Cyclodextrins — Useful excipients for oral peptide administration?

Cyclodextrins have been investigated for their potential use as excipients for the oral delivery of peptides

Barbara Haeberlin

2002

Scholarcy highlights

  • Cyclodextrins have been investigated for their potential use as excipients for the oral delivery of peptides
  • Physical mixtures of the peptides with α-cyclodextrin, β-cyclodextrin, γ-cyclodextrin, hydroxypropyl-β-cyclodextrin and dimethyl-β-cyclodextrin were used throughout the experiments
  • The use of β-cyclodextrin and hydroxypropyl-β-cyclodextrin resulted in an increased chemical and enzymatic stability of the peptides. β-Cyclodextrin, γ-cyclodextrin and hydroxypropyl-β-cyclodextrin showed absorption enhancing properties in the in vitro system as well as in the in situ study
  • An enhanced permeation of the paracellular marker PEG-4000 across the cell monolayers in the presence of distinct cyclodextrins indicated an impairment of the tight junctional integrity as one reason for improved peptide absorption
  • The results suggest that distinct cyclodextrins have protective and absorption enhancing effects on peptides by preparing simple physical mixtures of the two components
  • The extent of protection and absorption enhancement seems to depend strongly on the nature of the peptide used as well as the chosen cyclodextrin

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