Development of antifungal fibrous ocular insert using freeze-drying technique.
Autor: | Teba HE; Department of Pharmaceutics, Faculty of Pharmacy and Drug Manufacturing, Misr University for Science and Technology, 12566, 6th of October, Giza, Egypt., Khalil IA; Department of Pharmaceutics, Faculty of Pharmacy and Drug Manufacturing, Misr University for Science and Technology, 12566, 6th of October, Giza, Egypt., Gebreel RM; Department of Pharmaceutics, Faculty of Pharmacy and Drug Manufacturing, Misr University for Science and Technology, 12566, 6th of October, Giza, Egypt., Fahmy LI; Department of Microbiology and Immunology, Faculty of Pharmacy, October University for Modern Sciences and Arts, 12451, 6th of October, Giza, Egypt., Sorogy HME; Department of Pharmaceutics, Faculty of Pharmacy and Drug Manufacturing, Misr University for Science and Technology, 12566, 6th of October, Giza, Egypt. heba.moner@must.edu.eg. |
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Jazyk: | angličtina |
Zdroj: | Drug delivery and translational research [Drug Deliv Transl Res] 2024 Sep; Vol. 14 (9), pp. 2520-2538. Date of Electronic Publication: 2024 Feb 16. |
DOI: | 10.1007/s13346-024-01527-8 |
Abstrakt: | Candida species is one of the pathogenic fungi of the eye responsible for keratitis that frequently causes vision impairment and blindness. Effective treatment requires long-term use of antifungal drugs, which is opposed by the defensive mechanisms of the eye and inadequate corneal penetration. The objective of this study was to develop a carrier for prolonged ocular application of fluconazole (FLZ) to treat keratitis. FLZ was encapsulated into chitosan fibrous matrices (F1-F4) using different chitosan concentrations (0.02, 0.1, 0.5, and 1%w/v, respectively) by freeze-drying as a single-step technique. Studying the morphology and surface properties of the inserts revealed a porous matrix with fibrous features with a large surface area. Thermal stability and chemical compatibility were confirmed by DSC/TGA/DTA and FT-IR, respectively. Loading capacity (LC) and entrapment efficiency (EE) were determined. According to the in vitro release study, F4 (0.11 mg mg -1 LC and 87.53% EE) was selected as the optimum insert because it had the most sustained release, with 15.85% burst release followed by 75.62% release within 12 h. Ex vivo corneal permeation study revealed a 1.2-fold increase in FLZ permeation from F4 compared to FLZ aqueous solution. Also, in the in vivo pharmacokinetic study in rabbits, F4 increased the AUC (© 2024. The Author(s).) |
Databáze: | MEDLINE |
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