Formulation and evaluation of fluconazole emulgels for potential treatment of vaginal candidiasis

Abstract

Localised treatment of vaginal candidiasis could improve the therapeutic outcomes of patients with vaginal candidiasis as well as reduce drug dosage and dosing interval. The aim of the research project was to develop fluconazole emulgel formulations, and evaluate their physicochemical, drug release, antifungal, safety, and stability profile, for potential treatment of vaginal candidiasis. Xanthan gum and HPMC E5LV-based fluconazole emulgels were prepared using the spontaneous emulsification method and their physicochemical properties, drug content, drug release profile, anti-fungal activity against Candida albicans, in vivo vaginal biocompatibility and stability profile were evaluated using standard protocols. The fluconazole emulgels exhibited satisfactory properties: pH: 5.2–5.4; spreadability: 1.6–2.5 cm; apparent viscosity: 85–314 cP; zone of inhibition against Candida albicans: 22–38 mm; drug content: 91–102 %, and vaginal biocompatibility. All the studied fluconazole emulgels exhibited controlled fluconazole release over 6 h and their drug release kinetics fitted well with Korsmeyer-Peppas model. HPMC-based emulgels exhibited unsatisfactory real-time stability profile. To our knowledge, this is the first report where xanthan gum and HPMC E5LV-based fluconazole emulgels have been studied for possible treatment of vaginal candidiasis. Xanthan gum-based fluconazole emulgels are promising drug formulations that could reduce the drug dosage and dosing frequency. In addition, they could serve as alternative dosage forms to Flucos® gel.