Mass spectrometry imaging for drug distribution studies

Since its introduction mass spectrometry imaging (MSI) has proven to be a powerful tool for the localization of molecules in biological tissues. In drug discovery and development, understanding the distribution of both drug and its metabolites is of critical importance. Traditional methods suffer from a lack of spatial information (tissue extraction followed by LCMS) or lack of specificity resulting in the inability to resolve parent drug from its metabolites (whole body autoradiography). MSI is a sensitive and label-free approach for imaging drugs and metabolites in tissues. In this article we review the different MSI technologies that have been applied to the imaging of pharmaceuticals. Recent technical advances, applications and current analytical limitations are discussed.This article is part of a Special Issue entitled: Imaging Mass Spectrometry: A User’s Guide to a New Technique for Biological and Biomedical Research.

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► Mass Spectrometry Imaging is a powerful tool for localizing compounds and metabolites.
► MSI technologies are label-free enabling metabolites to be resolved from the parent drug.
► Cellular level spatial resolution has been demonstrated.
► Recent advancements include full quantitation and high throughput imaging.