Protonation kinetics compromise liposomal fluorescence assay of membrane permeation

Sezer, Deniz and Oruç, Tuğçe (2017) Protonation kinetics compromise liposomal fluorescence assay of membrane permeation. Journal of Physical Chemistry B, 121 (20). pp. 5218-5227. ISSN 1520-6106

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Abstract

The membrane permeation of weak acids and bases couples to the ambient pH and can be studied using pH-sensitive dyes as reporters. Such fluorescence measurements with aliphatic amine drugs have revealed biexponential kinetics of permeation into liposomes (Eyer et al. J. Controlled Release 2014, 173, 102). Permeability coefficients have been obtained using the faster of the two kinetic components. Here, the origin of the biexponential kinetics is studied with a kinetic rate model that in addition to drug permeation accounts for the protonation of the drug and the dye. Surprisingly, the experimental readout is found to strongly depend on the rates of protonation. The analysis demonstrates that fluorescence studies of drug permeation relying on pH-sensitive proxies should be accompanied by comprehensive modeling of the relevant kinetic processes.
Item Type: Article
Subjects: Q Science > QD Chemistry > QD450-801 Physical and theoretical chemistry
Divisions: Faculty of Engineering and Natural Sciences > Basic Sciences > Chemistry
Faculty of Engineering and Natural Sciences
Depositing User: Deniz Sezer
Date Deposited: 19 Aug 2017 14:15
Last Modified: 19 Aug 2017 14:15
URI: https://research.sabanciuniv.edu/id/eprint/32937

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