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,从水飞蓟素种子中获得的已知标准化提取物,用于治疗不同来源的肝脏疾病。为了改善口服产品的生物利用度,在研究其稳定性和体内保肝效率后,将水飞蓟素杂交脂质体引入口腔给药。制备了由卵磷脂 (L),胆固醇 (Ch),硬脂胺 (SA) 和吐温20 (T20) 组成的水飞蓟素杂化脂质体,摩尔比为 (9:1:1:0.5)。在4摄氏度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,浊度测量和视觉变化。使用ft-ir和DSC对磷脂和水飞蓟素之间的混合物进行表征,这表明可能存在相互作用。在颊给药后评估了水飞蓟素混合脂质体的稳定配方,以评估其对白化病大鼠四氯化碳诱导的氧化应激的保肝活性。使用生化参数 (例如血清谷草转氨酶 (SGOT) 和血清谷丙酮酸转氨酶 (SGPT)) 测量保护程度。与口服水飞蓟素混悬液相比,引入的水飞蓟素混合脂质体在用CCl(4) 攻击时 (腹膜内) 使两种转氨酶水平均显着降低。这种改善也在组织病理学上得到证实。

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