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基于可溶性藜科植物蛋白/海藻酸盐复合物的纳米乳剂用于槲皮素的结肠递送。

Nanoemulsions Based on Soluble Chenopodin/Alginate Complex for Colonic Delivery of Quercetin.

作者信息

Intiquilla Arturo, Arazo Migdalia, Gamboa Alexander, Caro Nelson, Gotteland Martin, Palomino-Calderón Alan, Abugoch Lilian, Tapia Cristian

机构信息

Laboratorio de Biología Molecular, Facultad de Farmacia y Bioquímica, Universidad Nacional Mayor de San Marcos, Jirón Puno 1002, Lima 15081, Peru.

Departamento de Ciencia de los Alimentos y Tecnología Química, Facultad de Ciencias Químicas y Farmacéuticas, Universidad de Chile, Santos Dumont 964, Santiago 8330015, Chile.

出版信息

Antioxidants (Basel). 2024 May 27;13(6):658. doi: 10.3390/antiox13060658.

DOI:10.3390/antiox13060658
PMID:38929097
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11200757/
Abstract

Inflammatory bowel disease (IBD) is an autoimmune disorder caused by uncontrolled immune activation and the subsequent destruction of the colon tissue. Quercetin (Qt) is a natural antioxidant and anti-inflammatory agent proposed as an alternative to mitigate IBD. However, its use is limited by its low oral bioavailability. This study aimed to develop nanoemulsions (NEs) based on a soluble chenopodin/alginate (QPA) complex and Tween 80 (T80), intended for the colonic release of Qt, activated by the pH (5.4) and bacteria present in the human colonic microbiota. NEs with different ratios of QPA/Tw80 (F1-F6) were prepared, where F4Qt (60/40) and F5Qt (70/30) showed sizes smaller than 260 nm, PDI < 0.27, and high encapsulation efficiency (>85%). The stability was evaluated under different conditions (time, temperature, pH, and NaCl). The DSC and FTIR analyses indicated hydrophobic and hydrogen bonding interactions between QPA and Qt. F4Qt and F5Qt showed the greater release of Qt in PBS1X and Krebs buffer at pH 5.4 (diseased condition), compared to the release at pH 7.4 (healthy condition) at 8 h of study. In the presence of and , they triggered the more significant release of Qt (ƒ2 < 50) compared to the control (without bacteria). The NEs (without Qt) did not show cytotoxicity in HT-29 cells (cell viability > 80%) and increased the antioxidant capacity of encapsulated Qt. Therefore, these NEs are promising nanocarriers for the delivery of flavonoids to the colon to treat IBD.

摘要

炎症性肠病(IBD)是一种自身免疫性疾病,由不受控制的免疫激活以及随后结肠组织的破坏引起。槲皮素(Qt)是一种天然抗氧化剂和抗炎剂,被提议作为缓解IBD的替代物。然而,其口服生物利用度低限制了其应用。本研究旨在开发基于可溶性藜科植物蛋白/海藻酸盐(QPA)复合物和吐温80(T80)的纳米乳剂(NEs),用于在人结肠微生物群存在的pH(5.4)条件下实现Qt的结肠释放。制备了具有不同QPA/Tw80比例(F1 - F6)的NEs,其中F4Qt(60/40)和F5Qt(70/30)的粒径小于260 nm,多分散指数(PDI)<0.27,且包封效率高(>85%)。在不同条件(时间、温度、pH和NaCl)下评估了稳定性。差示扫描量热法(DSC)和傅里叶变换红外光谱(FTIR)分析表明QPA和Qt之间存在疏水和氢键相互作用。与在pH 7.4(健康状态)下8小时的释放相比,F4Qt和F5Qt在pH 5.4(患病状态)的PBS1X和Krebs缓冲液中显示出更大的Qt释放量。在有[具体细菌名称1]和[具体细菌名称2]存在的情况下,与对照(无细菌)相比,它们引发了更显著的Qt释放(相似因子ƒ2 < 50)。NEs(不含Qt)在HT - 29细胞中未显示细胞毒性(细胞活力>80%),并提高了包封Qt的抗氧化能力。因此,这些NEs是用于将黄酮类化合物递送至结肠以治疗IBD的有前景的纳米载体。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/005d/11200757/7ce19923bcd3/antioxidants-13-00658-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/005d/11200757/5c595aeed1d5/antioxidants-13-00658-g001.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/005d/11200757/29164c802a46/antioxidants-13-00658-g005.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/005d/11200757/1901ca5891fa/antioxidants-13-00658-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/005d/11200757/3a7ddd9c53e4/antioxidants-13-00658-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/005d/11200757/7ce19923bcd3/antioxidants-13-00658-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/005d/11200757/5c595aeed1d5/antioxidants-13-00658-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/005d/11200757/ffed15c45d27/antioxidants-13-00658-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/005d/11200757/4086e05d5bfe/antioxidants-13-00658-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/005d/11200757/5ef03d79d2c0/antioxidants-13-00658-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/005d/11200757/29164c802a46/antioxidants-13-00658-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/005d/11200757/788535d06c98/antioxidants-13-00658-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/005d/11200757/9bb4b0ab5811/antioxidants-13-00658-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/005d/11200757/1901ca5891fa/antioxidants-13-00658-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/005d/11200757/3a7ddd9c53e4/antioxidants-13-00658-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/005d/11200757/7ce19923bcd3/antioxidants-13-00658-g010.jpg

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