Development and in vivo evaluation of chitosan-gel containing Mitracarpus frigidus methanolic extract for vulvovaginal candidiasis treatment

Biomed Pharmacother. 2020 Oct:130:110609. doi: 10.1016/j.biopha.2020.110609. Epub 2020 Aug 14.

Abstract

Vulvovaginal candidiasis (VVC) is characterized by inflammatory changes in the vaginal mucosa caused by abnormal colonization of Candida species. Traditional topical therapies using reference antifungal drugs usually present several issues and limitations for VVC treatment. Thus, the interest in new vaginal formulations, mainly those based on compounds from natural origin, has been growing over the last years. Methanolic extract from the plant species Mitracarpus frigidus (Willd. Ex Reem Schult.) K. Schum (MFM) has presented potential antifungal activity against C. albicans vaginal infection. Here, we aimed to develop and characterize a gynecological gel formulation based on chitosan containing MFM and to evaluate its anti-C. albicans effectiveness in the treatment of VVC. First, MFM was incorporated into a gel formulation based on chitosan in three final concentrations: 2.5 %, 5.0 %, and 10.0 %. Next, these gel formulations were subjected to stationary and oscillatory rheological tests. Finally, the gel was tested in an experimental VVC model. The rheological tests indicated pseudoplastic fluids, becoming more viscous and elastic with the increase of the extract concentration, indicating intermolecular interactions. Our in vivo analyses demonstrated a great reduction of vulvovaginal fungal burden and infection accompanied with the reduction of mucosal inflammation after MFM chitosan-gel treatment. The present findings open perspectives for the further use of the MFM-chitosan-gel formulation as a therapeutic alternative for VVC treatment.

Keywords: Antifungal; Chitosan; Mitracarpus frigidus; Rheological tests; Vulvovaginal candidiasis.

MeSH terms

  • Antifungal Agents / administration & dosage*
  • Antifungal Agents / chemistry
  • Candidiasis, Vulvovaginal / drug therapy*
  • Candidiasis, Vulvovaginal / microbiology*
  • Chemical Phenomena
  • Chitosan* / chemistry
  • Dose-Response Relationship, Drug
  • Female
  • Humans
  • Plant Extracts / administration & dosage*
  • Plant Extracts / chemistry
  • Rubiaceae / chemistry*
  • Vaginal Creams, Foams, and Jellies / administration & dosage*
  • Vaginal Creams, Foams, and Jellies / chemistry

Substances

  • Antifungal Agents
  • Plant Extracts
  • Vaginal Creams, Foams, and Jellies
  • Chitosan