Cyclodextrins and derivatives in drug delivery: New developments, relevant clinical trials, and advanced products

Cyclodextrins (CD) and derivatives are functional excipients that can improve the bioavailability of numerous drugs. Because of their drug solubility improving properties they are used in many pharmaceutical products. Furthermore, the stability of small molecular drugs can be improved by the incorporation in CDs and an unpleasant taste and smell can be masked. In addition to well-established CD derivatives including hydroxypropyl-β-CD, hydroxypropyl-γ-CD, methylated- β-CD and sulfobutylated- β-CD, there are promising new derivatives in development.

In particular, CD-based polyrotaxanes exhibiting cellular uptake enhancing properties, CD-polymer conjugates providing sustained drug release, enhanced cellular uptake, and mucoadhesive properties, and thiolated CDs showing mucoadhesive, in situ gelling, as well as permeation and cellular uptake enhancing properties will likely result in innovative new drug delivery systems.

Relevant clinical trials showed various new applications of CDs such as the formation of CD-based nanoparticles, stabilizing properties for protein drugs or the development of ready-to-use injection systems. Advanced products are making use of various benefical properties of CDs at the same time. Within this review we provide an overview on these recent developments and take an outlook on how this class of excipients will further shape the landscape of drug delivery.

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Gergely Kali, Soheil Haddadzadegan, Andreas Bernkop-Schnürch, Cyclodextrins and derivatives in drug delivery: New developments, relevant clinical trials, and advanced products, Carbohydrate Polymers, Volume 324, 2024, 121500, ISSN 0144-8617, https://doi.org/10.1016/j.carbpol.2023.121500.

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