Posted by Cyclodextrins have long been known as host molecules, a special feature that has led to their widespread use in a variety of fields, including cosmetics, food, agriculture and, in particular, pharmaceuticals. In the latter field, cyclodextrins have mainly been used as excipients. However, recent studies have shed light on their use, not only as excipients, but also as active pharmaceutical ingredients themselves.
Cyclodextrins: From Excipients to Active Ingredients
Since their discovery in 1891, cyclodextrins were initially valued for their ability to encapsulate and improve the functionalities of active compounds. Over time, the pharmaceutical industry recognized their usefulness primarily for their efficacy and biocompatibility. Cyclodextrins were first incorporated into drug formulations in the 1970s, starting with Prostarmon E™ (launched in Japan in 1976). Since then, more than 130 approved drug formulations have incorporated cyclodextrins as excipients.
Recently, a new level of interest in cyclodextrins has emerged: their role as active ingredients.
Research has shown that cyclodextrins can act as scavengers or artificial receptors, capable of capturing and neutralizing toxic compounds or even modulating cholesterol levels targeting a wide range of diseases and bringing hope to rare and orphan diseases such as Stargardt and Niemann-Pick C. In addition, studies have suggested the potential benefits of cyclodextrins in the therapy of COVID-19 and other viral infections.
On the road to eternity?
While the potential for cyclodextrins in medicine is huge, there are still challenges to overcome. One of the main hurdles is to simplify and standardize the synthesis of cyclodextrin derivatives. Small changes in their molecular structure can have a significant impact on their efficacy. Additionally, long-term safety data are still needed, especially for newer treatments. Nevertheless, the revival of cyclodextrins as active ingredients is a significant step forward in pharmaceutical research, offering hope for the treatment of various diseases.
Cyclodextrins are no longer just hosts. They are becoming key players in the future of medicine
M. Kfoury, E. Lichtfouse, S. Fourmentin: The revival of cyclodextrins as active pharmaceutical ingredients. Environmental Chemistry Letters. https://doi.org/10.1007/s10311-024-01782-8