Drug-free chitosan coated poly(isobutylcyanoacrylate) nanoparticles are active against trichomonas vaginalis and non-toxic towards pig vaginal mucosa

Pharm Res. 2015 Apr;32(4):1229-36. doi: 10.1007/s11095-014-1528-7. Epub 2014 Oct 16.

Abstract

Purpose: The present work reports a non-conventional therapeutic strategy based on the use of vaginally-applied formulations for the treatment of trichomoniasis due to Trichomonas vaginalis without adding a drug.

Methods: The formulations were based on a thermosensitive pluronic® F127 hydrogel containing mucoadhesive poly(isobutylcyanoacrylate) nanoparticles coated with a mixture of chitosan and thiolated chitosan (75/25 wt%). The nanoparticles were obtained by anionic emulsion polymerization of isobutylcyanoacrylate. The anti-T. vaginalis activity of the formulations was evaluated in vitro.

Results: Chitosan-coated nanoparticles showed a strong anti-T. vaginalis activity at 100 μg/mL independently on the proportion of thiolated chitosan. No anti-T. vaginalis activity was reported neither with chitosan-uncoated poly(isobutylcyanoacrylate) nanoparticles nor with chitosan used as a solution. These results suggest that the anti-T. vaginalis activity was related to poly(isobutylcyanoacrylate) nanoparticles but only when they are coated with chitosan. Histological analysis of ex vivo pig vaginal mucosa in contact with pluronic® F127 hydrogel containing poly(isobutylcyanoacrylate) nanoparticles coated with the mixture chitosan/thiolated chitosan (75/25 wt%) did not reveal any toxicity.

Conclusion: This study demonstrated that poly(isobutylcyanoacrylate) nanoparticles coated with chitosan were active against T. vaginalis without adding a drug. Besides their anti-T. vaginalis activity, the formulations are non-toxic towards pig vaginal mucosa.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antiprotozoal Agents / administration & dosage
  • Antiprotozoal Agents / pharmacology*
  • Antiprotozoal Agents / toxicity
  • Chitosan / chemistry*
  • Cyanoacrylates / administration & dosage
  • Cyanoacrylates / pharmacology*
  • Cyanoacrylates / toxicity
  • Drug Carriers / chemistry
  • Enbucrilate
  • Female
  • In Vitro Techniques
  • Mucous Membrane / drug effects*
  • Nanoparticles / chemistry*
  • Parasitic Sensitivity Tests
  • Swine
  • Tissue Adhesives / chemistry
  • Trichomonas vaginalis / drug effects*
  • Trichomonas vaginalis / growth & development
  • Vagina / drug effects*

Substances

  • Antiprotozoal Agents
  • Cyanoacrylates
  • Drug Carriers
  • Tissue Adhesives
  • Chitosan
  • Enbucrilate