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Antimicrobial Agents and Chemotherapy, November 2003, p. 3435-3441, Vol. 47, No. 11
0066-4804/03/$08.00+0     DOI: 10.1128/AAC.47.11.3435-3441.2003
Copyright © 2003, American Society for Microbiology. All Rights Reserved.

Synthesis, Degradation, and Antimicrobial Properties of Targeted Macromolecular Prodrugs of Norfloxacin

Eveline Roseeuw,1 Veerle Coessens,1 Anne-Marie Balazuc,2 Micheline Lagranderie,2 Pierre Chavarot,2 Augusto Pessina,3 Maria Grazia Neri,3 Etienne Schacht,1 Gilles Marchal,2 and Dominique Domurado4*

Biomaterial and Polymer Research Group, Department of Organic Chemistry, University of Ghent, 9000 Ghent, Belgium,1 Laboratoire de Référence des Mycobactéries, Institut Pasteur, 75724 Paris Cedex 15,2 Groupe de Pharmacocinétique des Prodrogues et Conjugués Macromoléculaires (INSERM), CRBA-UMR 5473 CNRS, Faculté de Pharmacie, 34093 Montpellier Cedex 5, France,4 Istituto de Microbiologia, Università di Milano, 20133 Milan, Italy3

Received 13 December 2002/ Returned for modification 14 April 2003/ Accepted 11 August 2003

Long-term antibiotic treatment is required to cure tuberculosis. Targeted antibiotics should improve the efficacy of treatment by concentrating the drugs close to the bacteria. The aim of the present study was to synthesize targeted conjugates. For this purpose, we used mannose as a homing device to direct norfloxacin into macrophages. Dextran was used as the polymer bearing both mannose and norfloxacin. Using different peptide spacer arms to link norfloxacin to dextran, we demonstrated that norfloxacin acts as an antibiotic only when it is released in its native form. Also, targeting by using mannose as a homing device is required to achieve antimycobacterial activity in vivo. Thus, norfloxacin, which is inactive against mycobacteria in its native form in vivo, can be transformed into an active drug by targeting.

* Corresponding author. Mailing address: CRBA, Faculté de Pharmacie, 15 Ave. Charles Flahault, BP 14491, 34093 Montpellier Cedex 5, France. Phone: (33) 467-418-268. Fax: (33) 467-520-898. E-mail: domurado{at}univ-montp1.fr.

Antimicrobial Agents and Chemotherapy, November 2003, p. 3435-3441, Vol. 47, No. 11
0066-4804/03/$08.00+0     DOI: 10.1128/AAC.47.11.3435-3441.2003
Copyright © 2003, American Society for Microbiology. All Rights Reserved.



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