Building new drug delivery systems: in vitro and in vivo studies of drug-hydroxybutenyl cyclodextrin complexes

In many respects, drug delivery is the perfect field for an organic chemist whose interest lies in structure-property relationships. Synthesis and characterization of a drug delivery system and subsequent introduction of a drug product incorporating this drug delivery technology into animals or humans is a complex and challenging structure-property problem. In this regard, we have developed hydroxybutenyl cyclodextrin (HBenCD) for oral and intravenous delivery of pharmaceutical actives having poor water solubility and low bioavailability. In this chapter, we summarize our recent research involving the synthesis and characterization of HBenCD, formation of drug-HBenCD complexes, in vitro solubility and dissolution studies of drug-HBenCD complexes, and pharmacokinetic studies in animals after oral and intravenous administration of drug-HBenCD complexes.