| Summary: | Objectives: Treatment of human brucellosis demands antibiotic targeting into the mononuclearphagocytic
system. The aim of this work was to prepare and characterize particulate carriers containing
gentamicin and to study their interactions with phagocytic cells and bactericidal activity against intracellular
Brucella melitensis.
Methods: Different poly(lactide-co-glycolide) (PLGA)polymers with free carboxylic end-group wereusedto
formulate micro- and nanoparticles containing gentamicin, by a water-oil-water solvent-evaporation technique.
PLGA 502H and 75:25H microparticles were selected because they showed the highest gentamicin
loadings as well as good physico-chemical properties and sustained release in vitro.
Results: Gentamicin-containing microspheres of both polymers were successfully phagocytosed by infected
THP-1 human monocytes, and immunocytochemistry studies revealed that the antibiotic reached
Brucella-specific compartments. A dose of 30 mg of encapsulated gentamicin was able to reduce intracellular
Brucella infection by 2.2 log.
Conclusions: Altogether, these results suggest that 502H and 75:25H microspheres are suitable carriers for
gentamicin targeting inside human macrophages and thus for brucellosis treatment.
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