Cyclodextrin as a magic switch in covalent and non-covalent anticancer drug release systems

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This article reviews the controlled release of current anticancer drugs based on cyclodextrins as a “flexible switch”, and discusses the classification of different types of release systems, highlighting their role in cancer treatment. Moreover, the opportunities and challenges of cyclodextrin as a magic switch in the controlled release of anticancer drugs are discussed. Through several examples, the review puts emphasis on the versatility of cyclodextrin as drug delivery vehicle: the produg concept is based on utilization of the hydroxyl groups on the cyclodextrin rims, the concept of inclusion complex formation is based on non-covalent hydrophobic interactions between the drug and the cyclodextrin cavity.

CD-bound drugs need to reach the colon site for release, and this colonic administration provides a potential route of application. In particular, the main strategy for forming prodrug is to use an ester or amide bond between the active group on the drug or linker and the hydroxyl group on the cyclodextrin. Only drugs or linkers with active groups such as carboxyl groups can be linked to cyclodextrin.


Tian, B., Liu, Y., & Liu, J. (2020). Cyclodextrin as a magic switch in covalent and non-covalent anticancer drug release systems. Carbohydrate Polymers, 116401. doi:10.1016/j.carbpol.2020.116401

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