Microfluidic ocular formulation of voriconazole designed for hospital production

Louise Stinat1,2, Marie Bonnin1,3, Jean-Christophe Gimel1,3

  • 1Université d'Angers, CHU Angers, INSERM, CNRS, MINT, SFR, ICAT, F-49000, Angers, France.

Insights

A new oil-in-water nanoemulsion formulation for voriconazole offers an effective alternative for fungal keratitis treatment. This ocular delivery system demonstrates comparable efficacy to existing hospital preparations.

Area of Science:

  • Ophthalmology
  • Pharmaceutics
  • Mycology

Background:

  • Fungal keratitis is a severe corneal infection with limited treatment options.
  • Current voriconazole formulations for ocular use are hospital preparations with drawbacks.
  • There is a need for a dedicated, effective ocular formulation for voriconazole.

Purpose of the Study:

  • To design and characterize a novel oil-in-water nanoemulsion for ocular delivery of voriconazole.
  • To evaluate the efficacy of the developed nanoemulsion against key fungal species causing keratitis.

Main Methods:

  • Formulation of a 0.4% voriconazole nanoemulsion using the phase inversion composition method and microfluidic technology.
  • Characterization of nanoemulsion properties including droplet size, zeta potential, pH, and osmolality.
  • In vitro minimal inhibitory concentration (MIC) testing against Aspergillus and Fusarium species.

Main Results:

  • A stable voriconazole nanoemulsion with a mean droplet size of approximately 100 nm and negative zeta potential was successfully prepared.
  • The formulation demonstrated stability after pH and osmolality adjustments.
  • Voriconazole was found to preferentially partition into the micellar compartment of the nanoemulsion.
  • In vitro MIC tests showed the nanoemulsion was as effective as the current 1% hospital preparation against tested fungal strains.

Conclusions:

  • A novel voriconazole oil-in-water nanoemulsion is a viable and effective formulation for ocular delivery.
  • This formulation addresses the limitations of current hospital preparations for fungal keratitis.
  • The microfluidic preparation method is suitable for hospital transposition, offering a promising therapeutic option.

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