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Abstract
Cyclodextrins are useful functional excipients that have enjoyed widespread attention
and use. The basis for this popularity from a pharmaceutical standpoint, is the ability
of these materials to interact with poorly water-soluble drugs and drug candidates
resulting in an increase in their apparent water solubility. The mechanism for this
solubilization is rooted in the ability of cyclodextrin to form non-covalent dynamic
inclusion complexes in solution. Other solubilizing attribute may include the ability
to form non-inclusion based complexes, the formation of aggregates and related domains
and the ability of cyclodextrins to form and stabilize supersaturated drug solutions.
The increase in solubility also can increase dissolution rate and thus improve the
oral bioavailability of BCS Class II and IV materials. A number of cyclodextrin-based
products have reached the market based on their ability to camouflage undesirable
physicochemical properties. This review is intended to give a general background to
the use of cyclodextrin as solubilizers as well as highlight kinetic and thermodynamic
tools and parameters useful in the study of drug solubilization by cyclodextrins.