Abstract: Cyclodextrins can be coupled to biorecognition molecules such as antibodies. The cyclodextrins so coupled provide a cavity or complexation zone into which active agents such as labels, drugs and the like may be incorporated. The active agent forms a noncovalently bonded inclusion complex within the cavity of the cyclodextrin. It remains associated with the cyclodextrin and the coupled biorecognition molecule and thus can be delivered to the other half of the biospecific recognition pair. A process for producing these materials is also disclosed. The process includes the steps of activating a primary hydroxyl site on a cyclodextrin; linking a biorecognition molecule to the activated primary hydroxyl site on the cyclodextrin in either a direct covalent linkage or through a covalently linked spacer; and introducing a guest molecule (active agent) into the cavity of the derivatized cyclodextrin to form an inclusion complex.