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胆酸钠包被的油橄榄多酚纳米脂质体:制备、稳定性、释放及生物活性

Sodium cholate-coated Olea europaea polyphenol nanoliposomes: Preparation, stability, release, and bioactivity.

作者信息

Li Wenjun, Antoniadi Lemonia, Zhou Hao, Chen Hongxia, Angelis Apostolis, Halabalaki Maria, Skaltsounis Leandros A, Qi Zhiwen, Wang Chengzhang

机构信息

Institute of Chemical Industry of Forest Products, CAF, National Engineering Laboratory for Biomass Chemical Utilization, Key and Open Laboratory on Forest Chemical Engineering, SFA, Key Laboratory of Biomass Energy and Material, Nanjing 210042, Jiangsu Province, China.

Division of Pharmacognosy and Natural Products Chemistry, National and Kapodistrian University of Athens, Panepistimioupoli Zografou, NKUA, 15771, Athens, Greece; Pharmagnose S.A., 57th km Athens-lamia National Road, Oinofyta 32011, Greece.

出版信息

Food Chem. 2025 Mar 30;469:142580. doi: 10.1016/j.foodchem.2024.142580. Epub 2024 Dec 19.

Abstract

Ultra-flexible nanoliposomes (UNL) coated with sodium cholate were fabricated using the thin film hydration technique to encapsulate oleocanthal (OLEO), oleacein (OLEA), oleuropein (OLEU), and hydroxytyrosol (HT) for improving their stability and bioactivity. Their physicochemical properties were further validated through DLS, FTIR, XRD, TGA, and DSC analyses. Negative-staining TEM imaging revealed well-dispersed UNL with laminar vesicles inside. Additionally, their transdermal studies in vitro demonstrated that UNL enhanced the cumulative release of OLEO, OLEA, OLEU, and HT by 3.13, 2.76, 2.59, and 2.83 times, respectively. Furthermore, their release mechanisms were better approximated the Peppas-Sahlin model rather than the Korsmeyer-Peppas and Higuchi models, which governed by Fickian diffusion. Moreover, comparing to their compounds, UNL structure exhibited improved their antioxidant and cytotoxicity properties, highlighting their potential as effective delivery agents in humans. These results offer a novel approach for stabilizing biologically active polyphenols from Olea europaea, paving the way for enhanced human health applications.

摘要

采用薄膜水化技术制备了胆酸钠包被的超柔性纳米脂质体(UNL),以包封油橄榄苦素(OLEO)、油橄榄素(OLEA)、橄榄苦苷(OLEU)和羟基酪醇(HT),以提高它们的稳定性和生物活性。通过动态光散射(DLS)、傅里叶变换红外光谱(FTIR)、X射线衍射(XRD)、热重分析(TGA)和差示扫描量热法(DSC)分析进一步验证了它们的物理化学性质。负染色透射电子显微镜(TEM)成像显示UNL分散良好,内部有层状囊泡。此外,它们的体外透皮研究表明,UNL分别将OLEO、OLEA、OLEU和HT的累积释放提高了3.13、2.76、2.59和2.83倍。此外,它们的释放机制更符合Peppas-Sahlin模型,而不是由菲克扩散控制的Korsmeyer-Peppas模型和Higuchi模型。此外,与它们的化合物相比,UNL结构表现出更好的抗氧化和细胞毒性特性,突出了它们作为人类有效递送剂的潜力。这些结果为稳定油橄榄中的生物活性多酚提供了一种新方法,为增强人类健康应用铺平了道路。

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