherical shells separated by aqueous layers, said lipid bilayers comprising a charge-localized single chain nonphospholipid surfactant selected from the group consisting of betaines and anionic sarcosinamides as the primary lipid, and any lipid-soluble materials to be incorporated in said lipid vesicle bilayers.
Claim 20
Dependent Claim
56 words
Aqueous-filled paucilamellar lipid vesicles consisting of 2-10 lipid bilayers in the form of substantially spherical shells separated by aqueous layers, said lipid bilayers comprising a charge-localized single chain nonphospholipid surfactant selected from the group consisting of betaines and anionic sarcosinamides as the primary lipid, and any lipid-soluble materials to be incorporated in said lipid vesicle bilayers.
Claim 21
Dependent Claim
27 words
The paucilamellar lipid vesicles of claim 12 wherein said betaine comprises a betaine having the structure: ##STR13## where R 2 is a long chain fatty acid ester.
Claim 22
Dependent Claim
17 words
The paucilamellar lipid vesicles of claim 18 wherein R 2 is propyl oleate, having the structure ##STR14##
Claim 23
Dependent Claim
35 words
The paucilamellar lipid vesicles of claim 17 wherein said sarcosinamide comprises a sarcosinamide having the structure ##STR15## where ##STR16## is the carbonyl derivative of a long chain fatty acid having 12 to 20 carbon atoms.
Claim 24
Dependent Claim
28 words
The paucilamellar lipid vesicles of claim 20 where R 1 is selected from the group consisting of lauric acid, fatty acids having 14-20 carbon atoms, and mixtures thereof.
Claim 25
Dependent Claim
15 words
The paucilamellar lipid vesicles of claim 17 wherein said lipophilic phase further comprises a sterol.
Claim 26
Dependent Claim
12 words
The paucilamellar lipid vesicles of claim 22 wherein said sterol comprises cholesterol.
Claim 27
Dependent Claim
16 words
The paucilamellar lipid vesicles of claim 17 wherein said lipophilic phase further comprises a charge-producing amphiphile.
Claim 28
Dependent Claim
66 words
Oil-filled paucilamellar lipid vesicles consisting of 2-10 lipid bilayers in the form of substantially spherical shells separated by aqueous layers, said lipid bilayers surrounding a substantially oil-filled amorphous central cavity, said lipid bilayers comprising a charge-localized single chain nonphospholipid surfactant selected from the group consisting of betaines and anionic sarcosinamides as the primary lipid, and any lipid-soluble materials to be incorporated in said lipid vesicle bilayers.
Claim 29
Dependent Claim
66 words
Oil-filled paucilamellar lipid vesicles consisting of 2-10 lipid bilayers in the form of substantially spherical shells separated by aqueous layers, said lipid bilayers surrounding a substantially oil-filled amorphous central cavity, said lipid bilayers comprising a charge-localized single chain nonphospholipid surfactant selected from the group consisting of betaines and anionic sarcosinamides as the primary lipid, and any lipid-soluble materials to be incorporated in said lipid vesicle bilayers.
Claim 30
Dependent Claim
27 words
The paucilamellar lipid vesicles of claim 25 wherein said betaine comprises a betaine having the structure: ##STR17## where R 2 is a long chain fatty acid ester.
Claim 31
Dependent Claim
17 words
The paucilamellar lipid vesicles of claim 26 wherein R 2 is propyl oleate, having the structure ##STR18##
Claim 32
Dependent Claim
36 words
The paucilamellar lipid vesicles of claim 25 wherein said anionic sarcosinamide comprises a sarcosinamide having the structure ##STR19## where ##STR20## is the carbonyl group of a long chain fatty acid having 12 to 20 carbon atoms.
Claim 33
Dependent Claim
28 words
The paucilamellar lipid vesicles of claim 28 where R 1 is selected from the group consisting of lauric acid, fatty acids having 14-20 carbon atoms, and mixtures thereof.
Claim 34
Dependent Claim
15 words
The paucilamellar lipid vesicles of claim 25 wherein said lipophilic phase further comprises a sterol.
Claim 35
Dependent Claim
12 words
The paucilamellar lipid vesicles of claim 30 wherein said sterol comprises cholesterol.
Claim 36
Dependent Claim
16 words
The paucilamellar lipid vesicles of claim 25 wherein said lipophilic phase further comprises a charge-producing amphiphile.
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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) | 1994-07-15 | 1995-01-14 | 1995-07-16 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1998-07-15 | 1999-01-14 | 1999-07-16 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2002-07-15 | 2003-01-14 | 2003-07-16 | $7700.00 | Window Closed / Lapsed |