Published : 2017-08-16

COMPOUNDS THAT BIND TO PLASMA PROTEINS IN HUMANS. SIGNIFICANCE IN THERAPY AND METHODS FOR QUANTIFICATION OF A FREE FRACTION

Martyna Chechłacz

Natalia Korytowska

Abstract

Many endogenous and exogenous substances are able to bind to plasma proteins, mainly to human serum albumin and α-1-acid glycoprotein. In the bloodstream, these substances are present both in a free and in a protein-bound form. The protein has on its surface binding sites, specific for a given compound, which differ in size, shape and affinity. Binding is mediated by hydrophobic, van der Waals and/or electrostatic interactions. The extent to which compounds bind to plasma proteins depends on a number of different factors, including the presence of inflammation, kidney and liver diseases, and age. Only the free fraction is biologically active and is able to cross biological barriers. Therefore, methods of measuring the free plasma concentration of compounds are crucial. The most commonly used method is equilibrium dialysis, which is considered to be the reference method. Other methods include ultrafiltration, ultracentrifugation, microdialysis, microextraction, high-performance frontal analysis and cloud point extraction.

Keywords:

unbound fraction, drug, albumin, plasma proteins, ultrafiltration, equilibrium dialysis


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Chechłacz, M., & Korytowska, N. (2017). COMPOUNDS THAT BIND TO PLASMA PROTEINS IN HUMANS. SIGNIFICANCE IN THERAPY AND METHODS FOR QUANTIFICATION OF A FREE FRACTION. Prospects in Pharmaceutical Sciences, 15(6), 50–59. https://doi.org/10.56782/pps.76

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Editorial Team
Stefana Banacha 1
02-097 Warsaw, Poland
biuletynfarmacji@wum.edu.pl
Publisher:
Medical University of Warsaw
ul. Żwirki i Wigury 61
02-091 Warszawa

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