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Development of antifungal fibrous ocular insert using freeze-drying technique
Hoda E Teba1, Islam A Khalil1, Rana M Gebreel1
1Department of Pharmaceutics, Faculty of Pharmacy and Drug Manufacturing, Misr University for Science and Technology, 12566, 6th of October, Giza, Egypt.
Drug Delivery and Translational Research
|February 17, 2024
Summary
This study developed a novel chitosan fibrous insert for sustained delivery of fluconazole (FLZ) to treat fungal keratitis. The optimized insert demonstrated enhanced corneal penetration and prolonged drug release, showing promise for effective ocular infection treatment.
Area of Science:
- Ophthalmology
- Pharmaceutics
- Biomaterials Science
Background:
- Fungal keratitis, often caused by Candida species, leads to significant vision impairment and blindness.
- Current antifungal treatments for ocular infections face challenges due to the eye's defense mechanisms and poor drug penetration.
- Prolonged drug delivery systems are needed to overcome these limitations and improve therapeutic outcomes.
Purpose of the Study:
- To develop and evaluate a chitosan-based fibrous matrix for sustained ocular delivery of fluconazole (FLZ).
- To assess the physicochemical properties, drug release kinetics, and ocular penetration of the developed formulation.
- To investigate the in vivo pharmacokinetics and safety of the fluconazole-loaded chitosan insert.
Main Methods:
- Fluconazole (FLZ) was encapsulated into chitosan fibrous matrices using freeze-drying.
- Formulations were characterized for morphology, thermal stability, chemical compatibility, loading capacity (LC), and entrapment efficiency (EE).
- In vitro drug release, ex vivo corneal permeation, in vivo pharmacokinetics in rabbits, and cytotoxicity assays were performed.
Main Results:
- The optimized F4 formulation exhibited a porous, fibrous structure with high surface area, LC (0.11 mg mg⁻¹), and EE (87.53%).
- F4 showed sustained drug release over 12 hours (75.62% release after 15.85% burst release) and a 1.2-fold increase in corneal permeation.
- In vivo studies demonstrated a 9.3-fold increase in AUC₀₋₈ and sustained therapeutic concentrations of FLZ in rabbit aqueous humor, with no observed cytotoxicity.
Conclusions:
- Freeze-dried fluconazole-loaded chitosan fibrous inserts represent a promising strategy for sustained ocular drug delivery.
- The developed formulation enhances corneal penetration and maintains therapeutic drug levels, offering a potential new treatment for fungal keratitis.
- The safety and biocompatibility of the chitosan insert support its potential clinical application.
