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

被引：35

作者：

Liu, Chang ^{[1
]}

Zhang, Wang ^{[2
]}

Yang, Hao ^{[1
]}

Sun, Weidong ^{[3
]}

Gong, Xiangdong ^{[2
]}

Zhao, Junxian ^{[1
]}

Sun, Yun ^{[1
]}

Diao, Guowang ^{[2
]}

机构：

[1] Yangzhou Univ, Coll Med, Yangzhou, Jiangsu, Peoples R China

[2] Yangzhou Univ, Coll Chem & Chem Engn, Yangzhou, Jiangsu, Peoples R China

[3] Chinese Med Hosp Yangzhou City, Yangzhou, Jiangsu, Peoples R China

来源：

PLOS ONE | 2014年 / 9卷 / 07期

基金：

中国国家自然科学基金;

关键词：

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

D O I：

10.1371/journal.pone.0101761

中图分类号：

O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];

学科分类号：

07 ; 0710 ; 09 ;

摘要：

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.

引用

页数：9

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