Inclusion Complex of Podophyllotoxin with γ-Cyclodextrin: Preparation, Characterization, Anticancer Activity, Water-Solubility and Toxicity

An inclusion complex of podophyllotoxin (PPT) with γ -cyclodextrin ( γ -CD) was prepared. The behavior, characterization, and water solubility of the inclusion complex were carefully investigated via fluorescence spectroscopy, thermogravimetry, differential scanning calorimetry, X-ray diffraction analysis, and 1 H and 2D nuclear magnetic resonance spectroscopy. Furthermore, antitumor activity to human cancer lines and toxicity in mice were studied. Results showed that the inclusion complex formed in a 1:1 ratio with a considerable apparent stability constant K s (4245.5 L·mol −1 ). Water solubility was considerably improved. In addition, the anticancer activity of the inclusion complex was better than that of cis -platinum (DDP, positive control). Most importantly, the toxicity of podophyllotoxin inclusion complex reduced and became more safety to mice which will be great valuable to research its applications as a kind of antitumor drug to human in the further.