Administration of drugs by inhalation is mainly used to treat lung diseases and is being investigated as a possible route for systemic drug delivery. It offers several benefits, but it is also fraught with many difficulties. The lung is a complex organ with complicated physiology and specific pharmacokinetic processes. Therefore, the exposure and subsequently efficacy of a drug after inhalation is affected by a number of factors. In this review, we summarize the main variables that may affect drug fate after inhalation delivery, such as physicochemical properties of the drug, pulmonary clearance and metabolism, pathophysiological factors and inhalation device. Factors that have impact on pharmacokinetic processes need to be considered during development as their correct setting can lead to new effective inhaled drugs.
Keywords: Drug delivery; Pharmacokinetics; Physicochemical properties; Pulmonary clearance; Pulmonary metabolism; Respiratory system.