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Article
2021
Increasing post-digestive solubility of curcumin is the most successful strategy to improve its oral bioavailability: A randomized cross-over trial in healthy adults and in vitro bioaccessibility experiments
Increasing post-digestive solubility of curcumin is the most successful strategy to improve its oral bioavailability: A randomized cross-over trial in healthy adults and in vitro bioaccessibility experiments
Abstract (English)
Scope:
Different mechanistic approaches to improve the low oral bioavailability of curcumin have been developed, but not yet directly compared in humans.
Methods and Results:
In a randomized, double-blind, cross-over trial with 12 healthy adults, the 24 h pharmacokinetics of a single dose of 207 mg curcumin is compared from the following formulations: native, liposomes, with turmeric oils, with adjuvants (including piperine), submicron-particles, phytosomes, γ-cyclodextrin complexes, and micelles. No free, but only conjugated curcumin is detected in all subjects. Compared to native curcumin, a significant increase in the area under the plasma concentration–time curve is observed for micellar curcumin (57-fold) and the curcumin-γ-cyclodextrin complex (30-fold) only. In vitro digestive stability, solubility, and micellization efficiency of micellar curcumin (100%, 80%, and 55%) and curcumin-γ-cyclodextrin complex (73%, 33%, and 23%) are higher compared to all other formulations (<72%, <8%, and <4%). The transport efficiencies through Caco-2 cell monolayers of curcumin from the digested mixed-micellar fractions did not differ significantly.
Conclusion:
The improved oral bioavailability of micellar curcumin, and to a lesser extent of γ-cyclodextrin curcumin complexes, appears to be facilitated by increased post-digestive stability and solubility, whereas strategies targeting post-absorptive processes, including inhibition of biotransformation, appear ineffective.
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Molecular nutrition and food research, 65 (2021), 24, 2100613.
https://doi.org/10.1002/mnfr.202100613.
ISSN: 1613-4133
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English
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610 Medicine and health
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Sustainable Development Goals
BibTeX
@article{Flory2021,
url = {https://hohpublica.uni-hohenheim.de/handle/123456789/16840},
doi = {10.1002/mnfr.202100613},
author = {Flory, Sandra and Sus, Nadine and Haas, Kathrin et al.},
title = {Increasing Post‐Digestive Solubility of Curcumin Is the Most Successful Strategy to Improve its Oral Bioavailability: A Randomized Cross‐Over Trial in Healthy Adults and In Vitro Bioaccessibility Experiments},
journal = {Molecular nutrition and food research},
year = {2021},
}