Hepatoprotective effects of a self-micro emulsifying drug delivery system containing Silybum marianum native seed oil against experimentally induced liver injury.

P. Fehér, Z. Ujhelyi, M. Vecsernyés, F. Fenyvesi, G. Damache, A. Ardelean, M. Costache, A. Dinischiotu, A. Hermenean, I. Bácskay
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引用次数: 10

Abstract

The main purpose of this study was to certify the effect of native silymarin oil (SM-oil) formulated in a self-microemulsifying drug delivery system (SMEDDS). The optimal formulation was 25% of SM-oil, 33.3 % of Cremophor RH40, 20% of Transcutol HP, 16.6% of Labrasol and 5% of Capryol 90. In this novel formulation the SM-oil was the active substance and the lipid part. The in vivo study examined the preventive effects of SMEDDS containing SM native seeds oil against carbon tetrachloride (CC14) induced hepatotoxicity in mice. Determination of alanine aminotransferase (ALT), aspartate aminotransferase (AST) levels and also liver histology investigations have been done. The liver antioxidant status was determined with the concentrations of superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GPX), glutathione reductase (GR), and glutathione (GSH) hepatic lipid peroxidation was examined and expressed in terms of malondialdehyde (MDA) content. The plasma levels of AST and ALT significantly diminished by pre-treatment with 500 mg/kg and 1000 mg/kg SMEDDS. The pre-treatment with 500 mg/kg and 1000 mg/kg SMEDDS increased GSH level by about 6% respectively 24% compared to the CC14 group. Due to preventive administration of 500 mg/kg and 1000 mg/kg of SMEDDS in the intoxicated animals, MDA levels were reduced by 22% respectively 58%. Also, an insignificant rise by almost 17% and 19% in the animals treated with the both doses of SMEDDS could be noticed. It can be concluded that hepatotoxicity may be avoided by the oral application of our formulation.
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含水飞蓟籽油的自微乳化给药系统对实验性肝损伤的保护作用。
本研究的主要目的是验证天然水飞蓟素油(SM-oil)在自微乳化给药系统(SMEDDS)中的作用。最佳配方为SM-oil 25%、cremoophor RH40 33.3%、Transcutol HP 20%、Labrasol 16.6%、Capryol 90 5%。在这个新配方中,sm -油是活性物质和脂质部分。体内实验研究了含SM乡土种子油的SMEDDS对四氯化碳(CC14)诱导的小鼠肝毒性的预防作用。测定丙氨酸转氨酶(ALT)、天冬氨酸转氨酶(AST)水平,并进行肝脏组织学检查。以超氧化物歧化酶(SOD)、过氧化氢酶(CAT)、谷胱甘肽过氧化物酶(GPX)、谷胱甘肽还原酶(GR)和谷胱甘肽(GSH)的浓度测定肝脏抗氧化状态,以丙二醛(MDA)含量测定肝脂质过氧化水平。500 mg/kg和1000 mg/kg SMEDDS预处理组血浆AST和ALT水平显著降低。与CC14组相比,500 mg/kg和1000 mg/kg SMEDDS预处理组GSH水平分别提高了约6%和24%。由于预防性给药500 mg/kg和1000 mg/kg的SMEDDS, MDA水平分别降低了22%和58%。此外,在接受两种剂量SMEDDS治疗的动物中,几乎可以注意到17%和19%的微不足道的上升。由此可见,口服本制剂可避免肝毒性。
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