Abstract The current research was intended to establish the impact of Silibinin nanoparticles (SB-APSP) produced by the antisolvent precipitation with a syringe pump (APSP). The in-vivo bioavailability and hepatoprotective activity of SB-APSP were evaluated in experimental animals. To determine the pharmacokinetic parameters, silibinin and its nanoparticles were given orally to rabbits at a dose of 50 mg/Kg body weight. Blood samples were drawn at different time intervals and were analyzed using HPLC. The bioavailability of un processed silibinin was lower as compared to silibinin nanoparticles (3.45 ± 0.07 and 23.76 ± 0.07 µg/mL respectively). The AUC and Cmax of SB-APSP were found to be 15.56 and 6.88 folds greater for nanoparticles when compared to silibinin. Hepatoprotective study in Male Sprague Dawley rats revealed that SB-APSP provide better recovery of the damaged liver cell induced by CCl4. Histopathology of the liver revealed that SB-APSP provide better protection to the liver cells from the damage induced by CCl4 and maintained the hepatic lobule histopathology more efficiently. It was concluded that the SB-APSP can more effectively protect the liver in experimental animals in a far better way compared to the un-processed Silibinin and could be used as an efficient hepatoprotective agent.

中文翻译：

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水飞蓟宾通过转化为液体抗溶剂法制备的纳米颗粒增强生物利用度和保肝作用

摘要 目前的研究旨在确定由注射泵 (APSP) 反溶剂沉淀产生的水飞蓟宾纳米粒子 (SB-APSP) 的影响。在实验动物中评估了 SB-APSP 的体内生物利用度和保肝活性。为了确定药代动力学参数，将水飞蓟宾及其纳米颗粒以 50 mg/Kg 体重的剂量口服给予兔子。在不同的时间间隔抽取血样并使用 HPLC 进行分析。与水飞蓟宾纳米颗粒相比，未加工的水飞蓟宾的生物利用度较低（分别为 3.45 ± 0.07 和 23.76 ± 0.07 µg/mL）。与水飞蓟宾相比，纳米颗粒的 SB-APSP 的 AUC 和 Cmax 被发现是 15.56 和 6.88 倍。雄性 Sprague Dawley 大鼠的保肝研究表明，SB-APSP 可以更好地恢复由 CCl4 诱导的受损肝细胞。肝脏组织病理学表明，SB-APSP 为肝细胞提供更好的保护，使其免受 CCl4 诱导的损伤，并更有效地维持肝小叶组织病理学。得出的结论是，与未加工的水飞蓟宾相比，SB-APSP 可以以更好的方式更有效地保护实验动物的肝脏，并可用作有效的保肝剂。