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Voriconazole Ternary Micellar Systems for the Treatment of Ocular Mycosis: Statistical Optimization and In Vivo Evaluation.

Abstract
Voriconazole (VRC) is a broad spectrum, second generation triazole antifungal. The main use of VRC is via the oral and intravenous route. The study aimed to formulate VRC into ternary micellar systems (TMSs) for the topical treatment of ocular mycosis. TMSs were successfully prepared by water addition/solvent evaporation method, applying a 3-factor D-optimal design. The numerical optimization process suggested an optimal formula (OTMS) composed of total Pluronics to drug weight ratio of 22.89: 1, 1:1 weight ratio of Pluronic® P123 and F68, and 2% w/v of Labrasol. OTMS had high solubilization efficiency of 98.0%, small micellar size of 21.8 nm and suitable zeta potential and polydispersity index values of -9.0 mV and 0.261, respectively. OTMS exhibited acceptable stability for 3 months. Transmission electron microscopy demonstrated the spherical morphology of micelles. OTMS was expected to cause no ocular irritation or blurring in vision as reflected by pH and refractive index measurements. The histopathological study revealed the safety of OTMS for ocular use. The fungal susceptibility testing using Candida albicans demonstrated the superiority of OTMS to VRC suspension, with greater and more durable growth inhibition. Therefore, ocular application of optimized VRC-loaded TMSs can be a promising treatment for ocular mycosis.
AuthorsAbdurrahman Muhammad Fahmy, Mariam Hassan, Doaa Ahmed El-Setouhy, Saadia Ahmed Tayel, Abdulaziz Mohsen Al-Mahallawi
JournalJournal of pharmaceutical sciences (J Pharm Sci) Vol. 110 Issue 5 Pg. 2130-2138 (05 2021) ISSN: 1520-6017 [Electronic] United States
PMID33346033 (Publication Type: Journal Article)
CopyrightCopyright © 2020 American Pharmacists Association®. Published by Elsevier Inc. All rights reserved.
Chemical References
  • Antifungal Agents
  • Drug Carriers
  • Micelles
  • Voriconazole
Topics
  • Antifungal Agents (therapeutic use)
  • Drug Carriers (therapeutic use)
  • Drug Delivery Systems
  • Eye Infections, Fungal (drug therapy)
  • Humans
  • Micelles
  • Particle Size
  • Voriconazole (therapeutic use)

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