Micellar Curcumin: Pharmacokinetics and Effects on Inflammation Markers and PCSK‐9 Concentrations in Healthy Subjects in a Double‐Blind, Randomized, Active‐Controlled, Crossover Trial
Scope: Preclinical models have demonstrated the anti‐inflammatory and lipid‐lowering effects of curcumin. Innovative formulations have been developed to overcome the poor bioavailability of native curcumin. The study hypothesizes that the bioavailability of micellar curcumin is superior to native cu...
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| Published in | Molecular nutrition & food research Vol. 66; no. 22; pp. e2200139 - n/a |
|---|---|
| Main Authors | , , , , , , , |
| Format | Journal Article |
| Language | English |
| Published |
Germany
Wiley Subscription Services, Inc
01.11.2022
John Wiley and Sons Inc |
| Subjects | |
| Online Access | Get full text |
| ISSN | 1613-4125 1613-4133 1613-4133 |
| DOI | 10.1002/mnfr.202200139 |
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| Abstract | Scope: Preclinical models have demonstrated the anti‐inflammatory and lipid‐lowering effects of curcumin. Innovative formulations have been developed to overcome the poor bioavailability of native curcumin. The study hypothesizes that the bioavailability of micellar curcumin is superior to native curcumin and investigates the potential anti‐inflammatory and proprotein convertase subtilisin/kexin type 9 (PCSK9) concentration lowering effects.
Methods and results: In this double‐blind, randomized, crossover trial, 15 healthy volunteers receive micellar or native curcumin (105 mg day−1) for 7 days with a ≥7 days washout period. Curcumin and metabolite concentrations are quantified by high‐performance liquid chromatography with fluorescence detection (HPLC‐FD), and pharmacokinetics are calculated. To analyze anti‐inflammatory effects, blood samples (baseline, 2 h, 7 days) are stimulated with 50 ng mL−1 lipopolysaccharides (LPS). Interleukin (IL)‐6, tumor‐necrosis factor (TNF‐α), and PCSK9 concentrations are quantified. Micellar curcumin demonstrates improved bioavailability (≈39‐fold higher maximum concentrations, ≈14‐fold higher area‐under‐the‐time‐concentration curve, p < 0.001) but does not reduce pro‐inflammatory cytokines in the chosen model. Subjects receiving micellar curcumin have significantly lower PCSK9 concentrations (≈10% reduction) after 7 days compared to baseline (p = 0.038).
Conclusion: Micellar curcumin demonstrates an improved oral bioavailability but does not show anti‐inflammatory effects in this model. Potential effects on PCSK9 concentrations warrant further investigation.
A micellar formulation of curcumin improves the absorption compared to native curcumin in 15 healthy volunteers. Intake of micellar curcumin reduces PCSK9 concentrations (≈10% reduction) after 7 days which could improve the blood lipid profile. In contrast to pre‐clinical studies, curcumin has no impact on the inflammatory response in our chosen model. Curcumin has an excellent safety profile. |
|---|---|
| AbstractList | Scope: Preclinical models have demonstrated the anti‐inflammatory and lipid‐lowering effects of curcumin. Innovative formulations have been developed to overcome the poor bioavailability of native curcumin. The study hypothesizes that the bioavailability of micellar curcumin is superior to native curcumin and investigates the potential anti‐inflammatory and proprotein convertase subtilisin/kexin type 9 (PCSK9) concentration lowering effects. Methods and results: In this double‐blind, randomized, crossover trial, 15 healthy volunteers receive micellar or native curcumin (105 mg day⁻¹) for 7 days with a ≥7 days washout period. Curcumin and metabolite concentrations are quantified by high‐performance liquid chromatography with fluorescence detection (HPLC‐FD), and pharmacokinetics are calculated. To analyze anti‐inflammatory effects, blood samples (baseline, 2 h, 7 days) are stimulated with 50 ng mL⁻¹ lipopolysaccharides (LPS). Interleukin (IL)‐6, tumor‐necrosis factor (TNF‐α), and PCSK9 concentrations are quantified. Micellar curcumin demonstrates improved bioavailability (≈39‐fold higher maximum concentrations, ≈14‐fold