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Invented the chemistry that made Doxil work, the first nanomedicine any regulator approved, which is still a standard treatment for relapsed ovarian cancer three decades later.
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.
| Title | Journal | Year |
|---|---|---|
| Doxil, the first FDA-approved nano-drug: lessons learned | Journal of Controlled Release | 2012 |
| PEGylation technology: addressing concerns, moving forward Hebrew University-Hadassah Medical School; indexed on Europe PMC | 2025 |
Shares Hebrew University of Jerusalem, Pegylated liposomal doxorubicin, Kaposi sarcoma, Doxorubicin and the tag drug-delivery.
Shares Pegylated liposomal doxorubicin, Doxorubicin, Ovarian cancer.
Shares Pegylated liposomal doxorubicin, Doxorubicin, Ovarian cancer.
Shares Hebrew University of Jerusalem, Hadassah Medical Center.
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