Sulfobutylether-β-cyclodextrin – Captisol®

This review presents the early history, the motivation, the research and some of the backstories behind the discovery and development of sulfobutylether-β-cyclodextrin as a novel parenterally safe solubilizer and stabilizer. A specific sulfobutylether-β-cyclodextrin with an average degree of 6.5 sulfobutyl-groups variably substituted on the 2-, 3- and 6-hydroxyls of the seven glucopyranose (dextrose) units of β-cyclodextrin, is known by its commercial name, Captisol®. Today it is in 13 FDA approved injectables and numerous clinical candidates. It is also an example of a novel product discovered and initially preclinically developed at an academic institution. Access the full publication here

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Some insights from this review:

FDA approved products utilizing Captisol
The first FDA approved product containing Captisol was Pfizer’s anti-psychotic-schizophrenia product Geodon® IM (ziprasidone mesylate) for intramuscular (IM) injection. Geodon IM is used to help treat patients in acute crisis. Here Captisol® prevented site-of-injection precipitation of the poorly water-soluble free base allowing for quantitative and rapid release following IM injection.

This was followed by Pfizer’s Vfend® IV (voriconazole). The delay in marketing was a business decision as the anti-fungal market decreased when effective anti-HIV drugs slowed the incidence of life-threatening fungal infections associated with AIDs. There is a now two additional generic forms of voriconazole IM approved that also utilize Captisol®. … continue reading here

Conclusion
This short history of the discovery and initial development steps at an academic institution of Captisol® as a novel pharmaceutical solubilizer and stabilizer provides some an insight into the challenges faced by investigators and graduate students. It provides a path to help others to consider following.

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Keywords: Cyclodextrin, Captisol. Solubility, Formulation, Stability, Synthesis, Safety