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The enhanced bioavailability of free curcumin and bioactive-metabolite tetrahydrocurcumin from a dispersible, oleoresin-based turmeric formulation

BACKGROUND: Curcuminoids have been widely studied for human health and disease applications, yet bioavailability remains a hurdle to actualizing all the benefits ascribed to them. The lack of standardization in analysis method, confusion about what constitutes an ideal analyte, and conflicting thoug...

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Autores principales: Panda, Sanjib Kumar, Nirvanashetty, Somashekara, Missamma, M., Jackson-Michel, Shavon
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Lippincott Williams & Wilkins 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8270635/
https://www.ncbi.nlm.nih.gov/pubmed/34232211
http://dx.doi.org/10.1097/MD.0000000000026601
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author Panda, Sanjib Kumar
Nirvanashetty, Somashekara
Missamma, M.
Jackson-Michel, Shavon
author_facet Panda, Sanjib Kumar
Nirvanashetty, Somashekara
Missamma, M.
Jackson-Michel, Shavon
author_sort Panda, Sanjib Kumar
collection PubMed
description BACKGROUND: Curcuminoids have been widely studied for human health and disease applications, yet bioavailability remains a hurdle to actualizing all the benefits ascribed to them. The lack of standardization in analysis method, confusion about what constitutes an ideal analyte, and conflicting thoughts around dosing strategies have made it difficult to draw parity between bioavailability and bioactivity and establish a baseline for formulation comparisons. METHODS: This randomized double-blinded, 2-way cross over, single oral dose, comparative bioavailability study differentially evaluates curcumin at the time of its absorption and along various biotransformation pathways, to include free curcumin, the readily usable form of curcumin; individual and composite totals of curcumin and its analogues as exogenously cleaved conjugates, for example, total curcumin, total demethoxycurcumin (DMC), total bisdemethoxycurcumin (BDMC), and total curcuminoids respectively; and the bioactive metabolite of curcumin, total tetrahydrocurcumin (THC). As a primary study objective, the relative bioavailability of CURCUGEN, a novel dispersible, 50% curcuminoids-concentrated turmeric extract was compared to the standard curcumin reference product, curcuminoids 95% standardized extract (C-95), using the maximum concentration (C(max)), and area under the curve (AUC(0-t)) of free curcumin, total curcumin, total DMC, total BDMC and the curcumin active metabolite, as total THC. RESULTS: The evaluation of free curcumin demonstrated that the C(max) and AUC(0-t) of the CURCUGEN was 16.1 times and 39 times higher than the C(max) and AUC(0-t) of C-95. Furthermore, total curcumin, total DMC, total BDMC, and total curcuminoids resulted in AUC(0-t) of the CURCUGEN at 49.5-, 43.5-, 46.8-, and 52.5-fold higher than C-95, respectively. The relative bioavailability of CURCUGEN for total THC was found to be 31 times higher when compared to C-95. CONCLUSION: As the first human pharmacokinetics study to apply best-practice recommendations and pharmaceutically-aligned guidance in the comprehensive evaluation of a novel curcuminoids formulation, we have established the novelty of said formulation while better standardizing for the common variances and discrepancies between curcuminoids and their derivatives in the literature and commercial marketing, alike.
