Ciprofloxacin-loaded lipid-core nanocapsules as mucus penetrating drug delivery system intended for the treatment of bacterial infections in cystic fibrosis

Int J Pharm. 2017 Jul 15;527(1-2):92-102. doi: 10.1016/j.ijpharm.2017.05.013. Epub 2017 May 10.

Abstract

Treatment of bacterial airway infections is essential for cystic fibrosis therapy. However, effectiveness of antibacterial treatment is limited as bacteria inside the mucus are protected from antibiotics and immune response. To overcome this biological barrier, ciprofloxacin was loaded into lipid-core nanocapsules (LNC) for high mucus permeability, sustained release and antibacterial activity. Ciprofloxacin-loaded LNC with a mean size of 180nm showed a by 50% increased drug permeation through mucus. In bacterial growth assays, the drug in the LNC had similar minimum inhibitory concentrations as the free drug in P. aeruginosa and S. aureus. Interestingly, formation of biofilm-like aggregates, which were observed for S. aureus treated with free ciprofloxacin, was avoided by exposure to LNC. With the combined advantages over the non-encapsulated drug, ciprofloxacin-loaded LNC represent a promising drug delivery system with the prospect of an improved antibiotic therapy in cystic fibrosis.

Keywords: Biofilm; Nanomedicines; Polymeric lipid-core nanocapsules; Pseudomonas aeruginosa; Respiratory mucus; Staphylococcus aureus.

MeSH terms

  • Bacterial Infections / drug therapy*
  • Ciprofloxacin / administration & dosage*
  • Cystic Fibrosis / microbiology*
  • Delayed-Action Preparations
  • Drug Carriers / chemistry*
  • Lipids / chemistry
  • Mucus / microbiology
  • Nanocapsules / chemistry*
  • Pseudomonas aeruginosa / drug effects
  • Staphylococcus aureus / drug effects

Substances

  • Delayed-Action Preparations
  • Drug Carriers
  • Lipids
  • Nanocapsules
  • Ciprofloxacin