Affect of Captisol^® on PK of Drug

Is the drug candidate released from the complex?

Complexes dissociate rapidly and completely in most cases. Complexation in aqueous solutions is an equilibrium situation with drug/cyclodextrin complexes continually forming and dissociating with lifetimes in the range of milliseconds or less. Dilution is the major driving force for dissociation after parenteral administration. If the drugs are strongly bound or if dilution is minimal (e.g. topical administration), then competitive displacement from endogenous lipophiles contributes to the dissociation process. (Stella, V.J., Rao, V. M., Zannou, E. A. and Zia, V., Mechanisms of Drug Release From Cyclodextrin Complexes, Adv. Drug Del. Rev., 36(1), 3?16, 1999)