Captisol® is a patent protected, uniquely modified cyclodextrin, whose chemical structure was rationally designed to maximize safety and optimize interaction to improve the solubility, stability, bioavailability or lessen volatility, irritation, smell or taste.
Captisol® is a polyanionic beta-cyclodextrin derivative with a sodium sulfonate salt separated from the lipophilic cavity by a butyl ether spacer group, or sulfobutylether (SBE). Captisol® is not a single chemical species, but comprised of a multitude of polymeric structures of varying degrees of substitution and positional/regional isomers dictated and controlled to a uniform pattern by a patented manufacturing process consistently practiced and improved to control impurities.
The selection of Captisol® and its desirable safety profile and drug solubilization properties was based upon extensive evaluations of the mono, tetra and hepta-substituted dominated compositions. Captisol® is the trade name for Ligand's modified beta-cyclodextrin technology.
Several hundred of pre-clinical and clinical studies have been performed and indicate that Captisol® is safe when administered parenterally or orally and does not exhibit the nephrotoxicity associated with beta-cyclodextrin. Relative to beta-cyclodextrin, Captisol® provides higher interaction characteristics and superior water solubility in excess of 100 grams/100 ml – a 50-fold improvement.