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Drug permeability profiling using cell-free permeation tools: Overview and applications

Faller, Bernard, Berben, Philippe, Bauer-Brandl, Annette, Flaten, Goril Eide, Jacobsen, Christin, Brouwers, Joachim and Augustijins, Patrick (2018) Drug permeability profiling using cell-free permeation tools: Overview and applications. European Journal of Pharmaceutical Sciences, 119. pp. 219-233. ISSN 18790720


Cell-free permeation systems are gaining interest in drug discovery and development as tools to obtain a reliable prediction of passive intestinal absorption without the disadvantages associated with cell- or tissue-based permeability profiling. Depending on the composition of the barrier, cell-free permeation systems are classified into two classes including (i) biomimetic barriers which are constructed from (phospho)lipids and (ii) non-biomimetic barriers containing dialysis membranes. This review provides an overview of the currently available cell-free permeation systems including Parallel Artificial Membrane Permeability Assay (PAMPA), Phospholipid Vesicle-based Permeation Assay (PVPA), Permeapad®, and artificial membrane based systems (e.g. the artificial membrane insert system (AMI-system)) in terms of their barrier composition as well as their predictive capacity in relation to well-characterized intestinal permeation systems. Given the potential loss of integrity of cell-based permeation barriers in the presence of food components or pharmaceutical excipients, the superior robustness of cell-free barriers makes them suitable for the combined dissolution/permeation evaluation of formulations. While cell-free permeation systems are mostly applied for exploring intestinal absorption, they can also be used to evaluate non-oral drug delivery by adjusting the composition of the membrane.

Item Type: Article
Keywords: Artificial membrane insert system (AMI-system) Oral drug delivery Parallel artificial membrane permeability assay (PAMPA) Permeability Permeapad® Phospholipid vesicle-based permeation assay (PVPA)
Date Deposited: 26 May 2018 00:45
Last Modified: 25 Jan 2019 00:45


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