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AssigneeThe Board of Regents of the University of Michigan
InventorsRaymond E. Counsell, Marc A. Longino, Jamey P. Weichert
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A surface-modified lipoprotein-like oil-in-water emulsion useful as a blood-pool selective delivery vehicle for lipophilic imaging agents or lipophilic derivatives of water-soluble imaging agents. The blood-pool selective delivery vehicle remains in the blood for several hours, shows very little early hepatic sequestration, and is cleared from the blood within 24 hours. The mean diameter of the oil phase is less than 150 nm which minimizes sequestration by the reticuloendothelial system. The surface of the oil phase is modified with a polyethyl glycol-modified phospholipid to prevent normal interactions with the receptor sites of the hepatocytes. In radiographic imaging, radioactive or stable, synthetic or semi-synthetic polyhalogenated triglycerides, such as 2-oleoylglycerol-1,3-bis[7-(3-amino-2,4,6-triiodophenyl)heptanoate], or lipid soluble derivatives of traditional water-soluble contrast agents, such as aliphatic esters of iopanoic, diatrizoic, and acetrizoic acid, may be incorporated into the lipophilic core of a lipoprotein-like emulsion particle.
A surface-modified lipoprotein-like oil-in-water emulsion having a lipophilic core surrounded by a monolayer of amphiphilic or polar lipids, in a non-ionic aqueous phase, the emulsion having a mean particle diameter of the oil phase of between 50 to 150 nm with at least 98% of the particles being between 50 to 250 nm, the lipophilic core including at least one pharmacologically inert nonpolar lipid and at least one lipophilic contrast agent, and the monolayer including an emulsifier, a derivatized polyethylene glycol , and a sterol, wherein the lipophilic core comprises between about 10% and 40% (w/v) of the total emulsion composition.
A surface-modified lipoprotein-like oil-in-water emulsion having a lipophilic core surrounded by a monolayer comprising up to about 10% (w/v) of an amphiphilic or polar lipid, in a non-ionic aqueous phase, the emulsion having a mean particle diameter of the oil phase of between 50 to 150 nm with at least 98% of the particles being between 50 to 250 nm, the lipophilic core including at least one lipophilic agent, and the monolayer including an emulsifier, a derivatized polyethylene glycol, and a sterol, wherein the lipophilic core comprises between about 10% and 40% (w/v) of the total emulsion composition.
A surface-modified lipoprotein-like oil-in-water emulsion having a lipophilic core surrounded by a monolayer of amphiphilic or polar lipids, in a non-ionic aqueous phase, the emulsion having a mean particle diameter of the oil phase of between 50 to 150 nm with at least 98% of the particles being between 50 to 250 nm, the lipophilic core including at least one lipophilic radiologic contrast agent, and the monolayer including an emulsifier, a derivatized polyethylene glycol, and a sterol, wherein the lipophilic core comprises between about 10% and 40% (w/v) of the total emulsion composition.
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