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高含量中链甘油三酯乳液载姜黄素的体内吸收增强和生物分布。

Enhanced in vivo absorption and biodistribution of curcumin loaded into emulsions with high medium-chain triglyceride content.

机构信息

Department of Food Technology, University of Lleida - Agrotecnio CERCA Center, Rovira Roure 191, 25198 Lleida, Spain.

Department of Food Technology, University of Lleida - Agrotecnio CERCA Center, Rovira Roure 191, 25198 Lleida, Spain.

出版信息

Food Res Int. 2023 Dec;174(Pt 1):113595. doi: 10.1016/j.foodres.2023.113595. Epub 2023 Oct 14.

DOI:10.1016/j.foodres.2023.113595
PMID:37986458
Abstract

The health benefits of curcumin have been demonstrated by several clinical studies, but its low bioavailability compromises its functionality. In this regard, emulsions have proven to be effective encapsulation systems for curcumin. Nevertheless, emulsions with a high oil content (50%) may offer some advantages due to the large amount of compound they can incorporate. Therefore, the aim of this work was to study the pharmacokinetics and biodistribution of curcumin when carried in optimized emulsions containing 50% MCT oil and a plant-based emulsifier (soybean lecithin) at 2 h or 4 h post-oral administration to rats. The most stable emulsion was obtained using 50% of oil and a surfactant-oil-ratio 0.1, through a microfluidization process. After the oral administration of the systems (150 mg curcumin/kg body weight), curcumin glucuronide was the main compound present in plasma (AUC = 1556.3 ng·h·ml), especially at 2-4 h post-administration. The total curcuminoid bioavailability was increased by 10.6-fold when rats were fed with the curcumin emulsion rather than with a control suspension. Moreover, rats fed with the emulsion showed the highest accumulation of free curcuminoids, which present the highest biological activity, in the liver (129 ng curcumin/g tissue) and brown adipose tissue (193 ng curcumin/g tissue). The obtained results are of great interest since the presence of curcumin in the brown adipose tissue has been shown to play a relevant role in the prevention of obesity and its related metabolic disorders.

摘要

姜黄素的健康益处已被多项临床研究证明,但由于其生物利用度低,限制了其功能。在这方面,乳液已被证明是姜黄素的有效包封系统。然而,高油含量(50%)的乳液可能由于可以包含大量化合物而具有一些优势。因此,本工作旨在研究姜黄素在以优化乳液(含有 50%MCT 油和植物来源乳化剂(大豆卵磷脂))经口给予大鼠 2 或 4 小时后的药代动力学和生物分布。通过微流化过程,使用 50%的油和表面活性剂-油比例为 0.1 可以获得最稳定的乳液。在给予这些系统(150mg 姜黄素/公斤体重)后,姜黄素葡萄糖醛酸苷是血浆中主要存在的化合物(AUC=1556.3ng·h·ml),特别是在给予后 2-4 小时。与对照混悬剂相比,当大鼠用姜黄素乳液喂养时,总姜黄素类生物利用度增加了 10.6 倍。此外,用乳液喂养的大鼠在肝脏(129ng 姜黄素/克组织)和棕色脂肪组织(193ng 姜黄素/克组织)中积累了最高的游离姜黄素类,这些姜黄素类具有最高的生物活性。所得结果非常有趣,因为在棕色脂肪组织中存在姜黄素已被证明在预防肥胖及其相关代谢紊乱方面发挥重要作用。

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