Effect of chitosan on the permeability of monolayers of intestinal epithelial cells (Caco-2)

  • Artursson P
  • Lindmark T
  • Davis S
 et al. 
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Abstract

All polymer preparation showed a statistically significant improvement of buserelin absorption compared to the control solution. The absolute bioavailabilities for the different polymer preparations were: control, 0.1%; 0.5% FNaC934P, 0.6%; 0.5% C934P, 2.0%; chitosan hydrochloride, 5.1% and FNaC934P/chitosan hydrochloride (1:1 (v/v» mixture, 1.0%. The higher bioavailability with chitosan hydrochloride cornpared to C934P and FNaC934P indicates that for buserelin the intestinal transmucosal transport enhancing effect of the polymer plays a more dominant ro1ethan the protection against proteases such as oe-chyrnotrypsin. Conclusions. The mucoadhesive polymers carbomer 934P and chitosan hydrochloride are able to enhance the intestinal absorption of buserelin in vivo in rats, and may therefore be promising excipients in peroraI delivery systems for peptide drugs.

Author-supplied keywords

  • Caco-2
  • Chitosan
  • Drug absorption
  • Nasal epithelium
  • Permeability

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