The pharmaceutical applications of cyclodextrins (CDs), cyclic oligosaccharides capable of including
hydrophobic molecules inside their cavities, have been known for decades. Besides the solubilising and encapsulating
abilities of natural and modified CDs due to the formation of inclusion complexes, there is an increasing
interest in organized macrostructures based on CDs as potential drug delivery devices and gene carrier systems.
The present review discusses first the case of drug carriers based on monomeric modified CDs (amphiphilic and
CD core-star polymers), in which self-assembly plays a major role. Polyrotaxanes, i.e., CDs threaded onto a
polymer chain, are then reviewed in relation to their pharmaceutical applications. Finally, covalently linked CDs,
either by grafting or crosslinking, are analyzed, including more complex structures formed by assembling CDcontaining
networks or chains. We have tried along this review to cover the most recent developments on these
structures for drug delivery in a “beyond the cyclodextrin” approach. The review will be helpful, both for readers
who want to be introduced into the world of these remarkable structures, or for specialists who are doing research
in this field.