IPC분류정보
국가/구분 |
United States(US) Patent
등록
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국제특허분류(IPC7판) |
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출원번호 |
US-0165501
(2002-06-07)
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발명자
/ 주소 |
- Melchior,Donald L.
- Carruthers,Anthony
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출원인 / 주소 |
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대리인 / 주소 |
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인용정보 |
피인용 횟수 :
2 인용 특허 :
9 |
초록
▼
This invention features in vitro methods of determining the rate and extent to which test compounds, such as drug candidates, enter, move within, and traverse lipid-associated barriers. This invention also features method that measure the accumulation, that is the partition coefficient, of test comp
This invention features in vitro methods of determining the rate and extent to which test compounds, such as drug candidates, enter, move within, and traverse lipid-associated barriers. This invention also features method that measure the accumulation, that is the partition coefficient, of test compounds in lipid structures relative to, e.g., an aqueous phase, as well as the rate of accumulation of test compounds in the lipid structures. In addition, the invention features lipid vesicles that contain fluorophores localized within the aqueous interior that can be employed in the methods described herein.
대표청구항
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The invention claimed is: 1. A vesicle comprising: (a) a lipid bilayer enclosing an aqueous interior; and (b) a fluorescent molecule comprising a fluorophore covalently bound to a water-soluble or water-suspendable carrier, wherein said fluorescent molecule is disposed in the aqueous interior enclo
The invention claimed is: 1. A vesicle comprising: (a) a lipid bilayer enclosing an aqueous interior; and (b) a fluorescent molecule comprising a fluorophore covalently bound to a water-soluble or water-suspendable carrier, wherein said fluorescent molecule is disposed in the aqueous interior enclosed by said lipid bilayer of said vesicle, wherein said carrier prevents said fluorophore from traversing said lipid bilayer and wherein said vesicle is not a biological cell. 2. The vesicle of claim 1, wherein said fluorophore is selected from the group consisting of 1,6-diphenylhexa-1,3,5-triene, nitrobenzene-2-oxa-1,3-diazole, tryptophan, tyrosine, dansyl chloride, pyrene, naphthalene, and fluorescein. 3. The vesicle of claim 1, wherein said carrier is selected from the group consisting of a protein, a polypeptide, a sugar, a synthetic polymer, and a natural polymer. 4. The vesicle of claim 1, wherein said carrier comprises a serum albumin or a serum lipoprotein. 5. The vesicle of claim 1, wherein said bilayer comprises at least one of a phospholipid, sphingolipid, or glycolipid. 6. The vesicle of claim 5, wherein said lipid bilayer comprises a phosphatidylcholine. 7. The vesicle of claim 1, wherein said lipid bilayer comprises cholesterol. 8. The vesicle of claim 1, wherein said lipid bilayer comprises a protein. 9. The vesicle of claim 1, wherein said lipid bilayer comprises an isolated cell membrane. 10. The vesicle of claim 9, wherein said cell membrane is a bacterial, protozoan, animal, plant, fungal, or mycoplasma cell membrane. 11. The vesicle of claim 10, wherein said cell membrane is a mammalian cell membrane. 12. The vesicle of claim 11, wherein said mammalian cell membrane is an intestinal endothelial cell membrane. 13. The vesicle of claim 1, wherein said lipid bilayer comprises a pump. 14. The vesicle of claim 13, wherein said lipid bilayer comprises an efflux pump. 15. The vesicle of claim 1, wherein said lipid bilayer comprises a P-glycoprotein. 16. The vesicle of claim 1, wherein said fluorophore is a fluorescent monomer in a natural polymer. 17. The vesicle of claim 1, wherein said fluorophore is a fluorescent monomer in a synthetic polymer. 18. The vesicle of claim 1, wherein said lipid bilayer comprises a phosphoglyceride, ether lipid, sterol, steroid, hopanoid, carotenoid, or terpenoid. 19. The vesicle of claim 1, further comprising a protein, polypeptide, sugar, nucleic acid, synthetic or naturally occurring polymer, fatty acid, aromatic compound, alcohol, or glycol in the aqueous interior. 20. The vesicle of claim 1, wherein said carrier comprises a protein, polypeptide, poly(ethylene glycol), poly(ethylene oxide), starch, cyclodextrin polymer, a water-soluble cellulose, nucleic acid, or carbohydrate. 21. The vesicle of claim 1, wherein said vesicle has a diameter of between 25 and 10,000 nm. 22. The vesicle of claim 21, wherein said vesicle has a diameter of between 25 and 1000 nm. 23. The vesicle of claim 21, wherein said vesicle has a diameter between 100 and 300 nm.
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