Improved art bioactivity by encapsulation within cyclodextrin carboxylate

Artemisinin (Art) is a natural sesquiterpene lactone that is claimed to exhibit various bioactivities. The poor solubility of Art in both water and oil hinders its application in formulations intended for oral administration. In this study, we investigated the potential of forming a host–guest complex between Art and succinic acid modified cyclodextrin (SACD) to improve its solubility characteristics. Art-SACD inclusion complexes (2:1 M ratio) were successfully formed in water, which was attributed to the relatively large cavity size of SACD, as well as the intermolecular interactions between the Art and succinic acid branches in the cavity. The thermal stability of the Art was retained after incorporation into the Art-SACD complexes, which may be useful for applications such as pasteurization or cooking. The encapsulated Art showed antibacterial activity against both Gram-positive and Gram-negative bacteria. Such encapsulation technology allows Art to be introduced into oral delivery systems in a bioactive form.