Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia.
Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia.
Eur J Pharm Sci. 2018 Jan 1;111:409-417. doi: 10.1016/j.ejps.2017.10.012. Epub 2017 Oct 10.
The objective of the present study was to formulate eprosartan mesylate loaded nano-bilosomes and investigates its potential for controlling streptozotocin induced diabetes nephropathy in Wistar rats. The eprosartan mesylate loaded nano-bilosomes comprising of various ratios of soybean phosphatidylcholine/sodium deoxycholate were prepared by thin film hydration technique. The prepared formulations were evaluated for vesicles size, polydispersity index, zeta potential and entrapment efficiency. Further the optimized formulation was characterized for vesicles morphology, and its efficacy for the management of diabetic nephropathy in Wistar rats. The optimized eprosartan mesylate loaded nano-bilosomes exhibited vesicles size, polydispersity index, zeta potential and entrapment efficiency of 63.88±3.46nm, 0.172±0.026, -30.40±2.75mV and 61.19±0.88% respectively. In vivo activity demonstrated that the prepared eprosartan mesylate loaded nano-bilosomes formulation demonstrated a nephro-protecting outcome as shown by the substantial decrease in serum creatinine, urea, lactate dehydrogenase, total albumin, and malondialdehyde. Additionally, an oral administration of eprosartan mesylate loaded nano-bilosomes decreases the raised expressions of Angiotensin II type 1 receptor, inducible nitric oxide synthase, and transforming growth factor-β1 in Wistar rats. Further, histopathological examination established the nephro-protective effect of prepared formulation. In conclusion, the research work in the paper suggests that the prepared eprosartan mesylate loaded nano-bilosomes could serve as a practical oral formulation for diabetic nephropathy in future therapy and may offer potential benefits in cases with hypertension and renal disease.
本研究的目的是制备甲磺酸依普罗沙坦负载的纳米双层囊泡,并研究其在控制链脲佐菌素诱导的 Wistar 大鼠糖尿病肾病中的潜力。采用薄膜水化法制备了不同比例大豆卵磷脂/脱氧胆酸钠的甲磺酸依普罗沙坦负载纳米双层囊泡。对制备的制剂进行了粒径、多分散指数、Zeta 电位和包封效率的评价。进一步对优化的制剂进行了囊泡形态学的表征,并考察了其对 Wistar 大鼠糖尿病肾病的治疗效果。优化的甲磺酸依普罗沙坦负载纳米双层囊泡的粒径、多分散指数、Zeta 电位和包封效率分别为 63.88±3.46nm、0.172±0.026、-30.40±2.75mV 和 61.19±0.88%。体内活性研究表明,所制备的甲磺酸依普罗沙坦负载纳米双层囊泡制剂表现出肾保护作用,表现为血清肌酐、尿素、乳酸脱氢酶、总白蛋白和丙二醛显著降低。此外,甲磺酸依普罗沙坦负载纳米双层囊泡的口服给药可降低 Wistar 大鼠血管紧张素 II 型 1 受体、诱导型一氧化氮合酶和转化生长因子-β1 的表达升高。进一步的组织病理学检查证实了所制备制剂的肾保护作用。总之,本文的研究工作表明,所制备的甲磺酸依普罗沙坦负载纳米双层囊泡可能成为未来治疗糖尿病肾病的一种实用口服制剂,并可能在高血压和肾脏疾病的情况下带来潜在的益处。