Lipidomics is the new frontier in biomolecular structural studies. Not only are lipids the main components in membranes that define the contours of the cell and its organelles, but they are also used for storage. Lipids form stable noncovalent complexes with proteins as well as with many drugs. Lipids are a storage depot for drugs and certain types of organic molecules. To study lipid composition and distribution, complex and time-consuming techniques are used. However, recent advances in mass spectrometry, mainly matrix-assisted laser desorption/ionization (MALDI) have made it possible to directly probe tissues to study structural components, as well as for the localization of drugs. Direct tissue imaging is a powerful tool as it gives a more complete and accurate structural picture and can trace and follow where drugs localize in tissue with minimal anatomical disruption and a minimum of manipulations. Hence, we believe that in addition to its accuracy and efficiency, this new approach will lead to a better understanding of physiological processes as well as the pathophysiology of disease.