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首页> 外文期刊>Biomedicine & pharmacotherapy =: Biomedecine & pharmacotherapie >Silymarin-loaded Eudragit (R) RS100 nanoparticles improved the ability of silymarin to resolve hepatic fibrosis in bile duct ligated rats
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Silymarin-loaded Eudragit (R) RS100 nanoparticles improved the ability of silymarin to resolve hepatic fibrosis in bile duct ligated rats

机译：负载水飞蓟素的Eudragit（R）RS100纳米颗粒改善了水飞蓟素在结扎胆管结扎大鼠中解决肝纤维化的能力

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Some nano-formulations of silymarin (SM), a drug commonly used for liver diseases, were developed to overcome its poor solubility and poor bioavailability; antifibrotic effect of these formulations has not been tested yet. In this study we aimed to formulate and evaluate silymarin-loaded Eudragit(R) RS100 nanoparticles (SMnps) and to test the capability of SMnps to reverse an established fibrosis model. SMnps were prepared by solvent evaporation and nano-precipitation techniques. The influence of drug: polymer ratio, concentration of surfactant in the aqueous phase on particle size, drug entrapment efficiency (EE) % and in vitro drug releases were investigated. For in vivo evaluation, bile duct ligated (BDL)-rats were treated with either SM or SMnps every other day (125 mg/kg) orally for 3 weeks started 3 weeks after BDL. Liver function tests, oxidative stress and fibrosis/fibrogenesis process were evaluated using biochemical and histopathological techniques. The formulation No (F4) of SMnps showed an average particle size of 632.28 +/- 12.15 nm, a drug EE% of 89.47 +/- 1.65% and released the drug in a prolonged manner over 24 h. The prepared SMnps were nearly spherical with smooth surfaces. In BDL-rats, treatments with either SM or SMnps corrected liver function and oxidative stress. Only SMnps was able to reverse the induced fibrosis; SMnps significantly decreased serum tumor necrosis factor-alpha (TNF-alpha), serum transforming growth factor-beta 1 (TGF-beta 1), hepatic hydroxyproline and downregulated the hepatic expression of tissue inhibitor metalloproteinase-1 (TIMP-1) and cytokeratin-19 (CK-19), whilst increased hepatic hepatocytes growth factor (HGF) and upregulated the hepatic expression of matrix metalloproteinase-2 (MMP-2) and increased MMP-2/TIMP-1 ratio at mRNA level. Livers of rats treated with SMnps showed very little collagen in ECM and restored hepatic architecture as compared to either BDL rats or rats treated with SM.
机译：开发了一些常用于肝脏疾病的药物水飞蓟素（SM）的纳米配方，以克服其不良的溶解性和不良的生物利用度。这些制剂的抗纤维化作用尚未测试。在这项研究中，我们旨在配制和评估水飞蓟素负载的Eudragit RS100纳米粒子（SMnps），并测试SMnps逆转已建立的纤维化模型的能力。通过溶剂蒸发和纳米沉淀技术制备SMnps。研究了药物：聚合物比率，表面活性剂在水相中的浓度对粒径，药物截留效率（EE）％和体外药物释放的影响。为了进行体内评估，从BDL后3周开始，每隔一天（125 mg / kg）用SM或SMnps口服胆管结扎（BDL）大鼠，持续3周。使用生化和组织病理学技术评估肝功能测试，氧化应激和纤维化/纤维化过程。 SMnps的配方No（F4）显示平均粒径为632.28 +/- 12.15 nm，药物EE％为89.47 +/- 1.65％，并在24小时内长时间释放。制备的SMnps几乎为球形，表面光滑。在BDL大鼠中，用SM或SMnps进行治疗可纠正肝功能和氧化应激。只有SMnps能够逆转诱导的纤维化。 SMnps显着降低血清肿瘤坏死因子-α（TNF-alpha），血清转化生长因子-β1（TGF-β1），肝羟脯氨酸，并下调组织抑制剂金属蛋白酶-1（TIMP-1）和细胞角蛋白- 19（CK-19），同时增加肝肝细胞生长因子（HGF）并上调基质金属蛋白酶2（MMP-2）的肝表达，并增加mRNA水平的MMP-2 / TIMP-1比率。与BDL大鼠或SM治疗的大鼠相比，SMnps治疗的大鼠肝脏的ECM中胶原蛋白很少，并且肝结构得以恢复。

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