Comprimido vaginal mucoadesivo com atividade antifúngica: Desenvolvimento farmacotécnico e avaliação biológica

Abstract

Vaginal candidiasis is a common and recurrent dengue, caused by yeasts belonging to the genus Candida, being the species C. albicans responsible for the conditions of inflammation in the vagina, which directly reflects on the quality of life of women. Fungal resistance against available conventional drugs is becoming more and more a strong threat to public health. In addition, the adverse effects caused by these drugs represent an inconvenience related to administration. Natural bioactives containing polyphenols as the main active component have gained ground in the development of antimicrobial therapies. Therefore, this study aimed to develop a mucoadhesive vaginal tablet, with antifungal activity against C. albicans, aiming at the release of Active Plant Pharmaceutical Ingredient (IFAV). The plant drug was obtained by grinding and the IFAV by the rotaevaporation technique using a ratio of 1:1 water/ethanol. Subsequently, quantification phytochemical and microbiological assays by microdilution were performed. The tablets were developed by fixing IFAV (40%), lubricant (2%), thinner/sweetener (33%), disintegrant (10%), adhesive agent (15%) and subjected to physical-chemical quality control, determined by Pharmacopoeia 6th edition. The results revealed that for every 100 g of extract, IFAV had 15 mg of gallic acid equivalents, 1.5 mg of quercetin equivalents, and tannins had 1 mg of catechin equivalents. The IFAV MIC against C.albicans strains was 62.5 µg mL–1. Different tablets were obtained, varying the adhesive agents: carboxymethylcellulose, hydroxypropylmethylcellulose and pluronic; however, none of them had good flow. Thus, the wet compression method was used. The macroscopic features showed a homogeneous surface, without erosion or adhesion. The quality control results (average weight, friability and hardness) met the requirements of the Brazilian Pharmacopoeia. The dissolution test revealed that tablets containing carboxymethylcellulose and hydroxypropylmethylcellulose disintegrated in a time ≤ 30 minutes, being considered conventional release formulations. Tablets developed with pluronic showed a prolonged dissolution profile, that is, after 72 h, approximately 55% of the IFAV was released. The mucoadhesion test showed high adhesion values between the tablet/mucin and the vaginal tablet/mucosa. Based on this, the tablets developed showed potential for commercialization, as they meet all the requirements of regulatory agencies and can benefit patients with vaginal candidiasis.