Nanoemulsions Containing a Coumarin-Rich Extract from Pterocaulon balansae (Asteraceae) for the Treatment of Ocular Acanthamoeba Keratitis

AAPS PharmSciTech. 2017 Apr;18(3):721-728. doi: 10.1208/s12249-016-0550-y. Epub 2016 May 25.

Abstract

This study describes the incorporation of a coumarin-rich extract from Pterocaulon balansae into nanoemulsions intended for the local treatment of ocular keratitis caused by Acanthamoeba. The n-hexane dewaxed extract of P. balansae was characterized by HPLC/PDA and UPLC/MS. The presence of four major coumarins was detected, where 5-methoxy-6,7-methylenedioxycoumarin was selected as a chemical marker. This extract was then incorporated into nanoemulsions composed of medium chain triglycerides and egg-lecithin, through spontaneous emulsification. Such a procedure yielded the formation of monodisperse nanoemulsions in a sub-300-nm range, regardless of the amount of extract incorporated (1.0-5.0 mg/mL). The amoebicidal activity against Acanthamoeba castellanii was both dose-dependent and incubation time-dependent. A reduction of 95% of trophozoite viability was detected after 24 h of incubation with a nanoemulsion at 1.25 mg/mL of coumarins, being a similar effect detected for chlorhexidine. These results suggest a potential of the formulations developed in this study as a new strategy for the treatment of ocular keratitis caused by Acanthamoeba.

Keywords: Acanthamoeba; Pterocaulon balansae; coumarins; nanoemulsion; ocular keratitis.

MeSH terms

  • Acanthamoeba Keratitis / drug therapy*
  • Acanthamoeba Keratitis / microbiology
  • Acanthamoeba castellanii / drug effects
  • Asteraceae / chemistry*
  • Benzodioxoles / chemistry
  • Coumarins / chemistry*
  • Coumarins / pharmacology*
  • Emulsions / chemistry*
  • Emulsions / pharmacology*
  • Hexanes / chemistry
  • Nanoparticles / chemistry*
  • Plant Extracts / chemistry
  • Plant Extracts / pharmacology

Substances

  • 5-methoxy-6,7-methylenedioxycoumarin
  • Benzodioxoles
  • Coumarins
  • Emulsions
  • Hexanes
  • Plant Extracts
  • n-hexane
  • coumarin