Enhanced antifungal efficacy of tebuconazole using gated pH-driven mesoporous nanoparticles

Int J Nanomedicine. 2014 May 23:9:2597-606. doi: 10.2147/IJN.S59654. eCollection 2014.

Abstract

pH-sensitive gated mesoporous silica nanoparticles have been synthesized. Increased extracellular pH and internalization into living yeast cells triggered molecular gate aperture and cargo release. Proper performance of the system was demonstrated with nanodevices loaded with fluorescein or with the antifungal agent tebuconazole. Interestingly, nanodevices loaded with tebuconazole significantly enhanced tebuconazole cytotoxicity. As alterations of acidic external pH are a key parameter in the onset of fungal vaginitis, this nanodevice could improve the treatment for vaginal mycoses.

Keywords: Saccharomyces cerevisiae; capped mesoporous nanoparticles; intracellular release; pH-responsive nanoparticles; tebuconazole loading.

MeSH terms

  • Antifungal Agents / administration & dosage
  • Antifungal Agents / chemistry
  • Cell Survival / drug effects
  • Delayed-Action Preparations / administration & dosage*
  • Delayed-Action Preparations / chemistry*
  • Diffusion
  • Drug Synergism
  • Hydrogen-Ion Concentration
  • Nanocapsules / administration & dosage
  • Nanocapsules / chemistry*
  • Nanocapsules / ultrastructure
  • Nanopores / ultrastructure*
  • Particle Size
  • Porosity
  • Saccharomyces cerevisiae / drug effects*
  • Saccharomyces cerevisiae / physiology
  • Triazoles / administration & dosage*
  • Triazoles / chemistry

Substances

  • Antifungal Agents
  • Delayed-Action Preparations
  • Nanocapsules
  • Triazoles
  • tebuconazole