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