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Inhaled anti-infective drugs play a pivotal role in the prophylaxis and treatment of respiratory tract infections. In this study, fluoroquinolone antibiotic levofloxacin hemihydrate-loaded PLGA microparticles were prepared and evaluated. PLGA microparticles were prepared using three different preparation methods such as oil-in-water (o/w), water-in-oil-in-water (w1/o/w2) and modified water-inoil-in-water (w1/o/w3) emulsion solvent evaporation methods. Effects of preparation methods and formulation parameters on physicochemical properties of microparticles characterized in terms of the particle size, encapsulation efficiency, production yield, in vitro release and aerodynamic properties were evaluated. Particle size results showed that the increasing volume of dichlorometane in the organic phase caused a significant decrease in particle size of microparticles. Microparticles prepared by using o/w emulsion solvent evaporation method showed a higher encapsulation efficiency value compared to those prepared with double emulsion methods. Biphasic extended-release profile was produced in vitro. All formulations prepared except of F1 coded formulation were of suitable aerodynamic size for inhalation having a mass median aerodynamic diameter less than 5 μm. These results showed that levofloxacin hemihydrate-loaded PLGA microparticles could be a potential alternative to the existing levofloxacin therapy in respiratory tract infections.

The Application Of Different Microencapsulation Methods And Formulation Parameters On Antibiotic Loaded Plga Microparticles For Pulmonary Delivery