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Ocular Inserts of Voriconazole-Loaded Proniosomal Gels: Formulation, Evaluation and Microbiological Studies

Ghada Ahmed El-Emam1, Germeen N S Girgis1, Mohamed M Adel El-Sokkary2

  • 1Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura, Egypt.

International Journal of Nanomedicine
|October 29, 2020
PubMed
Abstract

Insights

This study developed novel voriconazole (VRC) niosomal ophthalmic inserts (VRC-PNs Ocu) for improved fungal infection treatment. The new formulation demonstrated enhanced antifungal activity and stability, offering a promising alternative for ocular fungal infections.

Area of Science:

  • Ophthalmology
  • Nanotechnology
  • Pharmacology

Background:

  • Voriconazole (VRC) is a broad-spectrum antifungal agent crucial for treating fungal infections, especially fungal keratitis.
  • Short biological half-life necessitates frequent dosing, impacting patient compliance.
  • Niosomal delivery systems offer a potential solution to improve VRC's pharmacokinetic profile and therapeutic efficacy.

Purpose of the Study:

  • To develop and characterize voriconazole-loaded niosomal proniosomes (VRC-PNs).
  • To formulate VRC-PNs into stable ophthalmic inserts (VRC-PNs Ocu) for sustained ocular drug delivery.
  • To evaluate the in vitro antifungal activity and stability of the developed VRC-PNs Ocu.

Main Methods:

  • VRC-PNs were prepared using the coacervation technique and characterized for entrapment efficiency, size, and zeta potential.
  • Niosomal inserts (VRC-PNs Ocu) were formulated using hydroxypropyl methylcellulose and carbopol.
  • In vitro release kinetics, stability under different temperatures, and antifungal activity against Candida albicans and Aspergillus nidulans were assessed.

Main Results:

  • Optimized VRC-PNs showed high entrapment efficiency (87.4%) and suitable nano-range size with a negative zeta potential.
  • Characterization confirmed drug encapsulation within nanovesicles.
  • VRC-PNs Ocu exhibited significant antifungal activity and stability over six months of refrigerated storage, outperforming free VRC and commercial natamycin eye drops.

Conclusions:

  • VRC-PNs Ocu represent a stable, sustained-release topical ocular nanoparticulate system.
  • This formulation holds promise for effectively managing ocular fungal infections.
  • The developed system could enhance patient compliance through reduced dosing frequency.
Keywords:
antifungal activitycoacervationocusertproniosomesvoriconazole

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