Cyclodextrins are cyclic oligosaccharides produced through the enzymatic degradation of starch (e.g., by cyclodextrin glycosyltransferase, CGTase). Their molecular structure features:
• Hydrophilic exterior (hydroxyl-rich, ensuring good water solubility)
• Hydrophobic cavity (capable of encapsulating nonpolar molecules)
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Poor water solubility remains a critical hurdle in pharmaceutical development—affecting approximately 40% of marketed drugs and 75% of pipeline compounds. To address dissolution and controlled-release challenges, drug carriers are commonly employed, though formulation development remains technically demanding.
Among pharmaceutical carriers, cyclodextrins (CDs) have emerged as the most widely used system due to their superior molecular encapsulation capabilities. To date, over 130 drug products utilizing natural or modified CDs have gained global approval, spanning multiple therapeutic areas.
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The acceptance of cyclodextrins as food additives is steadily increasing. With production methods having become more appropriate and cost-effective, cyclodextrins can now be incorporated into food products at reasonable price points. Consequently, cyclodextrins enjoy promising future prospects due to growing consumer demand for health-focused and functional food products.
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Nucleic acid drugs (e.g., mRNA vaccines, siRNA therapies) face challenges such as poor stability, low cellular uptake efficiency, and rapid degradation in vivo. Cyclodextrins (CDs) can address these issues by:
√ Protecting nucleic acids from RNase/DNase degradation via electrostatic interactions or inclusion complexation
√ Enhancing cellular uptake and endosomal escape
√ Enabling targeted delivery and reducing toxicity
Compared to traditional carriers (e.g., lipid nanoparticles (LNPs), polymeric carriers), cyclodextrin-based delivery systems offer:
√ Superior biocompatibility (as natural derivatives, some CDs are FDA-approved)
√ Greater flexibility in chemical modification (e.g., cationic, PEGylated, or ligand-conjugated CDs)
√ Simpler manufacturing processes and cost-effectiveness
√ Retained activity after lyophilization (critical for mRNA vaccine storage)
Cyclodextrin Technology