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

Abstract

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 1H 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 Ks (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.

Artificial transmembrane potassium transporters: designs, functions, mechanisms and applications

“…They possess hydrophobic cavity interiors capable of forming complexes with various guest molecules. 44,45 Artificial ion channels are formed by designing suitable cyclodextrin structures and introducing appropriate functional groups. Xin et al successfully synthesized artificial potassium ion channels, 7a-7c, by combining columnar aromatic hydrocarbons with cyclodextrins (Fig.…”

Advances in nanoscale carrier-based approaches to reduce toxicity and enhance efficacy of podophyllotoxin

“…Cyclodextrins (CDs) are prominently suitable for functional delivery systems in the pharmaceutical industry [115,116]. Gamma-cyclodextrin (γ-CD), because of its appropriate geometric size, was selected to prepare a PPT inclusion complex [117]. The inclusion complex formed in a 1:1 ratio with a considerable apparent stability constant Ks (4245.5 L•mol −1 ), which greatly improved PPT water solubility.…”

Research Progress on Synthesis and Application of Cyclodextrin Polymers

“…Guo et al [ 46 ] prepared an inclusion compound of podophyllotoxin (PPT) and -CD, which could greatly reduce the toxicity of PPT. The behavior, characterization, and water solubility of the inclusion compound were carefully studied using multiple techniques.…”