Liposome‐encapsulated Desferrioxamine in Experimental Iron Overload

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Abstract
Deferrioxamine (DF) was encapsulated in multilamellar liposomes (ML) and unilamellar liposomes (UL). Liposomes were prepared with or without a glycolipid, i.e., galactocerebroside (GC). The average diameter of ML was 0.5 .mu.m, and that of UL was 0.08 .mu.m. Less than 5% of DF leaked out from the liposomes after incubation in mouse plasma for 6 h. 59Fe-ferritin and 59Fe-labeled heat damaged erythrocytes (59Fe-DRBC) were administered to normal and hypertransfused mice as models of Fe 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; liposomes without GC removed more 59Fe radioactivity from mice receiving 59Fe-DRBC. GC-liposomes may have a higher affinity for parenchymal cells of the liver; liposomes without the glycolipid may have a higher uptake by the Kupffer cells.