In situ forming pluronic® F127/chitosan hydrogel limits metronidazole transmucosal absorption

Eur J Pharm Biopharm. 2017 Mar:112:143-147. doi: 10.1016/j.ejpb.2016.11.024. Epub 2016 Nov 24.

Abstract

The objective of this work is to design topically-applied thermosensitive and mucoadhesive hydrogel containing metronidazole (MTZ) for the treatment of Trichomonas vaginalis infections. Hydrogel composed of pluronic® F127 (20wt%), chitosan (1wt%) and metronidazole MTZ (0.7wt%) mixture showed its ability to decrease by a factor 4 MTZ flux and apparent permeability absorption through vaginal mucosa. The impact of hydrogel on transmucosal penetration of MTZ was evaluated ex vivo on excised porcine vaginal mucosa mounted on Franz diffusion cell. The anti-T. vaginalis activity of MTZ formulated into F127/chitosan hydrogel was preserved since the viability curve evaluated in vitro was similar to MTZ solution.

Keywords: Chitosan; Hydrogel; Mucosal passage; Pluronic® F127; Thermosensitive; Trichomonas vaginalis.

MeSH terms

  • Animals
  • Antiprotozoal Agents / pharmacokinetics*
  • Chitosan / chemistry*
  • Female
  • Hydrogels / chemistry*
  • Metronidazole / pharmacokinetics*
  • Mucous Membrane / metabolism*
  • Permeability
  • Poloxamer / chemistry*
  • Swine
  • Vagina

Substances

  • Antiprotozoal Agents
  • Hydrogels
  • Poloxamer
  • Metronidazole
  • Chitosan