Comparative study of mucoadhesive vaginal tablets of Schinopsis brasiliensis Engler extract formulated with different polymers with antifungal activity

Abstract

Candida albicans is the main fungus responsible for acute and recurrent vaginal infections. Low adherence to treatment is due to dosing frequency and available topical medications. Thus, we developed mucoadhesive tablets based on Schinopsis brasiliensis Engler extract composed of Carboxymethylcellulose (F1), Hydroxypropylmethylcellulose (F2), or Pluronic (F3), against C. albicans . The extract metabolites determination showed presence of polyphenols (15 μg.mg-1), flavonoids (5.51 μg.mg-1), and tannins (4.80 μg.mg-1). The in vitro antifungal activity was performed by broth microdilution method. Quality control tests were performed according international pharmacopeias. Regarding the mucoadhesion test, in terms of the force expressed between the tablet:mucin disc, the average values were approximately 0.1267 N (F1), 0.0411 N (F2) and 0.814 N (F3), while in the tablet:vaginal mucosa, the average values were approximately 0.0294 N (F1), 0.0166 N (F2) and 0.0365 N (F3). The dry extract showed a minimum inhibitory concentration of 62.5 μg.mL-1. In evaluating the in vitro release of tablets, polymers derived from cellulose released 100% in less than 4 hours, while Pluronic released around 56.3% in 72 hours. It is concluded that F1 has greater mucoadhesion while F3 has a modified release rate, providing promising results for future application of the formulation in the clinical assay.

Keywords:
Vaginal fungal infections; Mucoadhesion; Carboxymethylcellulose; Hydroxypropylmethylcellulose; Pluronic