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玉米醇溶蛋白纳米颗粒提高了姜黄素在Wistar大鼠体内的口服生物利用度。

Zein Nanoparticles Improve the Oral Bioavailability of Curcumin in Wistar Rats.

作者信息

Brotons-Canto Ana, González-Navarro Carlos J, Gil Ana Gloria, Asin-Prieto Eduardo, Saiz María José, Llabrés Josep Manuel

机构信息

Nucaps Nanotechnology S.L., 31110 Noain, Spain.

Center for Nutrition Research, University of Navarra, 31008 Pamplona, Spain.

出版信息

Pharmaceutics. 2021 Mar 9;13(3):361. doi: 10.3390/pharmaceutics13030361.

DOI:10.3390/pharmaceutics13030361
PMID:33803271
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7998273/
Abstract

Curcumin is a natural compound obtained from turmeric root with high antioxidant and anti-inflammatory activities. However, clinical application of curcumin has been limited due to its low solubility and bioavailability and rapid metabolism and degradation. This study was conducted to evaluate the effect of curcumin incorporation in zein nanoparticles on the pharmacokinetic parameters of systemic curcumin in plasma. Wistar rats were administered a single oral dose of 250 mg/kg of standard curcumin (control) or nanocurcumin (zein-based nanoparticles, Nucaps). The proposed new formulation was also compared with two commercially available curcumin complexes. Blood samples were collected at different times, and plasma levels were determined using HPLC-MS/MS. Overall, nanocurcumin (Nucaps) formulation was well tolerated and showed a 9-fold increase in oral bioavailability when compared to the standard curcumin natural extract. In addition, the nanoparticles prepared in this study demonstrated a bioavailability profile superior to that of other bioavailability-enhanced curcumin complexes currently available in the marketplace. Thus, our nanoparticle-based formulation has shown great potential as a nutraceutical for the oral administration of curcumin.

摘要

姜黄素是一种从姜黄根中提取的天然化合物,具有高抗氧化和抗炎活性。然而,由于姜黄素的低溶解度、低生物利用度以及快速的代谢和降解,其临床应用受到限制。本研究旨在评估姜黄素负载于玉米醇溶蛋白纳米粒中对血浆中系统性姜黄素药代动力学参数的影响。给Wistar大鼠单次口服250mg/kg的标准姜黄素(对照)或纳米姜黄素(基于玉米醇溶蛋白的纳米粒,Nucaps)。所提出的新制剂还与两种市售姜黄素复合物进行了比较。在不同时间采集血样,并使用HPLC-MS/MS测定血浆水平。总体而言,纳米姜黄素(Nucaps)制剂耐受性良好,与标准姜黄素天然提取物相比,口服生物利用度提高了9倍。此外,本研究制备的纳米粒显示出优于目前市场上其他生物利用度增强型姜黄素复合物的生物利用度特征。因此,我们基于纳米粒的制剂作为姜黄素口服给药的营养保健品具有巨大潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2cea/7998273/d09d9f648322/pharmaceutics-13-00361-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2cea/7998273/d09d9f648322/pharmaceutics-13-00361-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2cea/7998273/d09d9f648322/pharmaceutics-13-00361-g001.jpg

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