Cited by 45Advanced Drug Delivery SystemsOcular Infections and TreatmentsSurfactants and Colloidal Systems

Voriconazole ternary micellar systems for the treatment of ocular mycosis: statistical optimization and in vivo evaluation

Fahmy, Abdurrahman Muhammad, Hassan, Mariam, El-Setouhy, Doaa Ahmed, Tayel, Saadia Ahmed, Al-mahallawi, Abdulaziz Mohsen·2021·Journal of Pharmaceutical Sciences

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.

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Crossref · 10.1016/j.xphs.2020.12.013

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Authors
Fahmy, A. M., Hassan, M., El-Setouhy, D. A., Tayel, S. A., & Al-mahallawi, A. M.
Affiliations
Cairo University (EG)
Corresponding author
Fahmy, Abdurrahman Muhammad
Venue
Journal of Pharmaceutical Sciences
Publisher
Elsevier BV
Published
2021-05
Volume
110
Issue
5
Pages
2130-2138
ISSN
0022-3549 (ISSN-L)
OpenAlex
W3113110058
Cited by
45
References
66
Citations by year
2026: 4 · 2025: 12 · 2024: 12 · 2023: 6 · 2022: 5 · 2021: 6
FWCI
1.66
Type
journal article
Language
en
Open access
closed
Locations
  • Journal of Pharmaceutical Sciences (publishedVersion)
  • PubMed (publishedVersion)
Topics
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
  • Health Sciences › Medicine › Ophthalmology › Ocular Infections and Treatments
  • Physical Sciences › Chemistry › Organic Chemistry › Surfactants and Colloidal Systems
Keywords
voriconazole, ocular mycosis, Pluronic P123, poloxamer 188, Labrasol, topical ocular drug delivery, antifungal formulation, Candida albicans, micellar stability, formulation optimization
MeSH terms
Antifungal Agents, Drug Carriers, Humans, Micelles, Particle Size, Eye Infections, Fungal, Drug Delivery Systems, Voriconazole

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