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We synthesized doxorubicin (Adriamycin, Adria Laboratories, Columbus, OH)-loaded human albumin microspheres (containing approximately 1% doxorubicin w/w) between 15 and 20 micron in diameter. Intrarenal arterial administration of 99mTC-labeled microspheres demonstrated a high renal entrapment ratio (97% of recovered radioactivity). The pharmacokinetics and metabolism of doxorubicin are different when it is administered in microspherical form. Peak plasma levels are lower (16 ng/ml versus 135 ng/ml) compared with treatment by a doxorubicin solution. Histologic studies showed that the microspheres were trapped within capillaries and small arterioles in the renal vascular arcade. It is apparent that chemoembolization with doxorubicin-loaded microspheres significantly reduces systemic exposure to the antineoplastic agent, and maintains intrarenal drug levels.

Original publication

DOI

10.1002/1097-0142(19880901)62:5<878::aid-cncr2820620505>3.0.co;2-2

Type

Journal article

Journal

Cancer

Publication Date

01/09/1988

Volume

62

Pages

878 - 883

Keywords

Albumins, Animals, Doxorubicin, Injections, Intra-Arterial, Kidney, Kidney Glomerulus, Metabolic Clearance Rate, Microspheres, Rabbits, Tissue Distribution