TIRF Microscopy-Based Monitoring of Drug Permeation Across a Lipid Membrane Supported on Mesoporous Silica
Journal article, 2021

There is an urgent demand for analytic approaches that enable precise and representative quantification of the transport of biologically active compounds across cellular membranes. In this study, we established a new means to monitor membrane permeation kinetics, using total internal reflection fluorescence microscopy confined to a ≈500 nm thick mesoporous silica substrate, positioned underneath a planar supported cell membrane mimic. This way, we demonstrate spatiotemporally resolved membrane permeation kinetics of a small-molecule model drug, felodipine, while simultaneously controlling the integrity of, and monitoring the drug binding to, the cell membrane mimic. By contrasting the permeation behaviour of pure felodipine with felodipine coupled to the permeability enhancer caprylate (C8), we provide evidence for C8-facilitated transport across lipid membranes, thus validating the potential for this approach to successfully quantify carrier system-induced changes to cellular membrane permeation.

total internal reflection fluorescence

drug delivery

supported lipid bilayer

membrane permeation

mesoporous silica


Paul Joyce

Chalmers, Physics, Biological Physics

Silver Jõemetsa

Chalmers, Physics, Biological Physics

Simon Isaksson

Chalmers, Physics, Nano and Biophysics

Shakhawath Hossain

Uppsala University

Per Larsson

Uppsala University

Christel A.S. Bergström

Uppsala University

Fredrik Höök

Chalmers, Physics, Nano and Biophysics

Angewandte Chemie - International Edition

1433-7851 (ISSN) 1521-3773 (eISSN)

Vol. 60 4 2069-2073

Subject Categories

Cell Biology

Biochemistry and Molecular Biology

Medical Biotechnology (with a focus on Cell Biology (including Stem Cell Biology), Molecular Biology, Microbiology, Biochemistry or Biopharmacy)



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2/1/2021 1