Drug delivery to the lung in vivo may be assessed using pharmacokinetic or pharmacodynamic techniques. The choice of method depends on drug class specificities. Pharmacokinetic determination of deposition to the lung for drugs without hepatic first-pass effect, such as short acting beta2-agonists, has to be done shortly after inhalation to minimize the effect of gastrointestinal absorption. For medication undergoing important hepatic first-pass metabolisation, such as inhaled corticosteroid, plasma concentration indirectly reflects bronchial deposition. The pharmacodynamic profile should be assessed through clinical effects and adverse events induced by inhaled drugs. Dose ranking of lung deposition for bronchodilators requires patient selection with sufficient bronchial obstruction to maintain room for improvement after the first dose. To assess dose effect relationship between inhaled corticosteroid, the Finney parallel line bioassay is the reference method with a study period of at least 6 weeks. Analysis of side effects with high doses of beta2-agonists or inhaled corticosteroids may also be used to compare lung deposition. Finally, pharmacological evaluation of lung deposition provides complementary information to scintigraphic studies, based on their clinical relevance.