Box–Behnken design for the development of fluconazole-loaded classical ethosomes
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), 057–070.
Article DOI: 10.30574/gscbps.2024.28.3.0316
Publication history:
Received on 26 July 2024; revised on 03 September 2024; accepted on 05 September 2024
Abstract:
Introduction: Ethosomes are soft and flexible vesicles mainly composed of phospholipids, ethanol and water. The presence of a high amount of ethanol ensure deeper drug penetration; however, an optimal formulation is necessary. This study aims to develop and characterize Fluconazole loaded classical ethosomes using Box-Behken design, in order to achieve to an optimal formulation having a minimal vesicle size, low polydispersity index, high zeta potential and good entrapment efficiency (% EE).
Methods: Fluconazole ethosomes were prepared using cold method and tested for vesicle size, polydispersity index, zeta potential and EE%. Box-Behken design was created using Design Expert® Software, where the impact of sonication time and amount of ethanol and soybean lecithin on resulting formulation were investigated.
Results: It was determined that increasing the concentration of ethanol up to an optimized limit reduces vesicle size and improves % EE. It was also observed that soybean lecithin concentrations affected positively vesicle size but negatively % EE. Whereas sonication time had an inverse effect both on, vesicle size and EE%. All prepared formulations showed a low polydispersity index and a good zeta potential indicating homogeneity and high stability. Therefore, the optimal formulation had % EE of 80.05±0.306 % and vesicular size of 226.501±5.34 nm with polydispersity index of 0.487±0.0078.
Conclusion: In summary, using Box-Behnken design can enhance the understanding of the correlations between the variables involved in ethosome formation and their effects on vesicle size, polydispersity index and % EE. The optimal formulation obtained can be incorporated into drug delivery systems to enhance skin permeation and antifungal activity.
Keywords:
Ethosomes; Fluconazole; Cold method; Box-Behken design.
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