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Improving the Stability and Activity of Oral Therapeutic Enzymes—Recent Advances and Perspectives

Fuhrmann, Gregor ; Leroux, Jean-Christophe

In: Pharmaceutical Research, 2014, vol. 31, no. 5, p. 1099-1105

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    Titre
    • Improving the Stability and Activity of Oral Therapeutic Enzymes—Recent Advances and Perspectives
    Auteur
    • Fuhrmann, Gregor. Institute of Pharmaceutical Sciences Department of Chemistry and Applied Biosciences, ETH Zurich, Wolfgang-Pauli-Str. 10, HCI H 301, 8093, Zurich, Switzerland
    • Leroux, Jean-Christophe. Institute of Pharmaceutical Sciences Department of Chemistry and Applied Biosciences, ETH Zurich, Wolfgang-Pauli-Str. 10, HCI H 301, 8093, Zurich, Switzerland
    Type de document
    • Postprint
    Langue
    • Inglese
    Publié dans
    • Pharmaceutical Research, 2014, vol. 31, no. 5, p. 1099-1105. Springer US; http://www.springer-ny.com
    Autre version électronique
    Identifiant OAI-PMH
    • oai:doc.rero.ch:325508
    Summary
    Exogenous, orally-administered enzymes are currently in clinical use or under development for the treatment of pathologies, such as celiac disease and phenylketonuria. However, the administration of therapeutic enzymes via the oral route remains challenging due to potential inactivation of these fragile macromolecular entities in the harsh environment of the gastrointestinal tract. Enzymes are particularly sensitive because both proteolysis and unfolding can lead to their inactivation. Current efforts to overcome these shortcomings involve the application of gastro-resistant delivery systems and the modification of enzyme structures by polymer conjugation or protein engineering. This perspective manuscript reviews and critically discusses recent progress in the oral delivery of therapeutic enzymes, whose substrate is localized in the gastrointestinal tract.