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Extensive and saturable accumulation of paclitaxel by the human platelet

  • Original Article
  • Taxol, Paclitaxel, Platelets
  • Published:
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Abstract

Little is known about the cellular distribution of paclitaxel in humans. In the present study we examined the distribution of [3H]-paclitaxel in human blood. When 1 μM paclitaxel was incubated with fresh blood at 37°C, the platelet/plasma concentration ratio was 240±17 (mean±SEM), whereas the red blood cell (RBC)/plasma concentration ratio was only 0.59±0.05. In kinetics experiments using platelet-rich plasma, we observed that the platelet accumulation of paclitaxel was highly temperature- and concentration-dependent. Scatchard analysis of the 37°C uptake data demonstrated a dissociation constant (K app) of 0.80±0.10 μM and a maximal binding capacity of 672±102 pmol/109 platelets. It is proposed that the platelet accumulation of paclitaxel reflects binding to microtubules and may serve as a useful model for binding to less accessible cellular sites.

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Authors and Affiliations

  1. Department of Cell and Molecular Pharmacology and Experimental Therapeutics, Medical University of South Carolina, 171 Ashley Avenue, 29425, Charleston, SC, USA

    Mark D. Wild, U. Kristina Walle & Thomas Walle

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  1. Mark D. Wild
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  2. U. Kristina Walle
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  3. Thomas Walle
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Wild, M.D., Walle, U.K. & Walle, T. Extensive and saturable accumulation of paclitaxel by the human platelet. Cancer Chemother. Pharmacol. 36, 41–44 (1995). https://doi.org/10.1007/BF00685730

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  • DOI: https://doi.org/10.1007/BF00685730

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