Triclosan loaded electrospun nanofibers based on a cyclodextrin polymer and chitosan polyelectrolyte complex

Int J Pharm. 2016 Nov 20;513(1-2):483-495. doi: 10.1016/j.ijpharm.2016.09.060. Epub 2016 Sep 21.

Abstract

This work focuses on the relevance of antibacterial nanofibers based on a polyelectrolyte complex formed between positively charged chitosan (CHT) and an anionic hydroxypropyl betacyclodextrin (CD)-citric acid polymer (PCD) complexing triclosan (TCL). The study of PCD/TCL inclusion complex and its release in dynamic conditions, a cytocompatibility study, and finally the antibacterial activity assessment were studied. The fibers were obtained by electrospinning a solution containing chitosan mixed with PCD/TCL inclusion complex. CHT/TCL and CHT-CD/TCL were also prepared as control samples. The TCL loaded nanofibers were analyzed by Scanning Electron Microscopy (SEM), Fourier Transformed Infrared spectroscopy (FTIR) and X-Ray Diffraction (XRD). Nanofibers stability and swelling behavior in aqueous medium were pH and CHT:PCD weight ratio dependent. Such results confirmed that CHT and PCD interacted through ionic interactions, forming a polyelectrolyte complex. A high PCD content in addition to a thermal post treatment at 90°C were necessary to reach a nanofibers stability during 15days in soft acidic conditions, at pH=5.5. In dynamic conditions (USP IV system), a prolonged release of TCL with a reduced burst effect was observed on CHT-PCD polyelectrolyte complex based fibers compared to CHT-CD nanofibers. These results were confirmed by a microbiology study showing prolonged antibacterial activity of the nanofibers against Escherichia coli and Staphylococcus aureus. Such results could be explained by the fact that the stability of the polyelectrolyte CHT-PCD complex in the nanofibers matrix prevented the diffusion of the PCD/triclosan inclusion complex in the supernatant, on the contrary of the similar system including cyclodextrin in its monomeric form.

Keywords: Antibacterial activity; Chitosan; Chitosan (PubChem CID: 71853); Controlled release; Cyclodextrin polymer; Cycloheptaamylose, beta-cyclodextrin (PubChem CID: 101136808); Electrospinning; Nanofibers; Polyelectrolyte complex; Polyethylene oxide (PubChem SID: 160698351); Triclosan; Triclosan (PubChem CID: 5564).

MeSH terms

  • Animals
  • Anti-Bacterial Agents / administration & dosage
  • Anti-Bacterial Agents / chemistry*
  • Cell Line
  • Cell Survival / drug effects
  • Cellulose / administration & dosage
  • Cellulose / chemistry
  • Chitosan / administration & dosage
  • Chitosan / chemistry
  • Cyclodextrins / administration & dosage
  • Cyclodextrins / chemistry
  • Drug Liberation
  • Drug Stability
  • Escherichia coli / drug effects
  • Mice
  • Nanofibers / administration & dosage
  • Nanofibers / chemistry*
  • Polyelectrolytes / administration & dosage
  • Polyelectrolytes / chemistry
  • Solubility
  • Staphylococcus aureus / drug effects
  • Technology, Pharmaceutical
  • Triclosan / administration & dosage
  • Triclosan / chemistry*

Substances

  • Anti-Bacterial Agents
  • Cyclodextrins
  • Polyelectrolytes
  • cyclodextrin polymer
  • Triclosan
  • Cellulose
  • Chitosan