Cyclodextrin‐Amino Acid Conjugates: Synthesis and Pharmaceutical Applications

Cyclodextrins (CDs) are cyclic oligosaccharides extensively utilized in pharmaceutical sciences owing to their ability to form inclusion complexes with a wide variety of hydrophobic guest molecules. This has made them invaluable carriers in drug delivery, enabling improvements in solubility, stability, and bioavailability of therapeutic agents. Beyond these intrinsic advantages, the chemical derivatization of CDs with amino acids (AAs) represents an emerging strategy to further expand their functional landscape. Such modifications not only enhance aqueous solubility and finely tune the binding selectivity but also introduce opportunities for designing stimuli‐responsive systems. The scope of this review is to provide a comprehensive overview of the current synthetic methodologies for both mono‐ and per‐substituted amino‐acid cyclodextrin derivatives. Coupling can be achieved through the amino, carboxyl, or specific side‐chain functionalities of AAs, thereby offering a versatile toolbox for tailoring structural and functional features. By consolidating knowledge on these synthetic strategies and highlighting representative applications, this work emphasizes the broad potential of AA‐CDs as adaptable platforms for biomedical use. Integrating these functionalized CDs into next generation nanocarriers and multifunctional therapeutic systems may pave the way toward innovative solutions for complex clinical challenges.