Pharmaceutical Research

, Volume 19, Issue 2, pp 169–174

The Potential of Chitosan in Enhancing Peptide and Protein Absorption Across the TR146 Cell Culture Model—An in Vitro Model of the Buccal Epithelium

  • Ana Portero
  • Carmen Remuñán-López
  • Hanne Mørck Nielsen

DOI: 10.1023/A:1014220832384

Cite this article as:
Portero, A., Remuñán-López, C. & Nielsen, H.M. Pharm Res (2002) 19: 169. doi:10.1023/A:1014220832384


Purpose. To investigate the potential of chitosan (CS) to enhance buccal peptide and protein absorption, the TR146 cell culture model, a model of the buccal epithelium, was used.

Methods. The sensitivity of TR146 cells to several CS solutions (different salts with different MW) was investigated by using the MTS/PMS assay. Permeability studies were performed to determine the enhancing effect of CS glutamate (1, 20, 40, 60, and 100 μg/mL) on the permeability of 3H-mannitol and fluorescein isothiocyanate labeled dextrans (FD) with various MW (4.4-19.5 kD) across the cell culture model.

Results. Sensitivity of TR146 cells to CS solutions depended on the concentration, the pH, and the type of CS salt. CS glutamate solutions (pH 6.0) were found to be the least harmful. CS glutamate was able to increase the permeability of model substances with MW up to 9.5 kD across the cell model. An enhancing effect was found for CS concentrations of 20 μg/mL and higher, correlating with a decrease in TEER values. The 20 μg/mL CS concentration had a negligible effect on the enzyme activity of the cells as determined by the MTS/PMS assay.

Conclusions. CS glutamate is effective in enhancing the transport of macromolecules across the buccal TR146 cell culture model. Therefore, it might be a promising vehicle for peptide and protein buccal administration.

buccal permeability enhancementchitosanpeptide and protein absorptionTR146 cell culture model

Copyright information

© Plenum Publishing Corporation 2002

Authors and Affiliations

  • Ana Portero
    • 1
  • Carmen Remuñán-López
    • 1
  • Hanne Mørck Nielsen
    • 2
  1. 1.Department of Pharmacy and Pharmaceutical Technology, School of PharmacyUniversity of Santiago de CompostelaSantiago de CompostelaSpain
  2. 2.Department of Pharmaceutics, The Royal Danish School of Pharmacy2 UniversitetsparkenCopenhagen ØDenmark