Posted by 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 amino acidAs, 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 amino acid-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.
Functionalization of CDs with residues such as Arg, Tyr, or Phe enhances host–guest interactions, enabling efficient encapsulation of chemotherapeutics like DOX and platinum complexes, while improving cellular uptake and reducing off-target toxicity. Modified CDs, including cross-linked polymers and MOF-based systems-demonstrate controlled, stimuli-responsive release, thermal or redox-triggered delivery, and enhanced stability under physiological and gastrointestinal conditions.
Cesari, Andrea, Lomuscio, Nicola, Bellina, Fabio (2026) Cyclodextrin-Amino Acid Conjugates: Synthesis and Pharmaceutical Applications. ChemistryEurope 4, 2751-4765. https://doi.org/10.1002/ceur.202500473