Preparation and characterization of a novel host-guest complex based on folate-modified β-cyclodextrin and artesunate

Abstract The purpose of this study was to develop a novel folate-modified host-guest complex to enhance antitumor activity of the artesunate and improve the solubility and stability by encapsulated in β-cyclodextrin and linked with folate. In this work, we designed and prepared the inclusion complex of adamantanamine conjugated artesunate (AD-ATS) with folic acid-ethylenediamine-β-cyclodextrin (FA-EN-β-CD). This material was characterized by 1D and 2D NMR, XRD, TG and SEM. The results suggested that AD-ATS was encapsulated within the FA-EN-β-CD cavity to form host-guest inclusion complex, and the water solubility of AD-ATS was improved in the form of inclusion complex with FA-EN-β-CD. The assessment of antitumor activity showed that cytotoxicity of AD-ATS/FA-EN-β-CD complex was significantly enhanced in comparison to free AD-ATS, ATS/β-CD inclusion complex and ATS/FA-EN-β-CD inclusion complex.