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一种内源性初级未代谢胆汁酸的第二代微/纳米胶囊,由Eudragit-海藻酸盐复合物与抗氧化化合物稳定。

A second-generation micro/nano capsules of an endogenous primary un-metabolised bile acid, stabilized by Eudragit-alginate complex with antioxidant compounds.

作者信息

Mooranian Armin, Zamani Nassim, Mikov Momir, Goločorbin-Kon Svetlana, Stojanovic Goran, Arfuso Frank, Kovacevic Bozica, Al-Salami Hani

机构信息

Biotechnology and Drug Development Research Laboratory, School of Pharmacy and Biomedical Sciences, Curtin Health Innovation Research Institute, Curtin University, Perth, Western Australia, Australia.

Department of Pharmacology, Toxicology and Clinical Pharmacology, Faculty of Medicine, University of Novi Sad, Novi Sad, Serbia.

出版信息

Saudi Pharm J. 2020 Feb;28(2):165-171. doi: 10.1016/j.jsps.2019.11.017. Epub 2019 Dec 7.

Abstract

Bile acids (BAs) are amphiphilic compounds and of recently have demonstrated wide range of formulation stabilizing effects. A recent study showed that primary un-metabolised bile acids (PUBAs) have β-cell protective effects, and synergistic antidiabetic effects when combined with antioxidant and anti-inflammatory drugs, such as probucol (PB). Thus, this study aimed to design and test microcapsules containing a PUBA incorporated with PB and an alginate-Eudragit matrix. Six types of microcapsules were developed without (control) or with (test) PUBA, and tested for internal and external features and β-cell protective effects. The incorporation of PB-alginate-Eudragit with PUBA produced stable microcapsules but did not exert consistent positive effects on cell viability in the hyperglycaemic state, which suggests that PUBA in alginate-Eudragit matrices did not exhibit synergistic effects with PB nor exerted antidiabetic effects.

摘要

胆汁酸(BAs)是两亲性化合物,最近已证明其具有广泛的制剂稳定作用。最近的一项研究表明,初级未代谢胆汁酸(PUBAs)具有β细胞保护作用,并且与抗氧化剂和抗炎药物(如普罗布考(PB))联合使用时具有协同抗糖尿病作用。因此,本研究旨在设计和测试含有与PB结合的PUBA以及藻酸盐-丙烯酸树脂基质的微胶囊。制备了六种不含(对照)或含有(测试)PUBA的微胶囊,并对其内部和外部特征以及β细胞保护作用进行了测试。PB-藻酸盐-丙烯酸树脂与PUBA的结合产生了稳定的微胶囊,但在高血糖状态下对细胞活力并未产生一致的积极影响,这表明藻酸盐-丙烯酸树脂基质中的PUBA既未与PB表现出协同作用,也未发挥抗糖尿病作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aa32/7000308/87fea0be1e71/gr1.jpg

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