With this historical paper, prof. Stella and Dr. Rajevski wanted to honor to Dr. Thornsteinn Loftsson, Professor Emeritus at University of Iceland (a former student at Kansas University) on the occasion of his 70th birthday.
The gripping story of the inventors started in the early 1980s at Kansas University (see the featured image above), continued with patent application filed in 1990 to US Patent Office, and still has not been finished yet as more and more drugs are being developed by using sulfobutylether β-cyclodextrin. While reading the paper the following exciting questions are answered:
- How the idea of developing a charged cyclodextrin derivative was born?
- Why β-cyclodextrin and not α- or γ-cyclodextrins?
- Why a sulfonic acid derivative?
- Why sulfobutyl and not sulfopropyl (the effect of spacer length between the charge and the cavity)?
- What about safety issues?
- Why SBE-β-CDs with an average of about seven degrees of substitution?
- How the interference process of two patents (Janssen and US-NIH) on HP-β-CD pushed Pfizer, the big American Pharma company to buy the license from University of Kansas for the development of voriconazole formulation with SBE-β-CDs?
- What was the role of Cydex and later Ligand in development of products with Captisol®?
The paper of Stella and Rajevski is interesting for the newcomers in cyclodextrin research as well as for those who witnessed at least some parts of this history.
Valentino J. Stella and Roger A. Rajewski (2020) Sulfobutylether-β-Cyclodextrin. Int J Pharm. 2020 May 4 : 119396. doi: 10.1016/j.ijpharm.2020.119396 [Epub ahead of print]