Pharmacoscintigraphic technique provides a non invasive method to monitor the in vivo fate of a different pharmaceutical dosage forms. This advanced approach combines gamma scintigraphy and pharmacokinetic information to predict the behaviour of dosage form in subjects under investigation. It is a technique whereby the transit of dosage form through its intended site of delivery can be non-invasively imaged in vivo via the judicious introduction of an appropriate short lived gamma emitting radioisotope. These studies provide an insight into the outcome of delivery systems, its integrity as well as enable the relationship between in vivo performance and resultant pharmacokinetic parameters. The present manuscript highlights several applications of this advanced approach in the evaluation of various drug delivery systems. Radiolabelling phenomenon, scintillation camera and safety consideration aspects have also been discussed.