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Development of TPGS/F127/F68 mixed polymeric micelles: Enhanced oral bioavailability and hepatoprotection of syringic acid against carbon tetrachloride-induced hepatotoxicity.
Food and Chemical Toxicology ( IF 4.3 ) Pub Date : 2020-01-16 , DOI: 10.1016/j.fct.2020.111126
Congyong Sun 1 , Wenjing Li 1 , Ping Ma 1 , Yang Li 1 , Yuan Zhu 1 , Huiyun Zhang 1 , Michael Adu-Frimpong 1 , Wenwen Deng 1 , Jiangnan Yu 1 , Ximing Xu 1
Affiliation  

Syringic acid (SA), a natural polyphenol found in fruits and vegetables, is claimed to show notable hepatoprotection. Nevertheless, low solubility and bioavailability hamper the application of SA. This study aimed to investigate the potential of TPGS/F127/F68 mixed polymeric micelles as a sustained and liver-targeting nanocarrier for SA. Herein, the prepared SA-loaded TPGS/F127/F68 mixed polymeric micelles (SA-TPGS-Ms) were spherically-shaped and homogeneously-distributed nanoparticles with high entrapment efficiency (94.67 ± 2.05%) and sustained release. Besides, in-vitro cell culture studies revealed that SA-TPGS-Ms substantially promoted cellular uptake with excellent biocompatibility. After oral administration, SA-TPGS-Ms demonstrated an increased bioavailability (2.3-fold) and delayed in-vivo elimination compared with the free SA. Furthermore, the alleviation of oxidative stress and amelioration of hepatic injury in CCl4-induced hepatotoxicity mice further demonstrated the excellent hepatoprotection of SA-TPGS-Ms. Collectively, SA-TPGS-Ms could be a promising nanocarrier for the utilization of SA in functional foods, with enhanced bioavailability and hepatoprotection.

中文翻译:

TPGS / F127 / F68混合聚合物胶束的开发:增强口服生物利用度和丁香酸对四氯化碳引起的肝毒性的肝保护作用。

丁香酸(SA)是一种在水果和蔬菜中发现的天然多酚,据称具有显着的肝保护作用。然而,低溶解度和生物利用度阻碍了SA的应用。这项研究旨在调查TPGS / F127 / F68混合聚合物胶束作为SA的持续且靶向肝的纳米载体的潜力。在此,制备的负载SA的TPGS / F127 / F68混合聚合物胶束(SA-TPGS-Ms)是球形的且均匀分布的纳米颗粒,具有高的包封率(94.67±2.05%)并持续释放。此外,体外细胞培养研究表明,SA-TPGS-Ms以优异的生物相容性大大促进了细胞摄取。口服后,与游离SA相比,SA-TPGS-Ms具有更高的生物利用度(2.3倍),并且体内清除延迟。此外,CCl4诱导的肝毒性小鼠中氧化应激的减轻和肝损伤的改善进一步证明了SA-TPGS-Ms具有出色的肝保护作用。总而言之,SA-TPGS-Ms可能是有前途的纳米载体,可用于在功能性食品中利用SA,并具有更高的生物利用度和肝保护作用。
更新日期:2020-01-16
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