Issue 7, 2024

A method for estimation of plasma protein binding using diffusion ordered NMR spectroscopy (DOSY)

Abstract

The plasma protein binding (PPB) of a drug plays a key role in both its pharmacokinetic and pharmacodynamic properties. During lead optimisation, medium and high throughput methods for the early determination of PPB can provide important information about potential PKPD profile within a chemotype or between different chemotype series. Diffusion ordered spectroscopy (DOSY) is an NMR spectroscopic technique that measures the diffusion of a molecule through the magnetic field gradient, according to its molecular size/weight. Here, we describe the use of DOSY for a rapid and straightforward method to evaluate the PPB of drug molecules, using their binding to bovine serum albumin (BSA) as a model.

Graphical abstract: A method for estimation of plasma protein binding using diffusion ordered NMR spectroscopy (DOSY)

Supplementary files

Article information

Article type
Research Article
Submitted
09 Apr 2024
Accepted
06 Jun 2024
First published
11 Jun 2024

RSC Med. Chem., 2024,15, 2372-2379

A method for estimation of plasma protein binding using diffusion ordered NMR spectroscopy (DOSY)

R. Taylor, T. Swift, D. Wilkinson and K. Afarinkia, RSC Med. Chem., 2024, 15, 2372 DOI: 10.1039/D4MD00244J

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