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Self-Nanoemulsification of Healthy Oils to Enhance the Solubility of Lipophilic Drugs
Published on: July 27, 2022
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Self-nanoemulsifying System Optimization for Higher Terconazole Solubilization and Non-Irritant Ocular Administration
Carol Yousry1, Pakinam Mohsen Zikry2, Emad Basalious Basalious1
1Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Kasr El-Aini, Cairo 11562, Egypt.
Advanced Pharmaceutical Bulletin
|July 16, 2020
Summary
This study developed novel self-nanoemulsifying systems (SNESs) to improve the ocular delivery of terconazole (TZ), an antifungal drug. The optimized SNES formulation enhanced drug release and showed no irritation, indicating improved potential for treating ocular fungal infections.
Area of Science:
- Pharmaceutical Sciences
- Ophthalmology
- Drug Delivery Systems
Background:
- Poor aqueous solubility of drugs like terconazole (TZ) limits their efficacy in ophthalmic formulations.
- Low ocular bioavailability restricts the therapeutic use of antifungal agents for eye infections.
Purpose of the Study:
- To enhance the solubilization and ocular permeation of terconazole (TZ).
- To develop a self-nanoemulsifying system (SNES) for improved ocular bioavailability of TZ.
Main Methods:
- Preparation and characterization of various SNES formulations using different oils, surfactants, and co-surfactants.
- Ternary phase diagrams were used to identify optimal self-nanoemulsification regions.
- In vitro drug release and Hen's Egg test-chorioallantoic membrane (HET-CAM) assay were performed for optimized systems.
Main Results:
- An optimized SNES formulation using Labrafil® M2125 CS, Tween® 80, and Transcutol® HP was developed.
- The optimized system exhibited small globule size (15.13 nm) and rapid self-emulsification (12.80 seconds).
- 100% drug release was achieved within 30 minutes, significantly faster than TZ suspension, with no observed ocular irritation.
Conclusions:
- The developed self-nanoemulsifying system (SNES) effectively enhances terconazole (TZ) solubilization and ocular permeation.
- This formulation presents a promising strategy for improving the therapeutic efficacy of TZ in treating ocular fungal infections.
- The non-irritating nature of the SNES formulation is crucial for ophthalmic drug delivery.
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