Endogenously triggered electrospun fibres for tailored and controlled antibiotic release

J Biomater Sci Polym Ed. 2013;24(11):1305-19. doi: 10.1080/09205063.2012.757725. Epub 2013 Jan 11.

Abstract

The study was aimed at assessing the potential of enzyme-embedded antibiotic-releasing polycaprolactone (PCL)-based electrospun fibres for tunable drug delivery. This was attempted by incorporation of gentamicin sulphate (GS) in the biocompatible polymer (PCL) matrix, with the degradation of the matrix being ensured by co-impregnating a polymer-degrading enzyme (lipase). Single phase solutions were obtained by hydrophobic ion pairing of GS and surfactant coating of lipase with an anionic surfactant, docusate sodium salt Aerosol OT (AOT). By electrospinning the solution, we could produce PCL fibres containing 11% (w/w) GS-AOT and 28 U (w/w) lipase-AOT. However, sustained release of GS was not obtained. FESEM analysis showed that the fibres did not undergo the expected degradation. Subsequent experiments with unmodified lipase gave satisfactory results; the polymer underwent degradation displaying characteristic perforations in the fibres, suggestive of 'endo-attack'. By modulating the concentrations of lipase (1 to 28 U, w/w), we could obtain GS release rates that varied from 0.53 to 32 mg/ml/d. Accordingly, the lifetime of the fibres could be tuned (10 h to 25 days). The fibres showed excellent antibacterial activity against Staphylococcus aureus throughout their lifetime.

MeSH terms

  • Anti-Bacterial Agents / administration & dosage*
  • Anti-Bacterial Agents / pharmacokinetics
  • Candida / drug effects
  • Candida / growth & development
  • Delayed-Action Preparations
  • Drug Carriers / chemical synthesis*
  • Drug Carriers / chemistry
  • Drug Carriers / pharmacokinetics*
  • Electrochemical Techniques
  • Gentamicins / administration & dosage
  • Gentamicins / pharmacokinetics
  • Materials Testing
  • Microbial Sensitivity Tests
  • Microscopy, Atomic Force
  • Nanofibers / chemistry*
  • Polyesters / chemical synthesis
  • Polyesters / chemistry*
  • Polyesters / pharmacokinetics
  • Polymers / chemical synthesis
  • Polymers / chemistry
  • Polymers / pharmacokinetics
  • Staphylococcus aureus / drug effects
  • Staphylococcus aureus / growth & development

Substances

  • Anti-Bacterial Agents
  • Delayed-Action Preparations
  • Drug Carriers
  • Gentamicins
  • Polyesters
  • Polymers
  • polycaprolactone