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槲皮素/甲基-β-环糊精复合物的表征及抗氧化活性

Characterization and Antioxidant Activity of Quercetin/Methyl-β-Cyclodextrin Complexes.

作者信息

Güleç Kadri, Demirel Müzeyyen

机构信息

Department of Pharmaceutical Technology, Faculty of Pharmacy, Anadolu University, P.O. Box: 26470, Eskişehir, Turkey.

出版信息

Curr Drug Deliv. 2016;13(3):444-51. doi: 10.2174/1567201813666151207112514.

Abstract

Quercetin (Qu), a polyphenolic flavonoid, is one of the most effective plant originated antioxidants. Despite the potential use of Qu in clinical trials, low water solubility, stability problems and the scarcity of cellular bioavailability limit its applications. The purpose of this study was to enhance aqueous solubility, dissolution rate and antioxidant activity of Qu by complexation with Methyl-β- cyclodextrin (M-β-CD). Analyses results showed that the aqueous solubility, dissolution rate and antioxidant activity of the complex were increased 254-fold, ~3-fold and 10% respectively compared to the pure Qu. Complexes were prepared by freeze-drying and evaporation method. The characteristics of the complexes were evaluated by DSC, XRD, (1)H-NMR, FT-IR, SEM, encapsulation efficacy, in-vitro dissolution rate analyses. Antioxidant activity studies on complexes carried out with DPPH tests. Analyses results showed that the formation of the complexes resulted in enhanced solubility with increased its antioxidant activity of Qu.

摘要

槲皮素(Qu)是一种多酚类黄酮,是最有效的植物源抗氧化剂之一。尽管槲皮素在临床试验中有潜在用途,但其低水溶性、稳定性问题以及细胞生物利用度低限制了其应用。本研究的目的是通过与甲基-β-环糊精(M-β-CD)络合来提高槲皮素的水溶性、溶解速率和抗氧化活性。分析结果表明,与纯槲皮素相比,该络合物的水溶性、溶解速率和抗氧化活性分别提高了254倍、约3倍和10%。络合物通过冷冻干燥和蒸发法制备。通过差示扫描量热法(DSC)、X射线衍射法(XRD)、核磁共振氢谱(¹H-NMR)、傅里叶变换红外光谱(FT-IR)、扫描电子显微镜(SEM)、包封率、体外溶解速率分析等对络合物的特性进行了评估。用二苯基苦味酰基自由基(DPPH)试验对络合物进行抗氧化活性研究。分析结果表明,络合物的形成导致槲皮素的溶解度提高,其抗氧化活性增强。

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