Preparation, in vitro release and antibacterial activity evaluation of rifampicin and moxifloxacin-loaded poly(D,L-lactide-co-glycolide) microspheres

Abstract

Osteomyelitis is difficult to treat because infective bone is poorly accessible for intravenously administering antibiotics and biofilm formation increases bacterial resistance. In this study, microspheres prepared using poly(lactide-co-glycolide) (PLGA) and embedded with moxifloxacin (MOX–PLGA microspheres) and rifampicin/moxifloxacin (RIF/MOX–PLGA microspheres) using the water-in-oil-in-water double emulsion solvent evaporation technique were used for local delivery. Shape of MOX–PLGA microspheres and RIF/MOX–PLGA microspheres were spherical, mean particle size of them were 20.52 μm and 16.62 μm, respectively. Encapsulation efficiency of the MOX-PLGA microspheres was 17.35% ± 2.42%. However, the encapsulation efficiency for MOX and RIF in RIF/MOX–PLGA microspheres was 33.25% ± 7.51% and 49.0% ± 11.25%, respectively. Moxifloxacin and rifampicin were released slowly from microspheres. Both microspheres can efficiently release antibiotics in vitro. Antibacterial and bacterial biofilm-inhibition properties of the released solution were investigated from RIF/MOX–PLGA, MOX–PLGA, and blank PLGA microspheres at varying time points in vitro. RIF/MOX–PLGA microspheres demonstrated the strongest antibacterial activity and bacterial biofilm-inhibition property than the other two microspheres (p < .05). This study suggests that the novel RIF/MOX–PLGA microspheres can be used as a promising carrier for osteomyelitis treatment.