Chromatographic measurement of drug-protein interaction: determination of HIV protease inhibitor-serum albumin association

Analytical Biochemistry
K A Koeplinger, Z Zhao

Abstract

A chromatographic method for evaluation of the serum protein binding of a large number of non-peptide human immunodeficiency virus (HIV) protease inhibitors in short analysis time and automated fashion was developed. The method utilizes a size exclusion HPLC column. Bovine or human serum albumin is added to the mobile-phase running buffer. Qualitatively, a shift to shorter drug retention time in the presence of protein in the mobile phase is indicative of binding interaction of the drug and protein. The extent of binding of the drug to the protein is quantitated by comparison of the shift in retention time in the presence of protein to the retention time of the drug in the same buffer in the absence of protein (i.e., the drug's "intrinsic" retention time on the column). Binding measurements were carried out a 37 degrees C with a temperature-controlled autosampler and column oven. Results were compared with those obtained by ultrafiltration. The method yields thermodynamically valid binding measurements and is capable of directly detecting differences in the protein binding of individual stereoisomers present in mixtures (either enantiomers or diastereomers) without prior purification of the individual stereoisomers. The method ...Continue Reading

Citations

Apr 29, 2011·The Journal of Physical Chemistry. B·Uttam AnandSaptarshi Mukherjee
Feb 23, 2012·Physical Chemistry Chemical Physics : PCCP·Uttam AnandSaptarshi Mukherjee
Mar 18, 2005·Journal of Medicinal Chemistry·Dominique L N G SurlerauxPiet B T P Wigerinck

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