Silymarin, a known standardized extract obtained from seeds of Silybum marianum is used in treatment of liver diseases of varying origins. Aiming at improving its poor bioavailability from oral products, silymarin hybrid liposomes are introduced in this work for buccal administration after investigating their stability and in vivo hepatoprotective efficiency. Silymarin loaded hybrid liposomes composed of lecithin (L), cholesterol (Ch), stearyl amine (SA) and Tween 20 (T20) in molar ratio of (9:1:1:0.5) were prepared. Their stability upon storage was studied at 4 degrees C and at ambient conditions. Stored samples were analyzed for percent encapsulation, drug release, particle size, turbidity measurement and visual changes. Characterization of the blend between phospholipid and silymarin was done using FT-IR and DSC which indicated a possible interaction. The stabilized formula of silymarin hybrid liposomes was evaluated upon buccal administration regarding its hepatoprotective activity against carbon tetrachloride-induced oxidative stress in albino rats. The degree of protection was measured using biochemical parameters like serum glutamic oxalacetate transaminase (SGOT) and serum glutamic pyruvate transaminase (SGPT). The introduced silymarin hybrid liposomes produced a significant decrease in both transaminase levels when challenged with CCl(4) (intraperitonially) in comparison with orally administered silymarin suspension. This improvement was also confirmed histopathologically.

译文

:水飞蓟素是从水飞蓟种子中获得的一种已知的标准化提取物,用于治疗各种起源的肝脏疾病。为了改善口服产品的不良生物利用度,在研究了水飞蓟素混合脂质体的稳定性和体内保肝效率后,将其引入口腔给药。制备了由卵磷脂(L),胆固醇(Ch),硬脂胺(SA)和吐温20(T20)以摩尔比(9:1:1:0.5)组成的水飞蓟素杂化脂质体。在4℃和环境条件下研究了它们在储存时的稳定性。分析存储的样品的包封百分比,药物释放,粒径,浊度测量和外观变化。使用FT-IR和DSC对磷脂和水飞蓟素之间的混合物进行了表征,表明可能存在相互作用。经颊部给药评估了水飞蓟素杂化脂质体的稳定配方关于其在白化病大鼠中对四氯化碳诱导的氧化应激的肝保护活性。使用生化参数(例如血清谷氨酸草酰乙酸转氨酶(SGOT)和血清谷氨酸丙酮酸转氨酶(SGPT))测量保护程度。与口服水飞蓟素混悬液相比,引入的水飞蓟素杂化脂质体在受到CCl(4)挑战时(腹膜内)产生了两种转氨酶水平的显着降低。在组织病理学上也证实了这种改善。

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