4.7 Review

Recent Experimental Developments in Studying Passive Membrane Transport of Drug Molecules

Journal

MOLECULAR PHARMACEUTICS
Volume 18, Issue 6, Pages 2122-2141

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.molpharmaceut.1c00009

Keywords

passive transport; biological membranes; drug-like molecules; fluorescence; surface plasmon resonance; second-harmonic light scattering

Funding

  1. NIH [R01 EY0024327, R01 EY026171]
  2. National Science Foundation [CHE-1465096]

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This review discusses recent developments in experimental approaches and theoretical models for quantitative and real-time analysis of membrane transport of drug-like molecules through mimetic and living cell membranes. The focus is on time-resolved fluorescence-based, surface plasmon resonance, and second-harmonic light scattering approaches, as well as the current understanding of how properties of the membrane and permeant affect the permeation process.
The ability to measure the passive membrane permeation of drug-like molecules is of fundamental biological and pharmaceutical importance. Of significance, passive diffusion across the cellular membranes plays an effective role in the delivery of many pharmaceutical agents to intracellular targets. Hence, approaches for quantitative measurement of membrane permeability have been the topics of research for decades, resulting in sophisticated biomimetic systems coupled with advanced techniques. In this review, recent developments in experimental approaches along with theoretical models for quantitative and real-time analysis of membrane transport of drug-like molecules through mimetic and living cell membranes are discussed. The focus is on time-resolved fluorescence-based, surface plasmon resonance, and second-harmonic light scattering approaches. The current understanding of how properties of the membrane and permeant affect the permeation process is discussed.

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