Abstract
The cell membrane is an impassable barrier for small hydrophilic molecules, termed nonpermeant, that are too hydrophilic for diffusing through the plasma membrane, and moreover are not recognized and internalized by a transporter, channel, or receptor system. Reversible cell electropermeabilization allows the cellular uptake of these nonpermeant small molecules. Studies demonstrating that bleomycin is a nonpermeant anticancer drug possessing a very high intrinsic cytotoxicity (the toxicity displayed when the drug has no biological barrier separating it from its target) have lead to the development of the electrochemotherapy concept. Indeed, cell electropermeabilization can increase bleomycin toxicity several thousand-fold in vitro and about thousand-fold in vivo. At the dosages used, bleomycin selectively kills the dividing cells by a mitotic cell death process. The physico-chemical bases reported in this chapter give light to the interesting aspects of the electrochemotherapy revealed and/or confirmed by the clinical trials, in particular, its efficacy and safety.
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Silve, A., Mir, L.M. (2011). Cell Electropermeabilization and Cellular Uptake of Small Molecules: The Electrochemotherapy Concept. In: Kee, S., Gehl, J., Lee, E. (eds) Clinical Aspects of Electroporation. Springer, New York, NY. https://doi.org/10.1007/978-1-4419-8363-3_6
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DOI: https://doi.org/10.1007/978-1-4419-8363-3_6
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