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Antimicrob Agents Chemother ; 50(6): 1982-8, 2006 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-16723555

RESUMO

Mycobacterium tuberculosis is an intracellular pathogen that persists within macrophages of the human host. One approach to improving the treatment of tuberculosis (TB) is the targeted delivery of antibiotics to macrophages using ligands to macrophage receptors. The moxifloxacin-conjugated dansylated carboxymethylglucan (M-DCMG) conjugate was prepared by chemically linking dansylcadaverine (D) and moxifloxacin (M) to carboxymethylglucan (CMG), a known ligand of macrophage scavenger receptors. The targeted delivery to macrophages and the antituberculosis activity of the conjugate M-DCMG were studied in vitro and in vivo. Using fluorescence microscopy, fluorimetry, and the J774 macrophage cell line, M-DCMG was shown to accumulate in macrophages through scavenger receptors in a dose-dependent (1 to 50 microg/ml) manner. After intravenous administration of M-DCMG into C57BL/6 mice, the fluorescent conjugate was concentrated in the macrophages of the lungs and spleen. Analyses of the pharmacokinetics of the conjugate demonstrated that M-DCMG was more rapidly accumulated and more persistent in tissues than free moxifloxacin. Importantly, therapeutic studies of mycobacterial growth in C57BL/6 mice showed that the M-DCMG conjugate was significantly more potent than free moxifloxacin.


Assuntos
Antituberculosos/farmacocinética , Compostos Aza/farmacocinética , Glucanos/química , Glucanos/farmacocinética , Macrófagos Alveolares/efeitos dos fármacos , Mycobacterium tuberculosis/efeitos dos fármacos , Quinolinas/farmacocinética , Animais , Antituberculosos/química , Área Sob a Curva , Compostos Aza/sangue , Compostos Aza/química , Líquido da Lavagem Broncoalveolar/citologia , Contagem de Colônia Microbiana , Compostos de Dansil/química , Relação Dose-Resposta a Droga , Fluoroquinolonas , Glucanos/sangue , Meia-Vida , Técnicas In Vitro , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Moxifloxacina , Quinolinas/sangue , Quinolinas/química
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