The quantitation of free drug fractions is important because this fraction is responsible for the overall pharmacological activity and toxicity of drugs inside our body. In this project, ultrafast affinity extraction has been employed to study the equilibrium and kinetic processes that take place during the interactions of various pharmaceutical agents (e.g., warfarin, gliclazide, glipizide and glibenclamide) with human serum albumin (HSA), the most abundant transport protein in the blood. HSA was covalently immobilized onto the diol bonded silica and placed into affinity microcolumns. These microcolumns were then used to extract the free fractions of drugs from drug-HSA mixtures in solution. Various experimental conditions, such as the flow rate and column size, were optimized for these free fraction measurements. The association equilibrium constants measured for the tested drugs were in the range of 104 to 106 M-1 s-1, and the corresponding dissociation rate constants were in the range of 0.5 to 2.2 s-1. The measured equilibrium and rate constants showed good agreement with literature values. Advantages of this method were its ability to use small sample injection volumes (5-20 µL), its rapid analysis times (typically 1-10 min), and its ability to directly examine solution-phase interactions. The information obtained from this method can be useful in understanding how these drugs interact with HSA when they are circulated in blood. 

Analysis of drug-protein interactions using ultra fast affinity extraction

Macromolecular Chemistry: The Second Century

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ACS Spring 2020 National Meeting & Expo

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.