Temperature-Sensitive Liposomal Formulation
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Abstract
A liposome contains an active agent and has a gel-phase lipid bilayer membrane comprising phospholipid and a surface active agent. The phospholipids are the primary lipid source for the lipid bilayer membrane and the surface active agent is contained in the bilayer membrane in an amount sufficient to increase the percentage of active agent released at the phase transition temperature of the lipid bilayer, compared to that which would occur in the absence of the surface active agent. The surface active agent is present in the lipid bilayer membrane so as to not destabilize the membrane in the gel phase.
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Citations
87 Claims
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1-65. -65. (canceled)
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66. A liposome having a gel-phase bilayer membrane, comprising:
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an active agent selected from the group consisting of a pharmacologically active agent, a therapeutic agent, a flavor agent, a diagnostic or imaging agent, a nutritional agent, and combinations thereof, wherein the gel-phase bilayer has a phase transition temperature of 39°
C. to 45°
C., and wherein the gel-phase lipid bilayer membrane comprises;(a) a first component which is dipalmitoylphosphatidylcholine (DPPC) in an amount ranging from 80 to 98 mol %; and (b) a second component which is monostearoylphosphatidylcholine (MSPC) in an amount ranging from 2 to 20 mol %. - View Dependent Claims (67, 68, 69, 70, 71, 72, 73, 74, 75, 76)
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77. A liposome having a gel-phase bilayer membrane, comprising:
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an active agent selected from the group consisting of a pharmacologically active agent, a therapeutic agent, a flavor agent, a diagnostic or imaging agent, a nutritional agent, and combinations thereof, wherein the gel-phase bilayer has a phase transition temperature of 39°
C. to 45°
C., and wherein the gel-phase lipid bilayer membrane comprises;(a) a first component which is dipalmitoylphosphatidylcholine (DPPC) in an amount ranging from 80 to 98 mol %; and (b) a second component which is monostearoylphosphatidylcholine (MSPC) in an amount ranging from 2 to 20 mol %; and (c) a third component which is 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[poly(ethyleneglycol) 2000] (DSPE-PEG-2000). - View Dependent Claims (78, 79, 80, 81, 82, 83, 84, 85, 86, 87)
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Specification