PLoS ONE (Jan 2017)

Gallic acid/hydroxypropyl-β-cyclodextrin complex: Improving solubility for application on in vitro/ in vivo Candida albicans biofilms.

  • Guilherme Rodrigues Teodoro,
  • Aline Vidal Lacerda Gontijo,
  • Aline Chiodi Borges,
  • Márcia Hiromi Tanaka,
  • Gabriela de Morais Gouvêa Lima,
  • Marcos José Salvador,
  • Cristiane Yumi Koga-Ito

DOI
https://doi.org/10.1371/journal.pone.0181199
Journal volume & issue
Vol. 12, no. 7
p. e0181199

Abstract

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The aim of this study was to increase the solubility of gallic acid (GA) for the treatment of Candida albicans biofilm, which is very difficult to treat and requires high drug concentrations. Cyclodextrins (CDs) were used for this purpose. Complexes were evaluated by phase-solubility studies, prepared by spray drying and characterized by drug loading, scanning electron microscopy (SEM) and differential scanning calorimetry (DSC). The complexes were tested on C. albicans biofilm using in vitro and in vivo models. HPβCD formed soluble inclusion complexes with GA. The percentage of GA in GA/HPβCD was 10.8 ± 0.01%. The SEM and DSC analyses confirmed the formation of inclusion complexes. GA/HPβCD maintained the antimicrobial activity of the pure GA. GA/HPβCD was effective on C. albicans biofilms of 24 and 48h. The in vivo results showed an anti-inflammatory activity of GA/HPβCD with no difference in invading hypha counting among the groups. This study encourages the development of new antifungal agents.