Premium
Target organ disposition and plasma pharmacokinetics of doxorubicin incorporated into albumin microspheres after intrarenal arterial administration
Author(s) -
Kerr D. J.,
Willmott N.,
McKillop J. H.,
Cummings J.,
Lewi H. J.,
McArdle C. S.
Publication year - 1988
Publication title -
cancer
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 3.052
H-Index - 304
eISSN - 1097-0142
pISSN - 0008-543X
DOI - 10.1002/1097-0142(19880901)62:5<878::aid-cncr2820620505>3.0.co;2-2
Subject(s) - doxorubicin , pharmacokinetics , medicine , albumin , microsphere , pharmacology , human serum albumin , serum albumin , kidney , urology , chemotherapy , chemistry , chromatography , chemical engineering , engineering
We synthesized doxorubicin (Adriamycin, Adria Laboratories, Columbus, OH)‐loaded human albumin microspheres (containing approximately 1% doxorubicin w/w) between 15 and 20 μm in diameter. Intrarenal arterial administration of 99m TC‐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 micro‐spheres 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.