Analysis of absorption enhancers in epithelial cell models

Authors

  • Rita Rosenthal,

    1. Institute of Clinical Physiology, Campus Benjamin Franklin, Charité– Universitätsmedizin Berlin, Freie Universität and Humboldt Universität, Berlin, Germany.
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  • Miriam S. Heydt,

    1. Department of Anesthesiology and Critical Care Medicine, Campus Benjamin Franklin, Charité Universitätsmedizin Berlin, Freie Universität and Humboldt Universität, Berlin, Germany.
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  • Maren Amasheh,

    1. Department of Gastroenterology, Division of Nutritional Medicine, Campus Benjamin Franklin, Charité Universitätsmedizin Berlin, Freie Universität and Humboldt Universität, Berlin, Germany
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  • Christoph Stein,

    1. Department of Anesthesiology and Critical Care Medicine, Campus Benjamin Franklin, Charité Universitätsmedizin Berlin, Freie Universität and Humboldt Universität, Berlin, Germany.
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  • Michael Fromm,

    1. Institute of Clinical Physiology, Campus Benjamin Franklin, Charité– Universitätsmedizin Berlin, Freie Universität and Humboldt Universität, Berlin, Germany.
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  • Salah Amasheh

    1. Institute of Clinical Physiology, Campus Benjamin Franklin, Charité– Universitätsmedizin Berlin, Freie Universität and Humboldt Universität, Berlin, Germany.
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Salah Amasheh, Institute of Clinical Physiology, Charité, Campus Benjamin Franklin, Hindenburgdamm 30, 12203 Berlin, Germany. salah.amasheh@charite.de

Abstract

A variety of chemical compounds are currently being discussed as novel drug delivery strategies. One promising strategy is to selectively open the paracellular pathway of epithelia for the passage of macromolecules. A prerequisite for this effect is a rapid and reversible action of these compounds, to allow a marked translocation of a drug, but also to avoid unwanted adverse effects, such as the translocation of noxious agents. Bioactive molecules that elevate paracellular permeability include Ca2+ chelators, bacterial toxins, and other compounds, some of which perturb the structural basis of epithelial barrier function—the tight junction. Within the tight junction, organ- and tissue-specific barrier properties are determined mainly by claudins. The majority of members of the claudin protein family seal the paracellular pathway. This paper focuses on recent approaches concerning absorption-enhancing effects, with regard to selectivity and mechanism.

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