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载有替米沙坦胆盐的囊泡的开发和生物学评价用于治疗糖尿病肾病。

Development and biological evaluation of vesicles containing bile salt of telmisartan for the treatment of diabetic nephropathy.

机构信息

a Department of Pharmaceutics, College of Pharmacy , King Saud University , Riyadh , Saudi Arabia.

b Department of Clinical Pharmacy, College of Pharmacy , King Saud University , Riyadh , Saudi Arabia.

出版信息

Artif Cells Nanomed Biotechnol. 2018;46(sup1):532-539. doi: 10.1080/21691401.2018.1430700. Epub 2018 Jan 26.

Abstract

The aim of present study was to develop and evaluate vesicles containing bile salt formulation of telmisartan for the treatment of diabetic nephropathy. Different vesicles containing bile salt formulations were developed by varying ratios of soybean phosphatidylcholine and sodium deoxycholate. Prepared formulations were characterized for their size, polydispersity index, zeta potential, morphology and entrapment efficiency. Further, the renoprotective outcome of optimized formulation was studied in streptozotocin-induced diabetic nephropathy rat model. Results of the present study demonstrated that the average vesicles size, polydispersity index, zeta potential and entrapment efficiency were found to be in the range of 64.98 ± 1.40 to 167.60 ± 6.46 nm, 0.02 ± 0.04 to 0.31 ± 0.01, -24.30 ± 1.39 to -42.60 ± 6.67 mV and 29.68 ± 1.08% to 77.21 ± 0.52%, respectively. Further, the best chosen formulation F4 presented vesicles size, polydispersity index, zeta potential and entrapment efficiency of 64.98 ± 1.40 nm, 0.24 ± 0.02, -35.40 ± 1.48 mV and 77.21 ± 0.52%, respectively. In addition, formulation F4 improved the biological indices in streptozotocin-induced diabetic nephropathy in rats. It was concluded that prepared formulation exerts a valuable results on diabetic nephropathy and it may be a potential pharmaceutical dosage form for the treatment of diabetic nephropathy.

摘要

本研究旨在开发并评价含有胆汁盐的替米沙坦囊泡制剂用于治疗糖尿病肾病。通过改变大豆卵磷脂和脱氧胆酸钠的比例来制备不同的含胆汁盐囊泡制剂。对所制备的制剂进行粒径、多分散指数、Zeta 电位、形态和包封效率的表征。进一步,在链脲佐菌素诱导的糖尿病肾病大鼠模型中研究了优化制剂的肾保护作用。研究结果表明,囊泡的平均粒径、多分散指数、Zeta 电位和包封效率分别为 64.98±1.40 至 167.60±6.46nm、0.02±0.04 至 0.31±0.01、-24.30±1.39 至-42.60±6.67mV 和 29.68±1.08%至 77.21±0.52%。此外,最佳选择的 F4 制剂具有 64.98±1.40nm 的粒径、0.24±0.02 的多分散指数、-35.40±1.48mV 的 Zeta 电位和 77.21±0.52%的包封效率。此外,F4 制剂改善了链脲佐菌素诱导的糖尿病肾病大鼠的生物学指标。研究结论认为,所制备的制剂对糖尿病肾病具有重要的治疗效果,可能成为治疗糖尿病肾病的一种有潜力的药物剂型。

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