Optimization of the experimental design parameters for synthesis of Fluconazole loaded transethosomes as nano-based antifungal vesicles
1 Department of Pharmacy, Dr BENZERDJEB Benaouda Faculty of Medicine, Abou Bekr BELKAID University, Tlemcen, Algeria.
2 Laboratory of Organic Chemistry Natural Substances and Analysis (C.O.S.N.A.), Abou bekr BELKAID University, Tlemcen, Algeria.
3 Department of Pharmacy, Faculty of Medicine, University of Oran 1, Oran, Algeria.
Research Article
GSC Biological and Pharmaceutical Sciences, 2024, 28(03), 071–083.
Article DOI: 10.30574/gscbps.2024.28.3.0317
Publication history:
Received on 26 July 2024; revised on 03 September 2024; accepted on 05 September 2024
Abstract:
Introduction: Antifungal drugs formulated in conventional pharmaceutical forms are not fully effective due to various factors. New approaches have focused on transdermal delivery drugs, including transethosomes, where the mixture of ethanol and surfactant allows a deeper drug skin’s penetration. Formulation parameters and process variables can make their optimization a considerable challenge. This study aimed to formulate Fluconazole-loaded transethosomes using a full-factorial design with the goal of optimizing formulation and process variables.
Method: Fluconazole transethosomes were developed using the cold Method. A 21,31 full-factorial design was created by Design Expert® Software, where the impact of surfactant’s type and soy lecithin to surfactant ratio on resulting formulation were investigated. The formulations were tested for vesicle size, polydispersity index, zeta potential and entrapment efficiency.
Results: Formulations containing Tween®80 presented the smaller particle sizes and showed a considerable entrapment efficiency for Fluconazole, they were more homogenous and highly stable compared to those prepared with Span®80. The optimized soy lecithin to surfactant ratio of 90:10 with Tween®80 was deemed apt for the synthesis of transethosomes giving the optimal formulation with a small particle size (300.2±5.57 nm), a low PDI (0.203±0.004), a good zeta potential (−31.75±0.68 mV) and a high entrapment efficiency (88.11±0.74 %).
Conclusion: This study enabled the in-depth identification and optimization of the key factors involved in the experimental process, such as the type of surfactant used and the soybean lecithin-to-surfactant ratio. To ensure safety and effectiveness in use, this work provides the perspective of continuing the study by evaluating the antifungal activity, long-term stability and safety of Fluconazole-loaded transethosomes.
Keywords:
Fluconazole; Transethosomes; Cold method; Surfactant; Full-factorial design
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