Cyclodextrin-Based Delivery of Traditional Chinese Medicine Active Molecules

Active molecules derived from traditional Chinese medicine (TCM) represent a valuable source of lead compounds for modern drug discovery, demonstrating considerable potential in the prevention and treatment of chronic diseases, cancer therapy, and immune modulation. Nevertheless, their clinical translation is often impeded by intrinsic limitations such as poor aqueous solubility, low bioavailability, inadequate chemical stability, and significant gastrointestinal irritation. Cyclodextrins (CDs) and their derivatives, characterized by a hydrophobic internal cavity, are capable of forming inclusion complexes with TCM and their derived active constituents, thereby improving their physicochemical and pharmacokinetic profiles. Over the past five years, substantial progress has been made in this domain. CD-based inclusion strategies have been shown to markedly enhance the solubility and dissolution rate of poorly water-soluble TCM compounds, including flavonoids, alkaloids, and terpenoids. Moreover, this approach contributes to improved drug stability, effective taste masking, and the achievement of modified release profiles, such as sustained or targeted delivery, ultimately leading to enhanced therapeutic efficacy and reduced adverse effects. The development of novel CD derivatives and smart delivery systems has further broadened their application potential. This review summarizes recent advances in the CD-based encapsulation of TCM active molecules, highlighting key formulation strategies that address persistent challenges in the modernization of TCM. It also provides a foundation for future research and development in natural product-based therapeutics.