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黄连素及其通过液体抗溶剂法制备的纳米颗粒的生物利用度和肝保护作用增强

Bioavailability and hepatoprotection enhancement of berberine and its nanoparticles prepared by liquid antisolvent method.

作者信息

Sahibzada Muhammad Umar Khayam, Zahoor Muhammad, Sadiq Abdul, Ur Rehman Fazl, Al-Mohaimeed Amal M, Shahid Muhammad, Naz Sumaira, Ullah Riaz

机构信息

Department of Pharmacy, Sarhad University of Science and Information Technology, Peshawar 26000, KPK, Pakistan.

Department of Biochemistry, University of Malakand, Chakdara, Lower Dir, 18800 KPK, Pakistan.

出版信息

Saudi J Biol Sci. 2021 Jan;28(1):327-332. doi: 10.1016/j.sjbs.2020.10.006. Epub 2020 Oct 15.

Abstract

The study was devised to prepare berberine nanoparticles by anti-solvent precipitation method and were assessed for their hepatoprotective effect in Male Sprague-Dawley rats against carbon tetrachloride. The pharmacokinetic parameters of the prepared nanoparticles and berberine were evaluated in rabbits. Histopathological studies and blood biochemical analyses were carried out to evaluate the role of both forms of berberine in the experimental animals. Substantial improvement in the liver function test enzymes levels and liver histopathology were achieved in the animals treated with berberine nanoparticles in comparison to the unprocessed berberine whereas, pharmacokinetic parameters for nanoform of berberine were about 3.97 and 3.88 folds higher than that of the unprocessed berberine. The study revealed that the reduction of berberine particle size to nano range improved pharmacokinetic parameters in rabbits. The nano berberine provided better liver protection in experimental rats and high berberine blood concentration. Thus, better hepatoprotective and pharmacokinetics effects were observed for the nano form in comparison to unprocessed form.

摘要

该研究旨在通过反溶剂沉淀法制备小檗碱纳米颗粒,并评估其对雄性Sprague-Dawley大鼠四氯化碳肝损伤的保护作用。在兔体内评估了所制备纳米颗粒和小檗碱的药代动力学参数。进行了组织病理学研究和血液生化分析,以评估两种形式的小檗碱在实验动物中的作用。与未加工的小檗碱相比,用小檗碱纳米颗粒处理的动物肝功能测试酶水平和肝脏组织病理学有显著改善,而小檗碱纳米形式的药代动力学参数比未加工的小檗碱高约3.97倍和3.88倍。该研究表明,将小檗碱粒径减小至纳米范围可改善兔的药代动力学参数。纳米小檗碱在实验大鼠中提供了更好的肝脏保护和高血药浓度。因此,与未加工形式相比,纳米形式具有更好的肝脏保护和药代动力学效果。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2a7b/7783676/86207c68765d/gr1.jpg

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