Over the past decade, a number of different approaches have been propo
sed for the radiolabelling of metered dose inhalers (MDIs) in order to
permit gamma scintigraphic imaging of emitted aerosols following inha
led administration. More recently, methods have been described for the
indirect Tc-99m-labelling of drugs incorporated into commercial MDI p
roducts. This paper attempts to rationalise such methods from a surfac
e chemical perspective in order to: 1) elucidate the mechanism of asso
ciation of the radiolabel and drug; 2) predict the appropriateness of
the techniques to all MDI products and; 3) propose in vitro testing me
thods to validate the labelling efficiency prior to in vivo evaluation
.