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Cyclodextrins have occupied a preferential position in supramolecular chemistry and pharmaceutical technology for decades. Their molecular structure provides them with unique supramolecular features that have already found a plethora of applications for numerous purposes, including innovative solutions to formerly unmet pharmaceutical and biomedical challenges. The amalgamation of chemical, supramolecular and technological knowledge and the paradigmatic correlation between cyclodextrin structure and function has facilitated an unprecedent and fluent crosstalk among formerly distant research disciplines. This chapter emphasizes the role that cyclodextrins are playing in the era of nanosciences and the recent advances in cyclodextrins chemistry and technology that are making it feasible to address a broad range of pharmaceutical and biomedical challenges. A series of examples illustrates how the knowledge gained over a century of cyclodextrin research can applied: (i) for manipulation of the bioavailability of therapeutic agents, (ii) for the rational design of intelligent systems envisioned for targeted delivery and programmed release of cargos, (iii) for devising new therapeutic strategies for known maladies, and (iv) for the engineering of biosensing devices.

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