El-Samaligy Mohamed S, Afifi Nagia N, Mahmoud Enas A
Department of Pharmaceutics, Faculty of Pharmacy, Cairo University, Kasr El-aini Street, Cairo, Egypt.
Int J Pharm. 2006 Aug 17;319(1-2):121-9. doi: 10.1016/j.ijpharm.2006.04.023. Epub 2006 Jun 9.
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.
水飞蓟素是一种从水飞蓟种子中提取的标准化提取物,用于治疗各种病因引起的肝病。为了改善其口服制剂较差的生物利用度,本研究引入了水飞蓟素混合脂质体用于颊部给药,并研究了其稳定性和体内保肝效率。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)组成的载水飞蓟素混合脂质体。在4℃和环境条件下研究了它们储存时的稳定性。对储存的样品进行包封率、药物释放、粒径、浊度测量和外观变化分析。使用傅里叶变换红外光谱(FT-IR)和差示扫描量热法(DSC)对磷脂和水飞蓟素之间的混合物进行表征,结果表明可能存在相互作用。对水飞蓟素混合脂质体的稳定配方进行颊部给药评估,观察其对四氯化碳诱导的白化大鼠氧化应激的保肝活性。使用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)等生化参数来测量保护程度。与口服水飞蓟素悬浮液相比,引入的水飞蓟素混合脂质体在腹腔注射四氯化碳时,两种转氨酶水平均显著降低。组织病理学也证实了这种改善。