Yechezkel Barenholz

Yechezkel Barenholz's Laboratory of Membrane and Liposome Research at the Hebrew University-Hadassah Medical School devised the pegylated liposomal formulation of doxorubicin approved by the FDA in 1995 as Doxil, the first nano-drug approved anywhere. His own account in Journal of Controlled Release identifies three unrelated principles that had to work together: a polyethylene-glycol coat that keeps the liposome in circulation and away from the reticuloendothelial system, high and stable remote loading of doxorubicin driven by a transmembrane ammonium sulfate gradient that also allows release at the tumour, and a lipid bilayer held in a liquid-ordered phase by a high-melting phosphatidylcholine with cholesterol. The clinical effect is that hand-foot syndrome and mucositis replace the hair loss and heart damage of free doxorubicin. Barenholz's laboratory still publishes on liposome and PEGylation chemistry.