higher area‐under‐the‐time‐concentration curve, p < 0.001) but does not reduce pro‐inflammatory cytokines in the chosen model. Subjects receiving micellar curcumin have significantly lower PCSK9 concentrations (≈10% reduction) after 7 days compared to baseline (p = 0.038). Conclusion: Micellar curcumin demonstrates an improved oral bioavailability but does not show anti‐inflammatory effects in this model. Potential effects on PCSK9 concentrations warrant further investigation. Scope: Preclinical models have demonstrated the anti‐inflammatory and lipid‐lowering effects of curcumin. Innovative formulations have been developed to overcome the poor bioavailability of native curcumin. The study hypothesizes that the bioavailability of micellar curcumin is superior to native curcumin and investigates the potential anti‐inflammatory and proprotein convertase subtilisin/kexin type 9 (PCSK9) concentration lowering effects. Methods and results: In this double‐blind, randomized, crossover trial, 15 healthy volunteers receive micellar or native curcumin (105 mg day−1) for 7 days with a ≥7 days washout period. Curcumin and metabolite concentrations are quantified by high‐performance liquid chromatography with fluorescence detection (HPLC‐FD), and pharmacokinetics are calculated. To analyze anti‐inflammatory effects, blood samples (baseline, 2 h, 7 days) are stimulated with 50 ng mL−1 lipopolysaccharides (LPS). Interleukin (IL)‐6, tumor‐necrosis factor (TNF‐α), and PCSK9 concentrations are quantified. Micellar curcumin demonstrates improved bioavailability (≈39‐fold higher maximum concentrations, ≈14‐fold higher area‐under‐the‐time‐concentration curve, p < 0.001) but does not reduce pro‐inflammatory cytokines in the chosen model. Subjects receiving micellar curcumin have significantly lower PCSK9 concentrations (≈10% reduction) after 7 days compared to baseline (p = 0.038). Conclusion: Micellar curcumin demonstrates an improved oral bioavailability but does not show anti‐inflammatory effects in this model. Potential effects on PCSK9 concentrations warrant further investigation. A micellar formulation of curcumin improves the absorption compared to native curcumin in 15 healthy volunteers. Intake of micellar curcumin reduces PCSK9 concentrations (≈10% reduction) after 7 days which could improve the blood lipid profile. In contrast to pre‐clinical studies, curcumin has no impact on the inflammatory response in our chosen model. Curcumin has an excellent safety profile. Scope: Preclinical models have demonstrated the anti‐inflammatory and lipid‐lowering effects of curcumin. Innovative formulations have been developed to overcome the poor bioavailability of native curcumin. The study hypothesizes that the bioavailability of micellar curcumin is superior to native curcumin and investigates the potential anti‐inflammatory and proprotein convertase subtilisin/kexin type 9 (PCSK9) concentration lowering effects. Methods and results: In this double‐blind, randomized, crossover trial, 15 healthy volunteers receive micellar or native curcumin (105 mg day−1) for 7 days with a ≥7 days washout period. Curcumin and metabolite concentrations are quantified by high‐performance liquid chromatography with fluorescence detection (HPLC‐FD), and pharmacokinetics are calculated. To analyze anti‐inflammatory effects, blood samples (baseline, 2 h, 7 days) are stimulated with 50 ng mL−1 lipopolysaccharides (LPS). Interleukin (IL)‐6, tumor‐necrosis factor (TNF‐α), and PCSK9 concentrations are quantified. Micellar curcumin demonstrates improved bioavailability (≈39‐fold higher maximum concentrations, ≈14‐fold higher area‐under‐the‐time‐concentration curve, p < 0.001) but does not reduce pro‐inflammatory cytokines in the chosen model. Subjects receiving micellar curcumin have significantly lower PCSK9 concentrations (≈10% reduction) after 7 days compared to baseline (p = 0.038). Conclusion: Micellar curcumin demonstrates an improved oral bioavailability but does not show anti‐inflammatory effects in this model. Potential effects on PCSK9 concentrations warrant further investigation. A micellar formulation of curcumin improves the absorption