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Diferential adriamycin® istribution to blood components

Summary

The differential distribution of doxorubicin (Adriamycin® = AM) and daunorubicin (Daunomycin = DM) within the blood components, after an i.v. injection of 10 or 15 mg/kg of body weight, was investigated in Cd-COBS rats. AM and DM were measured by a fluorimetric procedure, and the unchanged compound was separated from its metabolites and quantified by means of the TLC scanning fluorescence technique. AM accumulated in the following order (of decreasing percentages): plasma and red cells (RBC), white cells (WBC), and platelets (PT), but the absolute amount of drug that reached each cell type was related to its relative volume. In the presence of higher blood concentrations (after injection of 15 mg/kg of body weight) the RBCs accumulated much more AM than the plasma, WBC, and PT; suggesting that the RBC fraction has a greater capacity to concentrate the drug. However, if the concentration of AM is expressed per unit volume of each component, a markedly higher value was observed for PT, and this was confirmed byin vitro results obtained by incubating blood in the presence of AM. DM seemed to be distributed on a percent basis to a greater extent than AM in the RBC fraction. Both compounds were taken up by blood cells, particularly platelets, to levels in excess of the extracellular concentration. This work was supported by NCI (Contract No. NOI CM 67064) and CNR (Progetto Finalizzato: Control of Cancer Growth).

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Correspondence to Maria Grazia Donelli.

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Colombo, T., Broggini, M., Garattini, S. et al. Diferential adriamycin® istribution to blood components. European Journal of Drug Metabolism and Pharmacokinetics 6, 115–122 (1981). https://doi.org/10.1007/BF03189477

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Key yords

  • Anticancer agents
  • Adriamycin®
  • pharmacokinetics in rats
  • blood cells distribution