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Polymeric prodrugs of antibiotics with improved efficiency

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Abstract

Macromolecular prodrugs of the antibiotic norfloxacin were prepared by coupling the drug via a peptide spacer onto a mannosylated dextran. The tetrapeptide gly-phe-gly-gly-gly-OMe was selected as substrate for lysosomal enzymes. The drug was coupled on the α-C of the terminal glycine. In vitro degradation studies demonstrated the release of the parent drug in the presence of cathepsin B. In vivo experiments on mice showed a promising therapeutic effect.

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Authors and Affiliations

  1. Polymer Materials Research Group,Institute for Biomedical Technologies (IBITECH), Department of Organic Synthesis, University of Ghent, Krijgslaan 281, S4 bis, 9000, Ghent, Belgium

    E. Roseeuw, V. Coessens, E. Schacht & B. Vrooman

  2. Groupe de Pharmacocine´tique des Conjugue´s Macromoleculaires (INSERM), Centre de Recherche sur les Biopolyme`res Artificiels (URA CNRS 1465), Faculte´ de Pharmacı´e, 15 Avenue Flahault, 34060, Montpellier, ce´dex 2, France

    D. Domurado

  3. Laboratoire de Physiopathologie Cellulaire, Institut Pasteur, 25 rue du Dr Roux 75015, Paris, France

    G. Marchal

Authors
  1. E. Roseeuw
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  2. V. Coessens
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  3. E. Schacht
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  4. B. Vrooman
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  5. D. Domurado
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  6. G. Marchal
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Roseeuw, E., Coessens, V., Schacht, E. et al. Polymeric prodrugs of antibiotics with improved efficiency. Journal of Materials Science: Materials in Medicine 10, 743–746 (1999). https://doi.org/10.1023/A:1008991508877

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  • DOI: https://doi.org/10.1023/A:1008991508877

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