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Synthesis and in vitro stability of macromolecular prodrugs of norfloxacin

1997; Elsevier BV; Volume: 47; Issue: 3 Linguagem: Inglês

10.1016/s0168-3659(97)01655-6

1873-4995

Veerle Coessens, Etienne Schacht, Dominique Domurado,

Antibiotic Resistance in Bacteria

Oligopeptide derivatives of the antimicrobial drug norfloxacin, having the tetrapeptides gly-phe-ala-leu or gly-phe-leu-gly substituted on the piperazine amino group, were subsequently coupled with chloroformate-activated dextran. In vitro release experiments in aqueous buffer demonstrate the conjugates to be stable in buffers of pH 7.4 and 5.5. However, in the presence of lysosomal enzymes, the derivatives are degraded. The rate of degradation is followed by HPLC-analysis.