Compositions of lipids and stabilizing materials
First Claim
1. A vesicular composition comprising, in an aqueous carrier, vesicles comprising a lipid, a gas or gaseous precursor encapsulated in the vesicles, and a material which is capable of stabilizing the composition, wherein said stabilizing material is associated non-covalently with said lipid and is present in an amount sufficient to coat said lipid but insufficient to raise the viscosity of the composition, wherein said gas and gaseous precursor comprise a fluorinated compound selected from the group consisting of perfluorocarbons and sulfur hexafluoride, and wherein said stabilizing material comprises a polymer.
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Abstract
Compositions comprising, in an aqueous carrier, a lipid and a material which is capable of stabilizing the composition. The stabilizing material is associated non-covalently with said lipid and is present in an amount sufficient to coat the lipid but insufficient to raise the viscosity of the composition. The compositions are particularly suitable for use in diagnostic applications, including ultrasound. The compositions can take the form of vesicular compositions, such as micelles and liposomes.
276 Citations
220 Claims
- 1. A vesicular composition comprising, in an aqueous carrier, vesicles comprising a lipid, a gas or gaseous precursor encapsulated in the vesicles, and a material which is capable of stabilizing the composition, wherein said stabilizing material is associated non-covalently with said lipid and is present in an amount sufficient to coat said lipid but insufficient to raise the viscosity of the composition, wherein said gas and gaseous precursor comprise a fluorinated compound selected from the group consisting of perfluorocarbons and sulfur hexafluoride, and wherein said stabilizing material comprises a polymer.
- 18. A formulation for therapeutic or diagnostic use comprising, in combination with a bioactive agent, vesicles comprising a lipid, a gas or gaseous precursor encapsulated in said vesicles, and a material which is capable of stabilizing the formulation, wherein said stabilizing material is associated non-covalently with said lipid and is present in an amount sufficient to coat said lipid but insufficient to raise the viscosity of the formulation, wherein said gas and gaseous precursor comprise a fluorinated compound selected from the group consisting of perfluorocarbons and sulfur hexafluoride, and wherein said stabilizing material comprises a polymer.
- 21. A process for the preparation of a stabilized vesicular composition comprising vesicles comprising a lipid, a gas or gaseous precursor encapsulated in the vesicles, and a stabilizing material which is capable of associating non-covalently with said lipid, wherein the process comprises combining together said lipid, gas or gaseous precursor, and stabilizing material, wherein said stabilizing material is combined with said lipid in an amount sufficient to coat said lipid but insufficient to raise the viscosity of the composition, wherein said gas and gaseous precursor comprise a fluorinated compound selected from the group consisting of perfluorocarbons and sulfur hexafluoride, and wherein said stabilizing material comprises a polymer.
- 23. A process for the preparation of a formulation for diagnostic or therapeutic use comprising, in combination with a bioactive agent, a vesicular composition which comprises a lipid, a gas or gaseous precursor encapsulated in said vesicles, and a stabilizing material which is associated non-covalently with the lipid, wherein the process comprises combining together said bioactive agent and vesicular composition, wherein said stabilizing material is present in said composition in an amount sufficient to coat said lipid but insufficient to raise the viscosity of said composition, wherein said gas and gaseous precursor comprise a fluorinated compound selected from the group consisting of perfluorocarbons and sulfur hexafluoride, and wherein said stabilizing material comprises a polymer.
- 25. A stabilized vesicular composition comprising a lipid, a gas or gaseous precursor encapsulated in the vesicles, and a stabilizing material which is capable of associating non-covalently with said lipid, wherein the composition is prepared by combining together said lipid, gas or gaseous precursor, and stabilizing material, wherein said stabilizing material is combined with said lipid in an amount sufficient to coat said lipid but insufficient to raise the viscosity of the composition, wherein said gas and gaseous precursor comprise a fluorinated compound selected from the group consisting of perfluorocarbons and sulfur hexafluoride, and wherein said stabilizing material comprises a polymer.
- 26. A stabilized formulation for diagnostic or therapeutic use comprising a bioactive agent and a vesicular composition which comprises a lipid, a gas or gaseous precursor encapsulated in said vesicles, and a material which is capable of stabilizing the formulation and is associated non-covalently with said lipid, wherein said composition is prepared by combining together said lipid, gas or gaseous precursor and stabilizing material, wherein said stabilizing material is present in an amount sufficient to coat said lipid but insufficient to raise the viscosity of the formulation, wherein said gas and gaseous precursor comprise a fluorinated compound selected from the group consisting of perfluorocarbons and sulfur hexafluoride, and wherein said stabilizing material comprises a polymer.
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27. A method for providing an image of an internal region of a patient comprising (i) administering to the patient a vesicular composition comprising, in an aqueous carrier, vesicles comprising a lipid, a gas or a gaseous precursor encapsulated in said vesicles, and a material which is capable of stabilizing the composition, wherein said stabilizing material is associated non-covalently with said lipid and is present in an amount sufficient to coat said lipid but insufficient to raise the viscosity of the composition, wherein said gas and gaseous precursor comprise a fluorinated compound selected from the group consisting of perfluorocarbons and sulfur hexafluoride, and wherein said stabilizing material comprises a polymer;
- and (ii) scanning the patient using ultrasound to obtain a visible image of the region.
- View Dependent Claims (156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176)
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28. A method for diagnosing the presence of diseased tissue in a patient comprising (i) administering to the patient a vesicular composition comprising, in an aqueous carrier, vesicles comprising a lipid, a gas or a gaseous precursor encapsulated in said vesicles, and a material which is capable of stabilizing the composition, wherein said stabilizing material is associated non-covalently with said lipid and is present in an amount sufficient to coat said lipid but insufficient to raise the viscosity of the composition, wherein said gas and gaseous precursor comprise a fluorinated compound selected from the group consisting of perfluorocarbons and sulfur hexafluoride, and wherein said stabilizing material comprises a polymer;
- and (ii) scanning the patient using ultrasound to obtain a visible image of any diseased tissue in the patient.
- View Dependent Claims (177, 178, 179, 180, 181, 182, 183, 184, 185, 186, 187, 188, 189, 190, 191, 192, 193, 194, 195, 196, 197)
- 29. A method for the therapeutic delivery in vivo of a bioactive agent comprising administering to a patient a therapeutically effective amount of a formulation which comprises, in combination with a bioactive agent, a vesicular composition comprising a lipid, a gas or gaseous precursor encapsulated in said vesicles, and a material which stabilizes said composition, wherein said stabilizing material is associated noncovalently with said lipid and is present in said composition in an amount sufficient to coat said lipid but insufficient to raise the viscosity of said composition, wherein said said gas and gaseous precursor comprise a fluorinated compound selected from the group consisting of perfluorocarbons and sulfur hexafluoride, and wherein said stabilizing material comprises a polymer.
Specification