pH-responsive and porous vancomycin-loaded PLGA microspheres: evidence of controlled and sustained release for localized inflammation inhibition in vitro

Adequate delivery of antibiotics to infected sites is crucial for the effective treatment of bacterial infections. A controlled and sustained release system based on porous and pH-responsive poly(lactic-co-glycolic acid) (PLGA)-vancomycin (Van) microspheres was developed. In this system, drug release is triggered by the weakly acidic environment, like local inflamed tissues. The microspheres, developed through the W1/0/W-2 double-emulsion evaporation method, comprised a PLGA-based shell and a core containing Van and the bubble-generating agent of NaHCO3. The optimized preparation conditions for PLGA-NaHCO3-Van microspheres were investigated and characterized. The PLGA-NaHCO3-Van microspheres exhibited porous microstructures with regular shape and uniform size and the characteristic of controlled drug release, which could be attributed to the incorporation of NaHCO3. The results of the Kirby-Bauer assay confirmed that released Van retained effective antibacterial activity towards standard Staphylococcus aureus and methicillin-resistant S. aureus (MRSA) infected clinical samples, suggesting their further promising application in local anti-infection.