Studies on cationic ocular emulsions containing bipartitioned oil droplets to codeliver cyclosporin A and etodolac

Nanomedicine (Lond). 2024;19(12):1035-1050. doi: 10.2217/nnm-2023-0364. Epub 2024 Apr 30.

Abstract

Background: To prepare ocular emulsions containing bipartitioned oil droplets to entrap cyclosporin A (0.05% w/w) and etodolac (0.2% w/w) by using castor, olive and silicon oils. Methods: The physicochemical characterizations of prepared emulsions were performed. The drug's biodistribution profiles and pharmacokinetic parameters from emulsions were checked using the ultraperformance liquid chromatography-tandem mass spectrometry method in the ocular tissues of the healthy rabbit eye model. Results: The emulsions displayed 365.13 ± 7.21 nm size and 26.45 ± 2.09 mV zeta potential. The ferrying of two drugs after releasing from emulsions occurred across corneal/conjunctival tissues to enter the vitreous and sclera following a single drop administration into the rabbit's eyes. Conclusion: The dual drug-loaded emulsions were more likely to produce synergistic anti-inflammatory activity for managing moderate-to-severe dry eye disease.

Keywords: anti-inflammatory; cyclosporin A; dry eye disease; etodolac; nanosized emulsions.

Plain language summary

[Box: see text].

MeSH terms

  • Animals
  • Castor Oil / chemistry
  • Cations / chemistry
  • Cornea / drug effects
  • Cornea / metabolism
  • Cyclosporine* / administration & dosage
  • Cyclosporine* / chemistry
  • Cyclosporine* / pharmacokinetics
  • Drug Liberation
  • Dry Eye Syndromes / drug therapy
  • Emulsions* / chemistry
  • Etodolac* / chemistry
  • Humans
  • Olive Oil / chemistry
  • Ophthalmic Solutions / chemistry
  • Particle Size
  • Rabbits
  • Silicone Oils / chemistry
  • Tissue Distribution

Substances

  • Emulsions
  • Cyclosporine
  • Etodolac
  • Castor Oil
  • Cations
  • Silicone Oils
  • Olive Oil
  • Ophthalmic Solutions