Penicillin-bound polyacrylate nanoparticles: Restoring the activity of β-lactam antibiotics against MRSA

This report describes the preparation of antibacterially active emulsified polyacrylate nanoparticles in which a penicillin antibiotic is covalently conjugated onto the polymeric framework. These nanoparticles were prepared in water by emulsion polymerization of an acrylated penicillin analogue pre-dissolved in a 7:3 (w:w) mixture of butyl acrylate and styrene in the presence of sodium dodecyl sulfate (surfactant) and potassium persulfate (radical initiator). Dynamic light scattering analysis and atomic force microscopy images show that the emulsions contain nanoparticles of approximately 40 nm in diameter. The nanoparticles have equipotent in vitro antibacterial properties against methicillin-susceptible and methicillin-resistant forms of Staphylococcus aureus and indefinite stability toward β-lactamase.

Polyacrylate nanoparticles bearing penicillin antibiotics attached to the polymeric matrix have been prepared in water by emulsion polymerization. The nanoparticles are uniformly 25–40 nm in diameter and are stable over a wide range of pH values and in blood serum. The nanoparticle emulsions display potent in vitro activity against Staphylococcus aureus and retain their full antibiotic capabilities against β-lactamase producing, methicillin-resistant S. aureus, suggesting their use as therapies for drug-resistant bacterial infections.Figure optionsDownload as PowerPoint slide