PDF(Pubmed)
Abstract：
Silibinin has considerable therapeutic potential for the treatment of diabetes through anti-inflammatory, antioxidant, and immunomodulatory properties. However, the therapeutic application of silibinin is quite limited due to its poor bioavailability. In the present study, an attempt was made to improve the antidiabetic efficacy of silibinin by its encapsulation in liposomal vesicles. The liposomes with a high encapsulation efficiency of silibinin (96%) and a zeta potential of -26.2 ± 0.6 mV were developed and studied using nicotinamide/streptozotocin-induced diabetic rats. Administration of silibinin-loaded liposomes to diabetic rats lowered glucose levels, increased insulin levels, and improved pancreatic islet architecture. The anti-inflammatory effect of silibinin-loaded liposomes was demonstrated by a decrease in serum C-reactive protein (CRP) levels and a reduced deposition of collagen fibers in the islets of diabetic rats. Furthermore, silibinin-loaded liposomes were more efficient in lowering glucose, alanine transaminase, triglyceride, and creatinine levels in diabetic rats than pure silibinin. In addition, silibinin-loaded liposomes had a significantly better effect on beta-cell mass and Glut2 glucose receptor distribution in diabetic islets than pure silibinin. The present results clearly show that liposome encapsulation of silibinin enhances its antidiabetic efficacy, which may contribute to the therapeutic benefit of silibinin in the treatment of diabetes and its complications.
摘要：
水飞蓟宾通过抗炎治疗糖尿病具有相当大的治疗潜力，抗氧化剂，和免疫调节特性。然而,由于水飞蓟宾的生物利用度较差，其治疗应用非常有限。在本研究中,尝试通过将水飞蓟宾包裹在脂质体囊泡中来提高其抗糖尿病功效。开发并使用烟酰胺/链脲佐菌素诱导的糖尿病大鼠研究了具有高水飞蓟宾包封率（96％）和-26.2±0.6mVζ电位的脂质体。给糖尿病大鼠服用载有水飞蓟宾的脂质体降低了葡萄糖水平，胰岛素水平升高，改善胰岛结构。糖尿病大鼠胰岛中血清C反应蛋白（CRP）水平降低和胶原纤维沉积减少，证明了载有水飞蓟宾的脂质体的抗炎作用。此外，负载水飞蓟宾的脂质体更有效地降低葡萄糖，丙氨酸转氨酶，甘油三酯，糖尿病大鼠的肌酐水平比纯水飞蓟宾高。此外,负载水飞蓟宾的脂质体对糖尿病胰岛β细胞质量和Glut2葡萄糖受体分布的影响明显优于纯水飞蓟宾。目前的结果清楚地表明，水飞蓟宾的脂质体封装增强其抗糖尿病功效，这可能有助于水飞蓟宾治疗糖尿病及其并发症的治疗益处。
