BACKGROUND Quercetin, a pigment (flavonoid) found in many plants and foods, has good effects on protecting liver function but poor solubility and bioavailability in vivo. A drug delivery system can improve the accumulation and bioavailability of quercetin in liver. In this study, we used liposomal nanoparticles to entrap quercetin and evaluated its protective and therapeutic effects on drug-induced liver injury in rats. METHODS The nanoliposomal quercetin was prepared by a thin film evaporation-high pressure homogenization method and characterized by morphology, particle size and drug content. Acute liver injury was induced in rats by composite factors, including carbon tetrachloride injection, high-fat corn powder intake and ethanol drinking. After pure quercetin or nanoliposomal quercetin treatment, liver function was evaluated by detecting serum levels of glutamic-pyruvic transaminase (GPT), glutamic-oxal acetic transaminase (GOT) and direct bilirubin (DBIL). Histology of injured liver tissues was evaluated by hematoxylin and eosin staining. RESULTS On histology, liposomal nanoparticles loading quercetin were evenly distributed spherical particles. The nanoliposomal quercetin showed high bioactivity and bioavailability in rat liver and markedly attenuated the liver index and pathologic changes in injured liver tissue. With nanoliposomal quercetin treatment, the serum levels of GPT, GOT and DBIL were significantly better than treated with pure quercetin. Using liposomal nanoparticles to entrap quercetin might be an effective strategy to reduce hepatic injury and protect hepatocytes against damage. CONCLUSION Liposomal nanoparticles may improve the solubility and bioavailability of quercetin in liver. Furthermore, nanoliposomal quercetin could effectively protect rats against acute liver injury and may be a new hepatoprotective and therapeutic agent for patients with liver diseases.

中文翻译：

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纳米脂质体槲皮素对大鼠急性肝损伤的保护和治疗作用。

背景技术槲皮素是一种存在于多种植物和食品中的色素（类黄酮），具有良好的肝功能保护作用，但在体内的溶解度和生物利用度较差。药物递送系统可以提高槲皮素在肝脏中的积累和生物利用度。在本研究中，我们使用脂质体纳米颗粒包埋槲皮素，并评估其对大鼠药物性肝损伤的保护和治疗作用。方法采用薄膜蒸发-高压均质法制备槲皮素纳米脂质体，并对其形貌、粒径和药物含量进行表征。四氯化碳注射液、高脂玉米粉摄入和乙醇饮用等复合因素诱发大鼠急性肝损伤。纯槲皮素或纳米脂质体槲皮素治疗后，通过检测血清谷丙转氨酶（GPT）、谷草乙醛转氨酶（GOT）和直接胆红素（DBIL）水平评估肝功能。通过苏木精和伊红染色评估受损肝组织的组织学。结果从组织学上看，负载槲皮素的脂质体纳米颗粒呈均匀分布的球形颗粒。纳米脂质体槲皮素在大鼠肝脏中表现出较高的生物活性和生物利用度，并显着减轻肝脏指数和受损肝组织的病理变化。纳米脂质体槲皮素治疗后，血清GPT、GOT和DBIL水平明显优于纯槲皮素治疗。使用脂质体纳米粒子包埋槲皮素可能是减少肝损伤并保护肝细胞免受损伤的有效策略。结论纳米脂质体可以提高槲皮素在肝脏中的溶解度和生物利用度。此外，纳米脂质体槲皮素可以有效保护大鼠免受急性肝损伤，可能成为肝病患者的一种新的保肝和治疗药物。