硝苯地平负载固体脂质纳米颗粒在果糖诱导的糖尿病大鼠体内的制备及降糖作用

Sabarni Sarker, Md. Ashraf Ali, R. Barman, Shuji Noguchi, Y. Iwao, S. Itai, M. I. I. Wahed
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引用次数: 4

摘要

硝苯地平(NI)是一种二氢吡啶钙通道阻滞剂,由于其水溶性差而受到限制。然而,已知负载NI的固体脂质纳米颗粒(NI- sln)具有合适的药代动力学特性和良好的生物相容性。本研究旨在探讨NI-SLN对果糖诱导的糖尿病大鼠葡萄糖稳态、脂质代谢和肝功能的影响。以海藻糖为冻干保护剂,采用高压均质法制备NI-SLN。在饮水中添加10%果糖,连续6周诱导大鼠患上糖尿病。在诱导糖尿病后,将大鼠分为四组,分别口服NI、NI- sln和/或载药,观察其对血糖水平、口服糖耐量试验(OGTT)、血脂、生化指标、电解质和组织病理学的影响。NI-SLN单次给药和给药对果糖诱导的糖尿病大鼠有明显的降血糖作用。虽然NI和NI- sln没有改变正常大鼠的空腹血糖水平,但NI- sln治疗的糖尿病大鼠血糖水平在24小时内显著降低。在OGTT中,NI-SLN在正常和糖尿病大鼠中均表现出显著的降糖活性。因此,NI- sln对糖尿病大鼠的降血糖作用优于纯NI。各治疗组大鼠存活率均为100%。与NI单独治疗相比,NI- sln治疗可显著改善血脂谱,且效果呈剂量依赖性。服用NI-SLN可显著降低尿酸、肌酐水平,维持良好的阳离子平衡。NI-SLN治疗两周后,肝细胞恢复正常结构,其有益作用可能与SGOT和总胆红素水平的降低有关。因此,NI-SLN被发现对提高生物利用度有用,并在大鼠中表现出深刻的抗糖尿病活性。本研究结果表明,NI- sln对血糖水平、血脂和器官保护的改善作用优于纯NI,可能对糖尿病患者的治疗有一定的有益作用。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Preparation and Antidiabetic Effect of Orally Administered Nifedipine‐Loaded Solid Lipid Nanoparticles in Fructose-Induced Diabetic Rats
The use of Nifedipine (NI), a dihydropyridine calcium channel blocker, is limited due to its poor aqueous solubility. However, NI loaded solid-lipid nanoparticles (NI-SLN) are known to exhibit suitable pharmacokinetic properties and good biocompatibility. The present investigation was designed to evaluate the effects of NI-SLN on glucose homeostasis, lipid metabolism and liver function in fructose-induced diabetic rats. NI-SLN was prepared by high pressure homogenization technique followed by lyophilization with trehalose as cryoprotectant. Diabetes was induced into rats by the administration of fructose (10%) in drinking water for six weeks. After induction of diabetes, rats were divided into four groups for the oral ingestion of NI, NI-SLN and/or vehicles and their effects on blood glucose levels, oral glucose tolerance test (OGTT), lipid profile, biochemical parameters, electrolytes and histopathology were observed. Single dose administration and treatment with NI-SLN showed significant glucose lowering efficacy in fructose-induced diabetic rats. Although NI and NI-SLN did not alter the fasting blood glucose level in normal rats, diabetic rats treated with NI-SLN resulted in significant reduction in glucose level for 24 hr. In OGTT, NI-SLN exhibited significant antihyperglycemic activity in both normal and diabetic rats. So, NI-SLN has better glucose lowering efficacy than that of pure NI in diabetic rats. The survival rates in rats among the treatment groups were 100%. Treatment with NI-SLN significantly improved lipid profiles than NI alone and the effect was dose-dependent. Administration of NI-SLN significantly reduced uric acid, creatinine levels and maintained a good cationic balance. After two weeks of NI-SLN treatment, hepatocytes regained their normal architecture, and the beneficial effect could be correlated with the reduction of SGOT and total bilirubin levels. Therefore, NI-SLN was found to be useful for the enhancement of bioavailability and exhibited profound antidiabetic activity in rats. The results of the study suggested that NI-SLN exerted better improvement in glucose levels, lipid profiles and organ protection than pure NI and might have some beneficial effects in the management of diabetic patients.
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