Document Detail


Norfloxacin-poly(L-lysine citramide imide) conjugates and structure-dependence of the drug release.
MedLine Citation:
PMID:  15512781     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Norfloxacin (Nflx), an antibiotic which is active against some intracellular bacteria, was coupled to a polymeric carrier, namely poly(L-lysine citramide) via a lysine or an ethylcarbamate spacer to obtain a macromolecular prodrug. The carrier, which derived from the two metabolites citric acid and L-lysine, is known to be biocompatible and slowly degradable under slight acidic conditions. Conjugates were characterised by UV, 1H and 13C NMR and SEC. The presence of Norfloxacin and the lysine type spacer caused chain aggregation, due to a probable physical cure. The release of Norfloxacin from these prodrugs and from a prodrug where Norfloxacin is bound to the carrier backbone without spacer arm was investigated comparatively in vitro. Conjugation via a carbamate-type linkage appeared as a method to achieve the release of Norfloxacin from a PLCA-type conjugate at neutral.
Authors:
Stéphanie Gac-Breton; Jean Coudane; Mahfoud Boustta; Michel Vert
Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Journal of drug targeting     Volume:  12     ISSN:  1061-186X     ISO Abbreviation:  J Drug Target     Publication Date:  2004 Jun 
Date Detail:
Created Date:  2004-10-29     Completed Date:  2004-12-30     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  9312476     Medline TA:  J Drug Target     Country:  England    
Other Details:
Languages:  eng     Pagination:  297-307     Citation Subset:  IM    
Affiliation:
CRBA-UMR CNRS 5473, Faculty of Pharmacy, Montpellier I University, France.
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MeSH Terms
Descriptor/Qualifier:
Drug Carriers
Hydrogen-Ion Concentration
Norfloxacin / administration & dosage*,  chemistry
Nylons*
Solubility
Chemical
Reg. No./Substance:
0/Drug Carriers; 0/Nylons; 0/poly(lysine citramide imide); 70458-96-7/Norfloxacin

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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