A pharmacokinetic study and critical reappraisal of curcumin formulations enhancing bioavailability

IF 4.6 2区综合性期刊 Q1 MULTIDISCIPLINARY SCIENCES

iScience Pub Date : 2025-05-03 DOI:10.1016/j.isci.2025.112575

Maurice A.G.M. Kroon , Hanneke W.M. van Laarhoven , Eleonora L. Swart , Olaf van Tellingen , E. Marleen Kemper

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Abstract

This independent crossover study assessed curcumin bioavailability and excretion in nine healthy males receiving three formulations (AOV, Longvida, and NovaSOL) at about 570 mg, while AOV was also tested at 2280 mg, with and without piperine. Plasma levels of unconjugated curcumin remained below 2 nM in most cases, including high-dose AOV and piperine combinations. NovaSOL achieved the highest levels (6.7–38 nM at 30 min), but these rapidly declined and were still 100-fold lower than concentrations used in vitro to show biological effects. Curcumin conjugates exceeded 10 nM with all formulations, particularly NovaSOL, which showed 100-fold higher levels. Fecal recovery mainly included unconjugated curcuminoids and was high, except for NovaSOL, suggesting better intestinal absorption. However, even when using a formulation with enhanced uptake, plasma levels of unconjugated curcumin remained minimal. Piperine addition provided no benefit. The findings underscore that bioavailability claims should be based on unconjugated curcumin and not on its poorly membrane permeable conjugates.

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提高生物利用度的姜黄素制剂的药代动力学研究和关键的再评价

这项独立的交叉研究评估了9名健康男性在接受三种配方（AOV， Longvida和NovaSOL）约570毫克时姜黄素的生物利用度和排泄，而AOV也在2280毫克时进行了测试，含和不含胡椒碱。在大多数情况下，包括高剂量AOV和胡椒碱联合用药，非共轭姜黄素的血浆水平保持在2 nM以下。NovaSOL达到了最高水平（6.7-38 nM， 30分钟），但这些水平迅速下降，仍然比体外使用的浓度低100倍，以显示生物效应。所有配方的姜黄素结合物均超过10 nM，特别是NovaSOL，其结合物含量高出100倍。除NovaSOL外，粪便中未结合的姜黄素回收率较高，表明肠道吸收较好。然而，即使使用增强摄取的制剂，血浆中未结合的姜黄素水平仍然很低。添加胡椒碱没有任何好处。研究结果强调，生物利用度声明应基于未偶联的姜黄素，而不是其膜渗透性差的偶联物。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

iScience Multidisciplinary-Multidisciplinary

CiteScore

7.20

自引率

1.70%

发文量

1972

审稿时长

6 weeks

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