Cefazolin-loaded polycaprolactone fibers produced via different electrospinning methods: Characterization, drug release and antibacterial effect

Eur J Pharm Sci. 2018 Nov 1:124:26-36. doi: 10.1016/j.ejps.2018.08.023. Epub 2018 Aug 18.

Abstract

Antibiotic containing polycaprolactone (PCL) fibers were produced by using three electrospinning methods: blend, emulsion and co-axial electrospinning (labeled as S1, S2 and S3, respectively). The profiles of drug release from three different systems were studied and antimicrobial properties of produced materials were evaluated. Morphology of the produced fibers was characterized and revealed that cefazolin-loaded PCL fibers had smaller diameter compared to neat PCL fibers, while the chemical interaction between the antibiotic and PCL showed that cefazolin neither had reacted with PCL phase, nor had degraded during the electrospinning process. The crystallinity and thermal characterization of fabricated fibers showed that the addition of cefazolin decreased the crystallinity of PCL. The results of the drug release behavior of the blend and co-axial electrospun fibers was on a higher level (~68% and ~43%, respectively) compared to the emulsion electrospun fibers (~5%), after a period of 30 days. The obtained data had the best fitting with the first order model and the Higuchi model, while the Korsmeyer-Peppas model showed a Pseudo-Fickian diffusion of the drug. Antibacterial evaluations showed that cefazolin-loaded PCL fibers had better effects on Staphylococcus aureus compared to Escherichia coli during the treatment period and that the effect of the emulsion fibers was notably weaker than the other two studied systems. The aim of the study was to test different systems for control drug release of different dynamics, which will be applied for prevent bacterial accumulation when indwelling urinary catheters, applied for different periods of time.

Keywords: Antibacterial activity; Cefazolin; Drug release; Drug release kinetics; Electrospinning; Polycaprolactone.

MeSH terms

  • Anti-Bacterial Agents / administration & dosage
  • Anti-Bacterial Agents / chemistry*
  • Cefazolin / administration & dosage
  • Cefazolin / chemistry*
  • Drug Compounding
  • Drug Liberation
  • Escherichia coli / drug effects
  • Escherichia coli / growth & development
  • Nanofibers / administration & dosage
  • Nanofibers / chemistry*
  • Polyesters / administration & dosage
  • Polyesters / chemistry*
  • Staphylococcus aureus / drug effects
  • Staphylococcus aureus / growth & development

Substances

  • Anti-Bacterial Agents
  • Polyesters
  • polycaprolactone
  • Cefazolin