Studies on the comparative distribution and biliary excretion of doxorubicin and 4'-epi-doxorubicin in mice and rats

M. Broggini, T. Colombo, A. Martini, M. G. Donelli

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Serum and tissue distribution of doxorubicin (DX) and its stereoisomer, 4'-epidoxorubicin (4'-epiDX), after iv injection f 15 mg/kg was investigated in C57BL mice bearing 14-day intramuscular Lewis lung carcinoma. Total fluorescence was measued together with unchanged drugs, separated, and quantitated by means of thin-layer chromatography combined with a scannig fluorescence technique. In serum the disappearance of 4'-epiDX paralleled that of DX and both unchanged isomers represente <50% of the total fluorescence measured as early as 30 minutes after drug injection. In tissues the fluorescence measurd was almost completely accounted for by the native compounds, both DX and 4'-epiDX, indicating that these drugs are take up as such by tissues. 4'-EpiDX levels were markedly lower than those of DX in tumor and spleen, whereas in heart, liver, ad kidneys the concentrations of the two isomers were the same. Traces of doxorubicinol and possibly 4'-epidoxorubicinol wre detected only in serum, liver, and kidneys. Comparative cumulative biliary excretion of DX and 4'-epiDX investigated i the rat indicated that a total of 40%-45% of the injected dose of both drugs was excreted either as unchanged compound or a reduced metabolite. However, the proportions were different and the presence of twice as much reduced metabolite and smaler amounts of native 4'-epiDX suggests that its metabolic rate is different from that of DX.

Original languageEnglish
Pages (from-to)897-904
Number of pages8
JournalCancer Treatment Reports
Issue number8-9
Publication statusPublished - 1980


ASJC Scopus subject areas

  • Cancer Research
  • Oncology

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