Inventor and worldwide provider of clodronate liposomes

Explaining The Mechanism of Clodronate Liposomes

Clodronate is not a toxic drug in itself and liposomes (if prepared of phosphatidylcholine and cholesterol) are not toxic either.

Free Clodronate will not easily pass phospholipid bilayers of liposomes and cell membranes but liposomes are eagerly swallowed by macrophages.

The implication is that Clodronate, once delivered into phagocytic cells using liposomes as vehicles, will not escape from the cell. After disruption of the phospholipid. bilayers of the liposomes under the influence of the lysosomal phospholipases in the macrophage, the drug, which is dissolved in the aqueous compartments between the liposomal bilayers, is released into the cell.

The Clodronate is accumulated intracellularly and after exceeding a threshold concentration, the cell is irreversibly damaged and dies by apoptosis (J. Immunol. Meth. 193: 93-99, 1996).