Chitosan-coated nanoparticles enhanced lung pharmacokinetic profile of voriconazole upon pulmonary delivery in mice

Nanomedicine (Lond). 2018 Mar 1;13(5):501-520. doi: 10.2217/nnm-2017-0291. Epub 2018 Jan 31.

Abstract

Aim: Chitosan-coated polylactic-co-glycolic acid nanoparticles of voriconazole (VChNP) were developed to increase residence time and provide sustained drug release locally to treat recurrent lung-fungal infection.

Materials & methods: VChNP has been developed using a simple, unique technique and characterized. Pharmacokinetics, lung deposition with time and gamma imaging were conducted with optimized formulations.

Results: The deposition of fluorescein isothiocyanate-labeled VChNP in lung was confirmed by confocal microscopy. Gamma-scintigraphic images showed that Tc-99m-labeled VChNP had better pulmonary retention for longer period than that of noncoated formulation. Drastic improvement in pharmacokinetic profile of VChNP than noncoated formulation was observed.

Conclusion: Thus, VChNP may be useful for effective pulmonary delivery with improved bioavailability. Such chitosan-coated nanoparticles may open up a new avenue for efficacious treatment of lung-fungal infection.

Keywords: aerodynamic diameter; chitosan-coated nanoparticles; gamma imaging; lung deposition; mucoadhesive; pharmacokinetics; voriconazole.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Inhalation
  • Animals
  • Antifungal Agents / administration & dosage
  • Antifungal Agents / chemistry*
  • Antifungal Agents / pharmacokinetics
  • Biological Availability
  • Chitosan / chemistry*
  • Drug Carriers / chemistry*
  • Drug Compounding
  • Drug Liberation
  • Female
  • Humans
  • Lung / metabolism*
  • Lung Diseases, Fungal / drug therapy*
  • Male
  • Mice
  • Nanoparticles / chemistry*
  • Particle Size
  • Polylactic Acid-Polyglycolic Acid Copolymer / chemistry
  • Surface Properties
  • Tissue Distribution
  • Voriconazole / administration & dosage
  • Voriconazole / chemistry*
  • Voriconazole / pharmacokinetics

Substances

  • Antifungal Agents
  • Drug Carriers
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Chitosan
  • Voriconazole