A Water-Soluble Inclusion Complex of Pedunculoside with the Polymer beta-Cyclodextrin: A Novel Anti-Inflammation Agent with Low Toxicity

作者：Liu, Chang; Zhang, Wang; Yang, Hao; Sun, Weidong; Gong, Xiangdong; Zhao, Junxian; Sun, Yun^*; Diao, Guowang

来源：PLos One, 2014, 9(7): e101761.

DOI：10.1371/journal.pone.0101761

• SAFETY EVALUATION
• EAR EDEMA
• IN-VITRO
• TERPENOIDS
• MICE
• INHIBITORS
• EFFICACY
• CANCER
• CELLS
• OIL

More than 50% of new drug candidates in drug discovery are lipophilic and exhibit poor aqueous solubility, which results in poor bioavailability and a lack of dose proportionality. Here, we improved the solubility of pedunculoside (PE) by generating a water-soluble inclusion complex composed of PE and the polymer beta-cyclodextrin (CDP). We characterized this novel complex by H-1 NMR, FT-IR, UV-vis spectroscopy, powder X-ray diffractometry and thermogravimetric analysis. The ratio of beta-cyclodextrin (beta-CD) units in CDP to PE was determined to be 2:1. The K-D value of the inclusion complex was determined to be 4.29x10(-3) mol.L-1. In contrast to the low solubility of PE, the water-solubility of the PE-CDP complex was greatly enhanced. A preclinical toxicological study indicated that PE-CDP was well tolerated for a single administration. Importantly, the anti-inflammation potency of the PE-CDP complex was higher than that of PE. As a result, the formation of inclusion complexes by water-soluble CDP opens up possible aqueous applications of insoluble drug candidates in drug delivery.

• 出版日期2014-7-11
• 单位扬州大学