Impact of PCL nanofiber mat structural properties on hydrophilic drug release and antibacterial activity on periodontal pathogens

Eur J Pharm Sci. 2018 Sep 15:122:347-358. doi: 10.1016/j.ejps.2018.07.024. Epub 2018 Jul 12.

Abstract

Electrospinning enables to design and manufacture novel drug delivery systems capable of advancing the local antibacterial therapy. In this study, two hydrophilic drugs - metronidazole and ciprofloxacin hydrochloride - were loaded both individually and in combination into hydrophobic poly(ε-caprolactone) (PCL) matrix using electrospinning. We aimed to develop prolonged release drug delivery systems suitable for the treatment of periodontal diseases and understand how different rarely studied structural features, such as nanofiber mat thickness, surface area, wettability, together with intrinsic properties, like solid state and localization of incorporated drugs in nanofibers, affect the drug release. Furthermore, the safety of nanofiber mats was assessed in vitro on fibroblasts, and their antibacterial activity was tested on selected strains of periodontopathogenic bacteria. The results showed that the structural properties of nanofiber mat are crucial in particular drug-polymer combinations, affecting the drug release and consequently the antibacterial activity. The hydrophobicity of a PCL nanofiber mat and its thickness are the key characteristics in prolonged hydrophilic drug release, but only when wetting is the rate-limiting step for the drug release. Combination of drugs showed beneficial effects by inhibiting the growth of all tested pathogenic bacterial strains important in periodontal diseases.

Keywords: Antibacterial activity; Drug release mechanism; Hydrophilic drug; Nanofibers; Periodontopathogenic bacteria; Wettability.

MeSH terms

  • Anti-Bacterial Agents* / administration & dosage
  • Anti-Bacterial Agents* / chemistry
  • Bacteria / drug effects
  • Bacteria / growth & development
  • Ciprofloxacin* / administration & dosage
  • Ciprofloxacin* / chemistry
  • Drug Liberation
  • Hydrophobic and Hydrophilic Interactions
  • Metronidazole* / administration & dosage
  • Metronidazole* / chemistry
  • Nanofibers* / administration & dosage
  • Nanofibers* / chemistry
  • Periodontium / microbiology
  • Polyesters* / administration & dosage
  • Polyesters* / chemistry

Substances

  • Anti-Bacterial Agents
  • Polyesters
  • Metronidazole
  • polycaprolactone
  • Ciprofloxacin