Synthesis and in vitro stability of macromolecular prodrugs of norfloxacin

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 conjug...

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Bibliographic Details
Published in:Journal of controlled release 1997-09, Vol.47 (3), p.283-291
Main Authors: Coessens, Veerle, Schacht, Etienne H, Domurado, Dominique
Format: Article
Language:English
Subjects:
Antibacterial agents
Antibiotics. Antiinfectious agents. Antiparasitic agents
Biological and medical sciences
Degradation
General pharmacology
In vitro release experiments
Lysosomal enzymes
Medical sciences
Norfloxacin
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Tetrapeptides
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Summary: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.
ISSN:0168-3659
1873-4995
DOI:10.1016/S0168-3659(97)01655-6