Efficacy of Poly-Lactic-Co-Glycolic Acid Micro- and Nanoparticles of Ciprofloxacin Against Bacterial Biofilms

J Pharm Sci. 2016 Oct;105(10):3115-3122. doi: 10.1016/j.xphs.2016.06.022. Epub 2016 Aug 9.

Abstract

Bacterial biofilms are associated with a number of recurring infectious diseases and are a major cause for antibiotic resistance. Despite the broad use of polymeric microparticles and nanoparticles in biomedical research, it is not clear which particle size is more effective against biofilms. The purpose of this study was to evaluate the efficacy of sustained release poly-lactic-co-glycolic acid (PLGA) micro- and nanoparticles containing ciprofloxacin against biofilms of Staphylococcus aureus and Pseudomonas aeruginosa. The PLGA particles were prepared by the double emulsion solvent evaporation method. The resulting microparticles (12 μm) and nanoparticles (300 nm) contained drug loads of 7.3% and 4.5% (wt/wt) ciprofloxacin, respectively. Drug release was complete within 1 week following comparable release profiles for both particle sizes. Micro- and nanoparticles demonstrated a similar in vitro antibiofilm performance against mature P aeruginosa and S aureus with marked differences between the 2 strains. The sustained release of ciprofloxacin from micro- and nanoparticles over 6 days was equally effective as the continuous treatment with ciprofloxacin solution over the same period resulting in the eradication of culturable S aureus suggesting that reformulation of ciprofloxacin as sustained release PLGA micro- and nanoparticles might be valuable formulation approaches for the treatment of biofilms.

Keywords: controlled release; drug resistance; encapsulation; microparticles; nanoparticles; poly(lactic/glycolic) acid (PLGA or PLA); polymeric drug carrier.

MeSH terms

  • Anti-Bacterial Agents / administration & dosage*
  • Biofilms / drug effects*
  • Biofilms / growth & development
  • Ciprofloxacin / administration & dosage*
  • Drug Carriers / administration & dosage
  • Lactic Acid / administration & dosage*
  • Microbial Sensitivity Tests / methods
  • Nanoparticles / administration & dosage*
  • Particle Size
  • Polyglycolic Acid / administration & dosage*
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Staphylococcus aureus / drug effects
  • Treatment Outcome

Substances

  • Anti-Bacterial Agents
  • Drug Carriers
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Polyglycolic Acid
  • Lactic Acid
  • Ciprofloxacin