Liposome‐encapsulated Desferrioxamine in Experimental Iron Overload

Summary. We have encapsulated desferrioxamine (DF) in multilamellar liposomes (ML) and unilamellar liposomes (UL). Liposomes were prepared either with or without a glycolipid, i.e. galactocerebroside (GC). The average diameter of ML was 0.5 μm, and that of UL was 0.08 μm. Less than 5% of DF leaked out from the liposomes after incubation in mouse plasma for 6 h. 59Fe-ferritin and 59Fe-labelled heat damaged erythrocytes (59Fe-DRBC) were administered to normal and hyper- transfused mice as models of iron overload. Ferritin was used to label liver parenchymal cells and DRBC to label the Kupffer cells of the liver. A single injection of ML or UL with or without galactocerebroside into normal and hypertransfused mice enhanced from 3- to 15-fold the urinary excretion of radioiron from 59Fe-ferritin and from 59Fe-DRBC injected mice. For both the normal and hypertransfused mice, liposomes containing GC removed more 59Fe radioactivity from 59Fe-ferritin injected mice than liposomes without the glycolipid; whereas liposomes without GC removed more 59Fe radioactivity from mice receiving 59Fe-DRBC. Thus GC-liposomes may have a higher affinity for parenchymal cells of the liver, whereas liposomes without the glycolipid may have a higher uptake by the Kupffer cells.