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新型载维格列汀 ZnO 纳米粒的制备及其抗糖尿病活性研究

Fabrication of novel vildagliptin loaded ZnO nanoparticles for anti diabetic activity.

机构信息

Department of Chemistry, School of Science, University of Management and Technology, Lahore, 54770, Pakistan.

Biomedical Engineering Department, College of Engineering and Technologies, Al-Mustaqbal University, Babylon, 51001, Iraq.

出版信息

Sci Rep. 2024 Aug 2;14(1):17893. doi: 10.1038/s41598-024-67420-z.

DOI:10.1038/s41598-024-67420-z
PMID:39095369
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11297240/
Abstract

Diabetes mellitus (DM) is a rapidly prevailing disease throughout the world that poses boundless risk factors linked to several health problems. Vildagliptin is the standard dipeptidyl peptidase-4 (DPP-4) inhibitor type of medication that is used for the treatment of diabetes anti-hyperglycemic agent (anti-diabetic drug). The current study aimed to synthesize vildagliptin-loaded ZnO NPs for enhanced efficacy in terms of increased retention time minimizing side effects and increased hypoglycemic effects. Herein, Zinc Oxide (ZnO) nanoparticles (NPs) were constructed by precipitation method then the drug vildagliptin was loaded and drug loading efficiency was estimated by the HPLC method. X-ray diffraction analysis (XRD), UV-vis spectroscopy, FT-IR, scanning electron microscope (SEM), and EDX analysis were performed for the characterization of synthesized vildagliptin-loaded ZnO NPs. The UV-visible spectrum shows a distinct peak at 363 nm which confirms the creation of ZnO NPs and SEM showed mono-dispersed sphere-shaped NPs. EDX analysis shows the presence of desired elements along with the elemental composition. The physio-sorption studies, which used adsorption isotherms to assess adsorption capabilities, found that the Freundlich isotherm model explains the data very well and fits best. The maximum adsorption efficiency of 58.83% was obtained. Further, In vitro, anti-diabetic activity was evaluated by determining the α-amylase and DPP IV inhibition activity of the product formed. The formulation gave maximum inhibition of 82.06% and 94.73% of α-amylase and DPP IV respectively. While at 1000 µg/ml concentration with IC values of 24.11 μg/per ml and 42.94 μg/ml. The inhibition of α-amylase can be ascribed to the interactive effect of ZnO NPs and vildagliptin.

摘要

糖尿病(DM)是一种在全球范围内迅速流行的疾病,它存在着与许多健康问题相关的无限风险因素。维格列汀是一种标准的二肽基肽酶-4(DPP-4)抑制剂,用于治疗糖尿病抗高血糖药物(抗糖尿病药物)。本研究旨在合成载维格列汀的氧化锌纳米粒子(NPs),以提高疗效,延长滞留时间,减少副作用,提高降血糖作用。在此,通过沉淀法构建氧化锌(ZnO)纳米粒子(NPs),然后负载药物维格列汀,并通过 HPLC 法估算载药量。进行了 X 射线衍射分析(XRD)、紫外-可见光谱、傅里叶变换红外光谱(FT-IR)、扫描电子显微镜(SEM)和能谱分析(EDX)对合成的载维格列汀的 ZnO NPs 进行了表征。紫外-可见光谱在 363nm 处显示出明显的峰,证实了 ZnO NPs 的形成,SEM 显示出单分散的球形 NPs。EDX 分析表明存在所需的元素以及元素组成。使用吸附等温线评估吸附能力的物理吸附研究发现,Freundlich 等温线模型很好地解释了数据,并且拟合得最好。最大吸附效率为 58.83%。此外,通过测定形成的产物对α-淀粉酶和 DPP IV 的抑制活性,对其体外抗糖尿病活性进行了评价。该配方对α-淀粉酶和 DPP IV 的最大抑制率分别为 82.06%和 94.73%。而在 1000µg/ml 浓度下,IC 值分别为 24.11µg/ml 和 42.94µg/ml。α-淀粉酶的抑制作用可以归因于 ZnO NPs 和维格列汀的相互作用。

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