Cyclodextrins (CDs) are cyclic oligosaccharides of natural origin that were discovered morethan 100 years ago. The peculiar cone-like conformation of the sugar ring, expressing a lipophiliccavity and a hydrophilic external surface, allows these substances to spontaneously complex poorlysoluble compounds in an aqueous environment. For more than 50 years, these substances havefound applicability in the pharmaceutical and food industries as solubilizing agents for poorlysoluble chemical entities. Nowadays, several research groups all over the world are investigatingtheir potential as active pharmaceutical ingredients (APIs) for the treatment of several illnesses(e.g., hypercholesterolemia, cancer, Niemann-Pick Type C disease). The aim of this review is to brieflyretrace cyclodextrins’ legacy as complexing agents and describe the current and future prospects ofthis class of chemical entities in pharmaceutics as new APIs.
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