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Ahmed TA, Alzahrani MM, Sirwi A, et al. The Antifungal and Ocular Permeation of Ketoconazole from Ophthalmic Formulations Containing Trans-Ethosomes Nanoparticles. Pharmaceutics. 2021;13(2)doi: 10.3390/pharmaceutics13020151.
Ahmed, T. A., Alzahrani, M. M., Sirwi, A., & Alhakamy, N. A. (2021). The Antifungal and Ocular Permeation of Ketoconazole from Ophthalmic Formulations Containing Trans-Ethosomes Nanoparticles. Pharmaceutics, 13(2), . https://doi.org/10.3390/pharmaceutics13020151
Ahmed, Tarek A, et al. "The Antifungal and Ocular Permeation of Ketoconazole from Ophthalmic Formulations Containing Trans-Ethosomes Nanoparticles." Pharmaceutics vol. 13,2 (2021). doi: https://doi.org/10.3390/pharmaceutics13020151
Ahmed TA, Alzahrani MM, Sirwi A, Alhakamy NA. The Antifungal and Ocular Permeation of Ketoconazole from Ophthalmic Formulations Containing Trans-Ethosomes Nanoparticles. Pharmaceutics. 2021 Jan 24;13(2). doi: 10.3390/pharmaceutics13020151. PMID: 33498849; PMCID: PMC7912274.
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Pharmaceutics. 2021 Jan 24;13(2). doi: 10.3390/pharmaceutics13020151.

The Antifungal and Ocular Permeation of Ketoconazole from Ophthalmic Formulations Containing Trans-Ethosomes Nanoparticles.

Pharmaceutics

Tarek A Ahmed, Maram M Alzahrani, Alaa Sirwi, Nabil A Alhakamy

Affiliations

  1. Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi Arabia.
  2. Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Al-Azhar University, Cairo 11651, Egypt.
  3. Department of Pharmaceutics, College of Pharmacy, Umm Al-Qura University, Makkah 21955, Saudi Arabia.
  4. Department of Natural Products, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi Arabia.

PMID: 33498849 PMCID: PMC7912274 DOI: 10.3390/pharmaceutics13020151

Abstract

Ketoconazole (KET), a synthetic imidazole broad-spectrum antifungal agent, is characterized by its poor aqueous solubility and high molecular weight, which might hamper its corneal permeation. The aim was to develop an ophthalmic formulation loaded with optimized trans-ethosomal vesicles to enhance KET ocular permeation, antifungal activity, rapid drug drainage, and short elimination half-life. Four formulation factors affecting the vesicles' size, zeta potential, entrapment efficiency, and flexibility of the trans-ethosomes formulations were optimized. The optimum formulation was characterized, and their morphological and antifungal activity were studied. Different ophthalmic formulations loaded with the optimized vesicles were prepared and characterized. The ocular irritation and in vivo corneal permeation were investigated. Results revealed that the drug-to-phospholipid-molar ratio, the percentage of edge activator, the percentage of ethanol, and the percentage of stearyl amine significantly affect the characteristics of the vesicles. The optimized vesicles were spherical and showed an average size of 151.34 ± 8.73 nm, a zeta potential value of +34.82 ± 2.64 mV, an entrapment efficiency of 94.97 ± 5.41%, and flexibility of 95.44 ± 4.33%. The antifungal activity of KET was significantly improved following treatment with the optimized vesicles. The developed in situ gel formulations were found to be nonirritating to the cornea. The trans-ethosomes vesicles were able to penetrate deeper into the posterior eye segment without any toxic effects. Accordingly, the in situ developed gel formulation loaded with KET trans-ethosomes vesicles represents a promising ocular delivery system for the treatment of deep fungal eye infections.

Keywords: antifungal; in situ gel; ketoconazole; ocular permeation; optimization; trans-ethosomes

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