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纳米制剂以提高其作为潜在抗糖尿病药物的生物利用度。 (注:原英文表述不太完整规范,翻译出来的中文也稍显生硬,但根据要求忠实翻译了。完整规范的英文或许应该是“Nanoformulation of [药物名称] to improve its bioavailability as a potential antidiabetic drug.” )

Nanoformulation of to improve its bioavailability as a potential antidiabetic drug.

作者信息

Odei-Addo Frank, Shegokar Ranjita, Müller Rainer H, Levendal R-A, Frost Carminita

机构信息

Department of Biochemistry and Microbiology, Nelson Mandela Metropolitan University, P.O. Box 77000, Port Elizabeth, 6031 South Africa.

Institute of Pharmacy, Department of Pharmaceutics, Biopharmaceutics and NutriCosmetics, Freie Universität Berlin, Kelchstr. 31, 12169 Berlin, Germany.

出版信息

3 Biotech. 2017 Oct;7(5):344. doi: 10.1007/s13205-017-0986-0. Epub 2017 Sep 23.

Abstract

Nanostructured lipid carriers (NLCs) of were successfully produced using high-pressure homogenisation (HPH) on a LAB 40 homogeniser. The particle size was determined for the formulation as well as short-term stability study. The formulation was exposed to Chang liver cells for a glucose uptake study and to INS-1 cells for a chronic insulin release study under normoglycaemic and hyperglycaemic conditions. The particle size of the extract NLC was 220 nm with a PdI of 0.08 after homogenisation at 800 bar. The formulation was stable at the tested temperatures. The extract NLC formulation at 1 µg/ml improved glucose uptake, relative to the control liver cells. Insulin release in INS-1 cells was also elevated under hyperglycaemic conditions when exposed to the NLCs, in comparison with the control untreated cells and the non-formulated extract. The plant extract encapsulated in NLC improved the uptake of glucose and enhanced the insulin sensitivity in vitro, compared to the extract.

摘要

使用LAB 40均质机通过高压均质法成功制备了纳米结构脂质载体(NLCs)。测定了该制剂的粒径并进行了短期稳定性研究。将该制剂暴露于Chang肝细胞进行葡萄糖摄取研究,并在正常血糖和高血糖条件下暴露于INS-1细胞进行慢性胰岛素释放研究。在800巴压力下均质后,提取物NLC的粒径为220纳米,多分散指数(PdI)为0.08。该制剂在测试温度下稳定。相对于对照肝细胞,1μg/ml的提取物NLC制剂改善了葡萄糖摄取。与未处理的对照细胞和未制成制剂的提取物相比,在高血糖条件下,当暴露于NLCs时,INS-1细胞中的胰岛素释放也有所增加。与提取物相比,包裹在NLC中的植物提取物在体外改善了葡萄糖摄取并增强了胰岛素敏感性。

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