Intravaginal delivery of syngonanthus nitens (Bong.) Ruhland fraction based on a nanoemulsion system applied to vulvovaginal candidiasis treatment

Abstract

In this study, was evaluated the chemical composition of a fraction from Syngonanthus nitens extract and its antimicrobial potential unloaded (Fr3) and loaded (F9Fr3) into a nanoemulsion (F9) composed of cholesterol as the oil phase (10%), polyoxyethylene 20-cetyl ether and soy phosphatidylcholine (2:1) as surfactant (20%), and a solution of phosphate buffer (pH 7.4) plus chitosan polymer dispersion (0.25%) as the aqueous phase (70%) to use for VVC treatment. Phytochemical procedures showed that Fr3 is rich in luteolin, which is responsible for the antimicrobial activity. F9 development showed satisfactory parameters for use in the vulvovaginal candidiasis (VVC) treatment, as F9 demonstrated pseudoplastic, elastic behavior, and adhesive properties on vaginal mucosa. In addition, we observed improvement in antimicrobial potential of Fr3 on planktonic and biofilms after incorporation in F9. Fr3 and F9Fr3 showed satisfactory parameters related to toxic profiles in cell lines and in a model of acute toxicity by Artemia salina. The in vivo VVC assay showed that F9Fr3 was more active than unloaded Fr3 in VVC treatment. In conclusion, this work showed that use of a fraction rich in luteolin can be a used as an antimicrobial for treatment of vaginal infections and that use of nanostructured lipid systems was an important factor in the biological efficacy of Fr3, especially in treatment of acute VVC.