Oral gel loaded by ethotransfersomes of antifungal drug for oral thrush: Preparation, characterization, and assessment of antifungal activity

Abstract

Of all the clinical forms of candidiasis, the most common presentation is the acute pseudomembranous type, also known as oral thrush. It is characterized by scrapable superficial white plaques that resemble curdled milk. To come up with therapeutically efficacious drug-loaded formulations, the miconazole (MIC)-loaded ethotransfersome (ET) was investigated for its potential in alleviating oral thrush in the present research work. ETs are flexible liposome vesicles that combine the advantages of transfersomes and ethosomes. The MIC-loaded ET formulations were prepared and optimized using Design Expert software. To convert the optimized MIC loaded ET into a gel, the psyllium seed husk arabinoxylan hemicellulose (AXHc) was used because it has ulcer-healing properties. The cumulative amount permeated and the permeability coefficient for the optimized formula were markedly increased in contrast with other formulations. The antifungal activity was assessed by measuring the zone of inhibition against Candida albicans; it indicated the superior activity of the optimized MIC-ET-AXHc oral gel base formulation (27 mm), which was markedly greater than that of an MIC powder dispersed within the AXHc gel (15 mm), an MIC aqueous dispersion (12 mm), and a commercially available formulation (18 mm). The results of an in vivo pharmacodynamic study demonstrated that the optimized MIC-ET-AXHc oral gel base formulation has remarkably improved pharmacodynamic activity with a substantially reduced ulcer index score (0.5 ± 0.25) in contrast to other formulations and the marketed gel (2.0 ± 0.25). In the current research work, this combination of two potential carrier vesicles along with gelling agents with healing properties resulted in substantial increases in the membrane permeability across the buccal mucosa, antifungal activity, and healing of ulcers of the mouth.