The conceptof drug distribution in tissue relates to defining the state of the drug (free/bound) as well as the spatial location in lung tissue at several levels. The chapter begins by theoretically introducing general pharmacokinetic concepts that determine drug distribution in tissue, that are also relevant for the lung and the inhaled drug. This is followed by the main section describing current state of knowledge of the actual mechanisms involved in inhaled drug distribution in conjunction with the applied experimental techniques. This is followed by a discussion on how to obtain data on the spatial distribution of compounds in the heterogenous lung tissue. Finally, some suggestions are put forth for improving the understanding of lung tissue distribution and its pharmacological consequences.