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水飞蓟宾磷脂复合物与水飞蓟素提取物在四氯化碳诱导的大鼠肝毒性中的抗氧化和保肝作用比较。

Antioxidant and hepatoprotective effects of silymarin phytosomes compared to milk thistle extract in CCl4 induced hepatotoxicity in rats.

机构信息

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University , Kasr El-aini Street, Cairo 11562 , Egypt and.

出版信息

J Microencapsul. 2014;31(1):23-30. doi: 10.3109/02652048.2013.805836. Epub 2013 Jul 1.

Abstract

Milk thistle extract is a well-known hepatoprotectant with low bioavailability (20-50%). The objective of the present study is to prepare and characterize silymarin phytosomes and to test the hepatoprotective effect of the phytosomes in CCl4 induced liver injury in rats compared to milk thistle extract. Phytosomes were prepared using lecithin from soybeans and from egg yolk. The prepared phytosomes were examined using scanning electron microscopy, transmission electron microscopy, differential scanning calorimetry, Fourier transform infrared spectroscopy and proton nuclear magnetic resonance spectroscopy (H(1)NMR). The loading efficiency was >85% in all phytosomal formulations. Formula P2 (with the molar ratio of soybean lecithin to silybin 1:1) and P4 (with the molar ratio of egg-yolk lecithin to silybin 0.25:1) exhibited significantly (p < 0.05) faster release than milk thistle extract. The in vivo study revealed that phytosomes significantly (p < 0.05) decreased glutamic pyruvic transaminase and super oxide dismutase activities compared to milk thistle extract.

摘要

水飞蓟素提取物是一种众所周知的具有低生物利用度(20-50%)的肝保护剂。本研究的目的是制备并表征水飞蓟宾类质体,并与水飞蓟素提取物进行比较,检测其在四氯化碳诱导的大鼠肝损伤中的肝保护作用。类质体使用大豆卵磷脂和蛋黄卵磷脂制备。使用扫描电子显微镜、透射电子显微镜、差示扫描量热法、傅里叶变换红外光谱和质子核磁共振波谱(H(1)NMR)对制备的类质体进行了检查。所有类质体配方的载药量均大于 85%。配方 P2(大豆卵磷脂与水飞蓟宾摩尔比为 1:1)和 P4(蛋黄卵磷脂与水飞蓟宾摩尔比为 0.25:1)的释放速度明显(p<0.05)快于水飞蓟素提取物。体内研究表明,与水飞蓟素提取物相比,类质体显著(p<0.05)降低了谷草转氨酶和超氧化物歧化酶的活性。

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