Controlled Systemic Release of Therapeutic Peptides from PEGylated Prodrugs by Serum Proteases

Authors

  • Friederike Inga Nollmann,

    1. Institut für Bioanalytische Chemie, Zentrum für Biotechnologie und Biomedizin, Universität Leipzig, Deutscher Platz 5, 04103 Leipzig (Germany
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    • F.I.N and T.G. contributed equally to this work.

  • Tina Goldbach,

    1. Institut für Bioanalytische Chemie, Zentrum für Biotechnologie und Biomedizin, Universität Leipzig, Deutscher Platz 5, 04103 Leipzig (Germany
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    • F.I.N and T.G. contributed equally to this work.

  • Nicole Berthold,

    1. Institut für Bioanalytische Chemie, Zentrum für Biotechnologie und Biomedizin, Universität Leipzig, Deutscher Platz 5, 04103 Leipzig (Germany
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  • Prof. Ralf Hoffmann

    Corresponding author
    1. Institut für Bioanalytische Chemie, Zentrum für Biotechnologie und Biomedizin, Universität Leipzig, Deutscher Platz 5, 04103 Leipzig (Germany
    • Institut für Bioanalytische Chemie, Zentrum für Biotechnologie und Biomedizin, Universität Leipzig, Deutscher Platz 5, 04103 Leipzig (Germany
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  • We thank Prof. Dr. M. Blüher for the serum samples, Dr. D. Knappe for helpful discussions, and Dr. A. Hagen for proofreading. This research was supported by the European Fund for Regional Structure Development (EFRE, European Union and Free State of Saxony).

Abstract

original image

A novel concept to release peptidic drugs systemically by serum proteases from a PEGylated precursor makes it possible to tune release kinetics to fit the medical needs. Drug release depends on the size of the PEG polymer and the sequence and length of the peptide linker. The antimicrobial activities of the prodrugs were even better than those of the free peptides, whereas direct PEGylation abolished the peptide activity.

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