Details

Autor(en) / Beteiligte

• Brewster, Marcus E.
• Noppe, Marc
• Peeters, Jef
• Loftsson, Thorsteinn

Titel

Effect of the unstirred water layer on permeability enhancement by hydrophilic cyclodextrins

Ist Teil von

• International journal of pharmaceutics, 2007-09, Vol.342 (1), p.250-253

Ort / Verlag

Amsterdam: Elsevier B.V

Erscheinungsjahr

2007

Quelle

Elsevier ScienceDirect Journals

Beschreibungen/Notizen

• Saturated solutions of three test compounds, carbamazepine, griseofulvin and hydrocortisone, were prepared in aqueous buffer (pH 7.4) containing 0, 1, 5 and 10% HPβCD. The permeability and flux of the drugs though a PAMPA membrane at different unstirred water layer (UWL) thicknesses was determined. In absence of HPβCD, permeability coefficients increased two- to three-fold with decreasing UWL thickness to a certain minimum values of about 40 μm. Addition of HPβCD to systems exhibiting larger UWL thicknesses significantly increased compound flux. The effect of HPβCD was linked to its association constant ( K 1:1) with the model drugs and decreased with decreasing UWL thickness to a certain minimum value. This suggests that hydrophilic cyclodextrins enhance flux when the UWL resistance significantly contributes to the overall barrier resistance.