As there is an increased volume of receptors of LDL in certain cells as a result of a disease or inflammation reaction, the LDE tends to concentrate in these cells when injected into the bloodstream, as demonstrated in patients carrying certain types of cancer. iCell has been successful in using the LDE to formulate new therapeutic agents applied to the treatment of subset of populations with tumors over-expressing LDL receptors.

LDE - a lipid emulsion without protein

LDE is an artificially made microemulsion formed of quasi-spherical nanoparticles basically composed of a monolayer of phosphatidylcholine surrounding a core of cholesteryl esters. Small amounts of unesterified cholesterol and triglycerides are also present. LDE mimics the lipid portion of LDL and when in contact with the plasma, acquires apolipoproteins from the circulating native lipoproteins undergoing lipolysis. One of the proteins acquired by the microemulsion, apo E, is recognized by the LDL receptors. This enables the LDE particles to bind to these receptors. LDE is then removed from the circulation by LDL receptors present on the cell membrane. Once taken up by LDL receptors, LDE is internalized into the cytoplasm via LDL receptor-mediated endocytosis.

Relative to native LDL, LDE is more rapidly removed from the plasma because it binds to the receptor through Apo E, and not through apo B100 as does native LDL. The affinity of apo E for the receptor is several folds greater than that of apoB1003. Consequently the emulsion particles are even more efficiently removed by the receptors than the native LDL.