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一种新型水飞蓟素作为成年雄性大鼠潜在抗糖尿病药物的制备与表征

Preparation and characterisation of a new form of silymarin as a potential antidiabetic agent in the adult male rat.

作者信息

Golestaneh Elnaz, Aslani Abolfazl, Aghaei Mahmoud, Hashemnia Mohammad, Aarabi Mohammad Hosein

机构信息

Department of Clinical Biochemistry, School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, Iran.

Department of Pharmaceutics, School of Pharmacy and Novel Drug Delivery Systems Research Center, Isfahan University of Medical Sciences, Isfahan, Iran.

出版信息

Arch Physiol Biochem. 2023 Jun;129(3):799-809. doi: 10.1080/13813455.2021.1874018. Epub 2021 Feb 2.

Abstract

Silymarin is used for a wide variety of biological applications including, antidiabetic activities. However, the effectiveness of Silymarin is affected by its poor aqueous solubility and low systemic bioavailability after oral administration. The present study aimed to formulate a new, simple, and inexpensive form of silymarin solution. A new form of silymarin solution (NFSM) characterised by small particle size (227.5 nm), high entrapment efficiency (>82%), and appropriate zeta potential(-24.7mv). Moreover, the antidiabetic effects of NESM were evaluated relative to native Silymarin (SM). Oral administration of NFSM for 14 days in diabetic rats significantly decreased fasting blood glucose, oxidative stress levels, and improved lipid profile compared with SM. Also, NFSM significantly increased serum insulin levels, the gene expression of insulin and Pdx1, restored and improved the structure of the liver, and pancreas histologically. Our results concluded that NFSM may be an efficient carrier for oral delivery of silymarin for the management of diabetes and aggravated antioxidant status.

摘要

水飞蓟素可用于多种生物学应用,包括抗糖尿病活性。然而,水飞蓟素的有效性受到其水溶性差和口服后全身生物利用度低的影响。本研究旨在制备一种新型、简单且廉价的水飞蓟素溶液剂型。一种新型水飞蓟素溶液(NFSM),其特点是粒径小(227.5纳米)、包封率高(>82%)且具有合适的ζ电位(-24.7毫伏)。此外,相对于天然水飞蓟素(SM),评估了NFSM的抗糖尿病作用。与SM相比,在糖尿病大鼠中口服NFSM 14天可显著降低空腹血糖、氧化应激水平并改善血脂谱。此外,NFSM显著提高血清胰岛素水平、胰岛素和Pdx1的基因表达,在组织学上恢复并改善肝脏和胰腺的结构。我们的结果表明,NFSM可能是用于口服递送水飞蓟素以治疗糖尿病和改善抗氧化状态的有效载体。

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