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载榄香烯口服类脂纳米囊改善链脲佐菌素诱导的 Wistar 大鼠糖尿病。

Embelin-loaded oral niosomes ameliorate streptozotocin-induced diabetes in Wistar rats.

机构信息

Plant Biotechnology Laboratory, Department of Pharmacognosy & Phytochemistry, School of Pharmaceutical Education and Research, Jamia Hamdard, M.B. Road, New Delhi, 110062, India.

Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh, 11451, Saudi Arabia.

出版信息

Biomed Pharmacother. 2018 Jan;97:1514-1520. doi: 10.1016/j.biopha.2017.11.073. Epub 2017 Nov 20.

DOI:10.1016/j.biopha.2017.11.073
PMID:29793314
Abstract

Embelin is a natural compound possessing a plethora of pharmacological activities, including antidiabetic activity. When formulated as niosomes, embelin offers additional advantages of nanoformulations and can be further exploited for clinical use. An oral niosome formulation of embelin was developed using a thin-film hydration technique, and its antidiabetic activity was studied. The formulation was characterized in terms of entrapment efficiency, vesicle size and morphology, in vitro release profile, and stability. Antidiabetic evaluation was performed in streptozotocin (STZ)-induced diabetic Wistar rats. An antioxidant assay was carried out by evaluating superoxide dismutase (SOD), catalase (CAT), thiobarbituric acid reactive substances (TBARS), and glutathione (GSH). The optimized formulation showed a significant hypoglycemic effect, which was comparable with that of repaglinide. Moreover, significant increases in SOD, CAT, and GSH, along with a decrease in the lipid peroxidation level, were observed, which confirmed the antioxidant efficacy of the formulation. Thus, it is evident that the embelin-loaded niosome formulation was efficacious in diabetes management in Wistar rats.

摘要

榄香醇是一种具有多种药理活性的天然化合物,包括抗糖尿病活性。当被制成非离子囊泡时,榄香醇具有纳米制剂的额外优势,可以进一步开发用于临床应用。本文采用薄膜水化技术开发了榄香醇的口服非离子囊泡制剂,并研究了其抗糖尿病活性。该制剂的包封效率、囊泡大小和形态、体外释放特性和稳定性进行了表征。通过评估超氧化物歧化酶 (SOD)、过氧化氢酶 (CAT)、硫代巴比妥酸反应物质 (TBARS) 和谷胱甘肽 (GSH),在链脲佐菌素 (STZ) 诱导的糖尿病 Wistar 大鼠中进行了抗糖尿病评价。优化后的制剂表现出显著的降血糖作用,与瑞格列奈相当。此外,还观察到 SOD、CAT 和 GSH 的显著增加,以及脂质过氧化水平的降低,这证实了该制剂的抗氧化功效。因此,榄香醇载非离子囊泡制剂在 Wistar 大鼠的糖尿病管理中是有效的。

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