Improvement of Oral Bioavailability and Anti-Tumor Effect of Zingerone Self-Microemulsion Drug Delivery System

被引：31

作者：

Cao, Xia ^{[1
]}

Zhu, Qin ^{[1
]}

Wang, Qi-Long ^{[1
]}

Adu-Frimpong, Michael ^{[2
]}

Wei, Chun-Mei ^{[1
]}

Weng, Wen ^{[1
]}

Bao, Rui ^{[1
]}

Wang, Ya-Ping ^{[1
]}

Yu, Jiang-Nan ^{[1
]}

Xu, Xi Ming ^{[1
]}

机构：

[1] Jiangsu Univ, Ctr Nano Drug Gene Delivery & Tissue Engn, Sch Pharm, Dept Pharmaceut, Zhenjiang, Jiangsu, Peoples R China

[2] Kwame Nkrumah Univ Sci & Technol, Dept Biochem & Biotechnol, Kumasi, Ghana

来源：

JOURNAL OF PHARMACEUTICAL SCIENCES | 2021年 / 110卷 / 07期

基金：

中国国家自然科学基金;

关键词：

Zingerone; Self-emulsifying; Pharmacokinetic; Oral drug delivery; Bioavailability apoptosis; IN-VITRO; ZINGIBER-OFFICINALE; OXIDATIVE STRESS; FORMULATION; SMEDDS; ANTICANCER; PERMEABILITY; INFLAMMATION; ENHANCEMENT; OIL;

D O I：

10.1016/j.xphs.2021.01.037

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

This study sought to prepare a self-microemulsion drug delivery system containing zingerone (ZSMEDDS) to improve the low oral bioavailability of zingerone and anti-tumor effect. Z-SMEDDS was characterized by particle size, zeta potential and encapsulation efficiency, while its pharmacokinetics and anti-tumor effects were also evaluated. Z-SMEDDS had stable physicochemical properties, including average particle size of 17.29 +/- 0.07 nm, the zeta potential of -22.81 +/- 0.29 mV, and the encapsulation efficiency of 97.96% +/- 0.02%. In vitro release studies have shown the release of zingerone released by ZSMEDDS was significantly higher than free zingerone in different release media. The relative oral bioavailability of Z-SMEDDS was 7.63 times compared with free drug. Meanwhile, the half inhibitory concentration (IC50)of Z-SMEDDS and free zingerone was 8.45 mg/mL and 13.30 mg/mL, respectively on HepG2. This study may provide a preliminary basis for further clinical research and application of ZSMEDDS. (C) 2021 Published by Elsevier Inc. on behalf of the American Pharmacists Association.

引用

页码：2718 / 2727

页数：10

共 52 条

[1] Novel cuminaldehyde self-emulsified nanoemulsion for enhanced antihepatotoxicity in carbon tetrachloride-treated mice [J].