Mass Spectrometry Imaging: Applications in Drug Distribution Studies

In the past decade, mass spectrometry imaging (MSI) has received an increasing amount of attention due to its ability in displaying the spatial distribution of a wide range of molecules, including peptides, proteins, lipids, endogenous and exogenous metabolites, and xenobiotics in biological tissues. Information regarding drug localization within tissues provides a better understanding of pharmacokinetic behaviors and pharmacological and toxicological effects. This review presents an introduction to MSI, along with an in-depth analysis of its general process. In addition, we highlighted several examples of various intensive applications of imaging drugs and metabolites in tissues by mass spectrometry. Furthermore, we present the prospect of quantitative MSI of small molecular chemicals, which may be particularly attractive to researchers in the pharmaceutical industry today. It is expected that with technological advancement, MSI will become an increasingly powerful tool in drug disposition studies and other fields of biomedical research.