title: Polymeric prodrugs of antibiotics with improved efficiency.
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 alpha-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.
authors.affiliation: Polymer Materials Research Group, Institute for Biomedical Technologies, Department of Organic Synthesis, University of Ghent, Krijgslaan 281, S4 bis, 9000 Ghent, Belgium.
authors.forename: E
authors.initials: E
authors.lastname: Roseeuw
authors.forename: V
authors.initials: V
authors.lastname: Coessens
authors.forename: E
authors.initials: E
authors.lastname: Schacht
authors.forename: B
authors.initials: B
authors.lastname: Vrooman
authors.forename: D
authors.initials: D
authors.lastname: Domurado
authors.forename: G
authors.initials: G
authors.lastname: Marchal