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spelling pubmed-82706352021-07-12 The enhanced bioavailability of free curcumin and bioactive-metabolite tetrahydrocurcumin from a dispersible, oleoresin-based turmeric formulation Panda, Sanjib Kumar Nirvanashetty, Somashekara Missamma, M. Jackson-Michel, Shavon Medicine (Baltimore) 3800 BACKGROUND: Curcuminoids have been widely studied for human health and disease applications, yet bioavailability remains a hurdle to actualizing all the benefits ascribed to them. The lack of standardization in analysis method, confusion about what constitutes an ideal analyte, and conflicting thoughts around dosing strategies have made it difficult to draw parity between bioavailability and bioactivity and establish a baseline for formulation comparisons. METHODS: This randomized double-blinded, 2-way cross over, single oral dose, comparative bioavailability study differentially evaluates curcumin at the time of its absorption and along various biotransformation pathways, to include free curcumin, the readily usable form of curcumin; individual and composite totals of curcumin and its analogues as exogenously cleaved conjugates, for example, total curcumin, total demethoxycurcumin (DMC), total bisdemethoxycurcumin (BDMC), and total curcuminoids respectively; and the bioactive metabolite of curcumin, total tetrahydrocurcumin (THC). As a primary study objective, the relative bioavailability of CURCUGEN, a novel dispersible, 50% curcuminoids-concentrated turmeric extract was compared to the standard curcumin reference product, curcuminoids 95% standardized extract (C-95), using the maximum concentration (C(max)), and area under the curve (AUC(0-t)) of free curcumin, total curcumin, total DMC, total BDMC and the curcumin active metabolite, as total THC. RESULTS: The evaluation of free curcumin demonstrated that the C(max) and AUC(0-t) of the CURCUGEN was 16.1 times and 39 times higher than the C(max) and AUC(0-t) of C-95. Furthermore, total curcumin, total DMC, total BDMC, and total curcuminoids resulted in AUC(0-t) of the CURCUGEN at 49.5-, 43.5-, 46.8-, and 52.5-fold higher than C-95, respectively. The relative bioavailability of CURCUGEN for total THC was found to be 31 times higher when compared to C-95. CONCLUSION: As the first human pharmacokinetics study to apply best-practice recommendations and pharmaceutically-aligned guidance in the comprehensive evaluation of a novel curcuminoids formulation, we have established the novelty of said formulation while better standardizing for the common variances and discrepancies between curcuminoids and their derivatives in the literature and commercial marketing, alike. Lippincott Williams & Wilkins 2021-07-09 /pmc/articles/PMC8270635/ /pubmed/34232211 http://dx.doi.org/10.1097/MD.0000000000026601 Text en Copyright © 2021 the Author(s). Published by Wolters Kluwer Health, Inc. https://creativecommons.org/licenses/by-nc/4.0/This is an open access article distributed under the terms of the Creative Commons Attribution-Non Commercial License 4.0 (CCBY-NC), where it is permissible to download, share, remix, transform, and buildup the work provided it is properly cited. The work cannot be used commercially without permission from the journal. http://creativecommons.org/licenses/by-nc/4.0 (https://creativecommons.org/licenses/by-nc/4.0/)
spellingShingle 3800
Panda, Sanjib Kumar
Nirvanashetty, Somashekara
Missamma, M.
Jackson-Michel, Shavon
The enhanced bioavailability of free curcumin and bioactive-metabolite tetrahydrocurcumin from a dispersible, oleoresin-based turmeric formulation
title The enhanced bioavailability of free curcumin and bioactive-metabolite tetrahydrocurcumin from a dispersible, oleoresin-based turmeric formulation
title_full The enhanced bioavailability of free curcumin and bioactive-metabolite tetrahydrocurcumin from a dispersible, oleoresin-based turmeric formulation
title_fullStr The enhanced bioavailability of free curcumin and bioactive-metabolite tetrahydrocurcumin from a dispersible, oleoresin-based turmeric formulation
title_full_unstemmed The enhanced bioavailability of free curcumin and bioactive-metabolite tetrahydrocurcumin from a dispersible, oleoresin-based turmeric formulation
title_short The enhanced bioavailability of free curcumin and bioactive-metabolite tetrahydrocurcumin from a dispersible, oleoresin-based turmeric formulation
title_sort enhanced bioavailability of free curcumin and bioactive-metabolite tetrahydrocurcumin from a dispersible, oleoresin-based turmeric formulation
topic 3800
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8270635/
https://www.ncbi.nlm.nih.gov/pubmed/34232211
http://dx.doi.org/10.1097/MD.0000000000026601
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