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Pharmaceutical Research

, Volume 29, Issue 4, pp 943–952 | Cite as

The Counterbalanced Effect of Size and Surface Properties of Chitosan-Coated poly(isobutylcyanoacrylate) Nanoparticles on Mucoadhesion Due to Pluronic F68 Addition

  • Bénédicte Petit
  • Kawthar Bouchemal
  • Christine Vauthier
  • Madeleine Djabourov
  • Gilles Ponchel
Research Paper

ABSTRACT

Purpose

To evaluate of the effect of size and surface characteristics of poly(isobutylcyanoacrylate) nanoparticles coated with pluronic F68 and thiolated chitosan on mucoadhesion.

Methods

Nanoparticles were obtained by radical emulsion polymerization in presence of different amounts of F68 (0–4%w/v). Mucoadhesion was ex vivo evaluated by applying nanoparticle suspension on rat intestinal mucosa and quantifying the amount of attached nanoparticles after incubation.

Results

F68 unimers added in the polymerization medium allowed decreasing nanoparticle size from 251 to 83 nm, but resulted in nanoparticle surface modification. The amount of thiolated chitosan onto nanoparticle surface was decreased resulting in lower thiol groups and zeta potential. Consequently, the decrease of nanoparticle hydrodynamic diameter resulted in eight-fold-increase of the number of nanoparticles attached to the mucosa but a significant decrease of the weight of attached nanoparticles was observed. This unexpected result was due to a decrease of the amount of chitosan and thiolated chitosan available to interact with mucus upon addition of F68 in the polymerization medium.

Conclusions

Addition of F68 should not be recommended to improve the amount of mucoadherent nanoparticles. Further studies could allow understanding if the low amount of small size nanoparticles could be able to improve oral bioavailability.

KEY WORDS

chitosan mucoadhesion nanoparticles pluronic F68 poly(isobutylcyanoacrylate) 

Notes

ACKNOWLEDGMENTS & DISCLOSURES

The authors want to thank Dr. K. Broadley from Henkel Biomedical (Ireland) for his kindness in providing the isobutylcyanoacrylate monomer, the Department of Organic Chemistry (Biocis UMR CNRS 8076), Faculty of Pharmacy, University Paris-Sud (Châtenay-Malabry, France) for their help in the synthesis of 2- iminothiolane.

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Copyright information

© Springer Science+Business Media, LLC 2011

Authors and Affiliations

  • Bénédicte Petit
    • 1
  • Kawthar Bouchemal
    • 1
    • 3
  • Christine Vauthier
    • 1
  • Madeleine Djabourov
    • 2
  • Gilles Ponchel
    • 1
  1. 1.Université Paris-SudUMR CNRS 8612Châtenay-MalabryFrance
  2. 2.Laboratoire de Physique ThermiqueESPCI-ParisTechParis Cedex 05France
  3. 3.Univ Paris-Sud, UMR CNRS 8612Physico-chemistry, Pharmacotechny & BiopharmacyChâtenay-MalabryFrance

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