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纳米植物鞘磷脂体增强槲皮素在链脲佐菌素诱导的糖尿病大鼠口服给药治疗糖尿病中的疗效。

Nanophytosomes for enhancement of rutin efficacy in oral administration for diabetes treatment in streptozotocin-induced diabetic rats.

机构信息

Department of Food Science and Technology, Faculty of Agriculture, Urmia University, Urmia, P.O. Box 57561-51818, Iran.

Pharmaceutical Analysis Research Center, Student Research Committee, and Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran.

出版信息

Int J Pharm. 2021 Dec 15;610:121208. doi: 10.1016/j.ijpharm.2021.121208. Epub 2021 Oct 18.

Abstract

Rutin is a natural antioxidant compound with several therapeutic benefits. However, the application of this bioactive compound is limited due to its low stability and bioavailability. To overcome these limitations, this study aimed to encapsulate rutin into nanophytosomes (NPs) and evaluate the therapeutic potency of this nanocarrier in streptozotocin (STZ)-induced diabetic rats. The particle size, zeta potential, and encapsulation efficiency of the prepared NPs were 72.72 nm, -22 mV, and 93.7%, respectively. The in vivo study showed that the oral administration of rutin-loaded NPs (containing 25 mg rutin/kg per day) for 4 weeks was more effective than free rutin in the control of hyperglycemia and hyperlipidemia in the STZ-induced diabetic rats. Additionally, the administration of rutin-loaded NPs regulated the activities of liver marker enzymes and the levels of total hemoglobin and glycated hemoglobin in the diabetic rats. The antioxidant defenses in the diabetic rats were increased by the administration of rutin-loaded NPs more than free rutin. Moreover, the histopathological study showed that the administration of rutin-loaded NPs restored the diabetes-induced damages in kidney, liver, and pancreas. In conclusion, encapsulation of rutin with phytosomes is an effective technique to benefit from its therapeutic potential, especially to attenuate diabetic complications.

摘要

芦丁是一种具有多种治疗益处的天然抗氧化化合物。然而,由于其低稳定性和生物利用度,该生物活性化合物的应用受到限制。为了克服这些限制,本研究旨在将芦丁包封到纳米植物鞘磷脂(NPs)中,并评估这种纳米载体在链脲佐菌素(STZ)诱导的糖尿病大鼠中的治疗效果。所制备的 NPs 的粒径、Zeta 电位和包封效率分别为 72.72nm、-22mV 和 93.7%。体内研究表明,口服芦丁负载 NPs(每天含 25mg 芦丁/千克)4 周对 STZ 诱导的糖尿病大鼠的高血糖和高血脂的控制效果优于游离芦丁。此外,芦丁负载 NPs 的给药调节了糖尿病大鼠中肝脏标记酶的活性以及总血红蛋白和糖化血红蛋白的水平。与游离芦丁相比,芦丁负载 NPs 的给药增加了糖尿病大鼠的抗氧化防御能力。此外,组织病理学研究表明,芦丁负载 NPs 的给药恢复了肾脏、肝脏和胰腺的糖尿病诱导损伤。总之,用植物鞘磷脂包封芦丁是一种从其治疗潜力中获益的有效技术,特别是可以减轻糖尿病并发症。

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