Journal
PHARMACEUTICS
Volume 11, Issue 3, Pages -Publisher
MDPI
DOI: 10.3390/pharmaceutics11030107
Keywords
6-shogaol; cytotoxic effect; HepG2 cells; micelles; hepatoprotection
Categories
Funding
- National Natural Science Foundation of China [30973677, 81373371]
- China Postdoctoral Science Foundation [2018M630533]
- Program for Scientific research innovation team in Colleges and Universities of Jiangsu Province
- Priority Academic Program Development of Jiangsu Higher Education Institutions
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6-shogaol is a promising anti-cancer and anti-inflammatory agent. However, the treatment effectiveness of 6-shogaol is limited by poor water solubility, poor oral absorption and rapid metabolism. Herein, 6-shogaol loaded in micelles (SMs) were designed to improve 6-shogaol's solubility and bioavailability. The micelles of a PEG derivative of linoleic acid (mPEG(2k)-LA) were prepared by the nanoprecipitation method with a particle size of 76.8 nm, and entrapment of 81.6 %. Intriguingly, SMs showed a slower release in phosphate buffer saline (PBS) (pH = 7.4) compared to free 6-shogaol while its oral bioavailability increased by 3.2-fold in vivo. More importantly, the in vitro cytotoxic effect in HepG2 cells of SMs was significantly higher than free 6-shogaol. Furthermore, SMs could significantly improve the tissue distribution of 6-shogaol, especially liver and brain. Finally, SMs showed a better hepatoprotective effect against carbon tetrachloride (CCl4)-induced hepatic injury in vivo than free 6-shogaol. These results suggest that the novel micelles could potentiate the activities of 6-shogaol in cancer treatment and hepatoprotection.
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