title: Antibiotic-conjugated polyacrylate nanoparticles: new opportunities for development of anti-MRSA agents.
abstract: This report describes the preparation of polyacrylate nanoparticles in which an N-thiolated beta-lactam antibiotic is covalently conjugated onto the polymer framework. These nanoparticles are formed in water by emulsion polymerization of an acrylated antibiotic pre-dissolved in a liquid acrylate monomer (or mixture of co-monomers) in the presence of sodium dodecyl sulfate as a surfactant and potassium persulfate as a radical initiator. Dynamic light scattering analysis and electron microscopy images of these emulsions show that the nanoparticles are approximately 40 nm in diameter. The emulsions have potent in vitro antibacterial properties against methicillin-resistant Staphylococcus aureus and have improved bioactivity relative to the non-polymerized form of the antibiotic. A unique feature of this methodology is the ability to incorporate water-insoluble drugs directly into the nanoparticle framework without the need for post-synthetic modification. Additionally, the antibiotic properties of the nanoparticles can be modulated by changing the length or location of the acrylate linker on the drug monomer.
authors.affiliation: Department of Chemistry, 4202 East Fowler Avenue, CHE 207, University of South Florida, Tampa, FL 33620, USA. eturos@shell.cas.usf.edu
authors.forename: Edward
authors.initials: E
authors.lastname: Turos
authors.forename: Jeung-Yeop
authors.initials: JY
authors.lastname: Shim
authors.forename: Yang
authors.initials: Y
authors.lastname: Wang
authors.forename: Kerriann
authors.initials: K
authors.lastname: Greenhalgh
authors.forename: G Suresh Kumar
authors.initials: GS
authors.lastname: Reddy
authors.forename: Sonja
authors.initials: S
authors.lastname: Dickey
authors.forename: Daniel V
authors.initials: DV
authors.lastname: Lim
mesh_terms: D000180:Acrylic Resins / Q000737:chemistry; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004655:Emulsions; D016106:Methicillin Resistance; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D017680:Potassium Compounds / Q000737:chemistry; D012967:Sodium Dodecyl Sulfate / Q000737:chemistry; D013211:Staphylococcus aureus / Q000187:drug effects*; D013431:Sulfates / Q000737:chemistry; D013438:Sulfhydryl Compounds / Q000737:chemistry; D014867:Water / Q000737:chemistry; D047090:beta-Lactams / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D000180:Acrylic Resins; D000900:Anti-Bacterial Agents; D004655:Emulsions; D017680:Potassium Compounds; D013431:Sulfates; D013438:Sulfhydryl Compounds; D047090:beta-Lactams; D014867:Water; D012967:Sodium Dodecyl Sulfate; C006903:carbopol 940; C009007:potassium persulfate