Pharmacokinetics of the iron chelator desferrioxamine as affected by liposome encapsulation: potential in treatment of chronic hemosiderosis

Journal Article · Sun Jan 22 23:00:00 EST 1978 · Life Sci.; (United States)

DOI:https://doi.org/10.1016/0024-3205(78)90138-8· OSTI ID:5111134

Guilmette, R A; Cerny, E A; Rahman, Y E

Desferrioxamine (DF), the chelator of choice for removal of excess stored iron, is limited by its rapid excretion, metabolic breakdown, and low cell uptake. We have encapsulated DF in unilamellar and multilamellar liposomes, and have compared the short-term pharmacokinetics of nonencapsulated and encapsulated /sup 59/Fe-labeled DF after intravenous administration. Disappearance of /sup 59/Fe-DF from the plasma was very rapid in mice receiving multilamellar liposome-encapsulated and nonencapsulated drug, but much slower in mice receiving unilamellar liposomes. Between 1 and 24 hours after injection, nonencapsulated /sup 59/Fe-DF never exceeded 1 to 5% of the injected dose (ID) in liver or <0.7% in spleen; whereas after either multilamellar or unilamellar liposomes, the uptake in liver was 30 to 35% ID, and in spleen was 1 to 5% ID. Excretion of /sup 59/Fe-DF was much slower with liposome encapsulation. These results indicate that liposomes can effectively deliver DF to critical organs of iron storage. Thus this drug delivery system is potentially useful for treatment of iron overload.

• Research Organization: Argonne National Lab., IL
• OSTI ID: 5111134
• Journal Information: Life Sci.; (United States), Journal Name: Life Sci.; (United States) Vol. 22:4; ISSN LIFSA
• Country of Publication: United States
• Language: English

Related Subjects

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550600 -- Medicine
560305* -- Chemicals Metabolism &amp; Toxicology-- Vertebrates-- (-1987)
59 BASIC BIOLOGICAL SCIENCES
62 RADIOLOGY AND NUCLEAR MEDICINE
63 RADIATION, THERMAL, AND OTHER ENVIRON. POLLUTANT EFFECTS ON LIVING ORGS. AND BIOL. MAT.
AMINES
ANIMALS
BETA DECAY RADIOISOTOPES
BETA-MINUS DECAY RADIOISOTOPES
BIOCHEMICAL REACTION KINETICS
BIOLOGICAL ACCUMULATION
BODY
CARBOXYLIC ACIDS
CELL CONSTITUENTS
CHELATING AGENTS
CLEARANCE
DAYS LIVING RADIOISOTOPES
DEFEROXAMINE
DIGESTIVE SYSTEM
DISEASES
ELEMENTS
EVEN-ODD NUCLEI
EXCRETION
GLANDS
HEMOSIDERIN
HETEROCYCLIC ACIDS
HETEROCYCLIC COMPOUNDS
INJECTION
INTAKE
INTERMEDIATE MASS NUCLEI
INTRAVENOUS INJECTION
IRON
IRON 59
IRON ISOTOPES
ISOTOPES
KINETICS
LABELLED COMPOUNDS
LIVER
MAMMALS
METABOLISM
METALS
MICE
NUCLEI
ORGANIC ACIDS
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANS
PIGMENTS
PORPHYRINS
RADIOISOTOPES
REACTION KINETICS
RODENTS
SPLEEN
THERAPY
TRANSITION ELEMENTS
VERTEBRATES