Effect of formulation parameters on the characteristics of binary ethosomes loaded with Fluconazole

Background: The emergence of fungal resistance to most conventional topical antifungal drugs remains a serious problem. New topical drug delivery systems, such as ethosomes, particularly binary ones, have proven to be effective due to their ability to efficiently target the deeper layers of the skin, due to the presence of a high amount of ethanol in their structure. They deliver an optimal drug dose with reduced toxicity. These are soft and flexible vesicles, composed of phospholipids, a binary alcohol phase and water. The combination of ethanol with other alcohols is believed to give them smaller vesicle sizes, higher skin permeability and better entrapment efficiency. This study aimed to formulate and characterize binary ethosomes loaded with Fluconazole to investigate the effect of formulation parameters on their characteristics.

Methods: A preliminary trial consisted on the preparation of blank classical ethosomes without active substance by varying the sonication time to select the optimal time, allowing for the subsequent the preparation of binary ethosomes loaded with Fluconazole, where ethanol and soybean lecithin concentrations were varied. The ethosomes were characterized by determining the particle size, zeta potential and the percentage of entrapment efficiency of Fluconazole.

Results: The particle size of the blank classical ethosomes ranged from 412,2±1,7nm to 5816±9,6nm, while the binary ethosomes ranged from 742,5±11,1nm to 2288±10nm. The zeta potential was between -8.15±0.1mV and -41.1±0.2mV for classical ethosomes and -9.91±0.1mV and -48.4±0.35mV for binary ethosomes. Finally, the entrapment efficiency percentage of the binary ethosomes ranged from 48,89±3.5% to 89,89±0.1%.

Conclusion: Based on the obtained results, the formulation parameters had a significant impact on the characteristics of the formulated ethosomes.