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Drug-Free Chitosan Coated Poly(isobutylcyanoacrylate) Nanoparticles Are Active Against Trichomonas vaginalis and Non-Toxic Towards Pig Vaginal Mucosa

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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.

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Abbreviations

HIV:

Human immunodeficiency virus

IBCA:

Isobutylcyanoacrylate

MTZ:

Metronidazole

Np:

Nanoparticle

PBS:

Phosphate buffer saline

PIBCA:

Poly(isobutylcyanoacrylate)

SVF:

Simulated vaginal fluid

TBA:

Thiol-butylamidine

TYM:

Trypticase-yeast extract-maltose

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ACKNOWLEDGMENTS AND DISCLOSURES

This work was supported by grants from Région Ile de France.

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Authors and Affiliations

  1. Institut Galien Paris Sud, UMR CNRS 8612, Faculté de Pharmacie, Univ Paris-Sud, Châtenay-Malabry, France

    Bénédicte Pradines, Christine Vauthier, Gilles Ponchel & Kawthar Bouchemal

  2. BioCis, UMR CNRS 8076, Antiparasitic Chemotherapy, Faculté de Pharmacie, Univ Paris-Sud, Châtenay-Malabry, France

    Bénédicte Pradines, Christian Bories & Philippe M. Loiseau

  3. Institut Galien Paris Sud, UMR CNRS 8612, Faculty of Pharmacy, University Paris-Sud, 5, Rue J.B. Clément, 92296, Châtenay-Malabry cedex, France

    Kawthar Bouchemal

Authors
  1. Bénédicte Pradines
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  2. Christian Bories
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  3. Christine Vauthier
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  4. Gilles Ponchel
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  5. Philippe M. Loiseau
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  6. Kawthar Bouchemal
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Correspondence to Kawthar Bouchemal.

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Pradines, B., Bories, C., Vauthier, C. et al. Drug-Free Chitosan Coated Poly(isobutylcyanoacrylate) Nanoparticles Are Active Against Trichomonas vaginalis and Non-Toxic Towards Pig Vaginal Mucosa. Pharm Res 32, 1229–1236 (2015). https://doi.org/10.1007/s11095-014-1528-7

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  • DOI: https://doi.org/10.1007/s11095-014-1528-7

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