Hepatocyte-selective oil-in-water emulsion

A heat stable oil-in-water emulsion comprising:

• a) up to 50% (w/v) a lipophilic or amphipathic diagnostic, therapeutic, or biologically active agent which is a polyhalogenated triglyceride selected from the group consisting of iodated arylaliphatic triglyceride analogs having a 1,3-disubstituted triglyceride backbone with a 3-substituted 2,4,6-triiodophenyl aliphatic chain or a monoiodophenyl aliphatic chain, and optionally a pharmaceutically acceptable fat or oil of natural, synthetic, or semi-synthetic origin which is a pharmacologically inert nonpolar lipid;
• b) up to 10% (w/v) phospholipid emulsifier;
• c) up to 5% (w/v) cholesterol, the amount of cholesterol being sufficient to facilitate apoprotein E association;
• d) up to 5% (w/v) of an osmolality adjusting agent;
• and
• e) the remainder of the emulsion being sterile water, the emulsion having a mean particle diameter of the oil phase between 50 to 200 nm with greater than 98% of the particles being less than 300 nm, and being substantially liposome-free and able to withstand heat sterilization without a significant change in mean particle size distribution and without losing its ability to associate with apoprotein E so as to be hepatocyte-selective.

A heat stable oil-in-water emulsion comprising:

• a) up to 50% (w/v) a lipophilic or amphipathic diagnostic, therapeutic, or biologically active agent which is a polyhalogenated triglyceride selected from the group consisting of iodated arylaliphatic triglyceride analogs having a 1,2,3-trisubstituted triglyceride backbone with a 3-substituted 2,4,6-triiodophenyl aliphatic chain or a monoiodophenyl aliphatic chain, and optionally a pharmaceutically acceptable fat or oil of natural, synthetic, or semi-synthetic origin which is a pharmacologically inert nonpolar lipid;
• b) up to 10% (w/v) phospholipid emulsifier;
• c) up to 5% (w/v) cholesterol, the amount of cholesterol being sufficient to facilitate apoprotein E association;
• d) up to 5% (w/v) of an osmolality adjusting agent;
• and
• e) the remainder of the emulsion being sterile water, the emulsion having a mean particle diameter of the oil phase between 50 to 200 nm with greater than 98% of the particles being less than 300 nm, and being substantially liposome-free and able too withstand heat sterilization without a significant change in mean particle size distribution and without losing its ability to associate with apoprotein E so as to be hepatocyte-selective.