compared to native curcumin in 15 healthy volunteers. Intake of micellar curcumin reduces PCSK9 concentrations (≈10% reduction) after 7 days which could improve the blood lipid profile. In contrast to pre‐clinical studies, curcumin has no impact on the inflammatory response in our chosen model. Curcumin has an excellent safety profile. Scope: Preclinical models have demonstrated the anti‐inflammatory and lipid‐lowering effects of curcumin. Innovative formulations have been developed to overcome the poor bioavailability of native curcumin. The study hypothesizes that the bioavailability of micellar curcumin is superior to native curcumin and investigates the potential anti‐inflammatory and proprotein convertase subtilisin/kexin type 9 (PCSK9) concentration lowering effects.Methods and results: In this double‐blind, randomized, crossover trial, 15 healthy volunteers receive micellar or native curcumin (105 mg day−1) for 7 days with a ≥7 days washout period. Curcumin and metabolite concentrations are quantified by high‐performance liquid chromatography with fluorescence detection (HPLC‐FD), and pharmacokinetics are calculated. To analyze anti‐inflammatory effects, blood samples (baseline, 2 h, 7 days) are stimulated with 50 ng mL−1 lipopolysaccharides (LPS). Interleukin (IL)‐6, tumor‐necrosis factor (TNF‐α), and PCSK9 concentrations are quantified. Micellar curcumin demonstrates improved bioavailability (≈39‐fold higher maximum concentrations, ≈14‐fold higher area‐under‐the‐time‐concentration curve, p < 0.001) but does not reduce pro‐inflammatory cytokines in the chosen model. Subjects receiving micellar curcumin have significantly lower PCSK9 concentrations (≈10% reduction) after 7 days compared to baseline (p = 0.038).Conclusion: Micellar curcumin demonstrates an improved oral bioavailability but does not show anti‐inflammatory effects in this model. Potential effects on PCSK9 concentrations warrant further investigation. Preclinical models have demonstrated the anti-inflammatory and lipid-lowering effects of curcumin. Innovative formulations have been developed to overcome the poor bioavailability of native curcumin. The study hypothesizes that the bioavailability of micellar curcumin is superior to native curcumin and investigates the potential anti-inflammatory and proprotein convertase subtilisin/kexin type 9 (PCSK9) concentration lowering effects. In this double-blind, randomized, crossover trial, 15 healthy volunteers receive micellar or native curcumin (105 mg day ) for 7 days with a ≥7 days washout period. Curcumin and metabolite concentrations are quantified by high-performance liquid chromatography with fluorescence detection (HPLC-FD), and pharmacokinetics are calculated. To analyze anti-inflammatory effects, blood samples (baseline, 2 h, 7 days) are stimulated with 50 ng mL lipopolysaccharides (LPS). Interleukin (IL)-6, tumor-necrosis factor (TNF-α), and PCSK9 concentrations are quantified. Micellar curcumin demonstrates improved bioavailability (≈39-fold higher maximum concentrations, ≈14-fold higher area-under-the-time-concentration curve, p < 0.001) but does not reduce pro-inflammatory cytokines in the chosen model. Subjects receiving micellar curcumin have significantly lower PCSK9 concentrations (≈10% reduction) after 7 days compared to baseline (p = 0.038). Micellar curcumin demonstrates an improved oral bioavailability but does not show anti-inflammatory effects in this model. Potential effects on PCSK9 concentrations warrant further investigation. Preclinical models have demonstrated the anti-inflammatory and lipid-lowering effects of curcumin. Innovative formulations have been developed to overcome the poor bioavailability of native curcumin. The study hypothesizes that the bioavailability of micellar curcumin is superior to native curcumin and investigates the potential anti-inflammatory and proprotein convertase subtilisin/kexin type 9 (PCSK9) concentration lowering effects.SCOPEPreclinical models have demonstrated the anti-inflammatory and lipid-lowering effects of curcumin. Innovative formulations have been developed to overcome the poor bioavailability of native curcumin. The study hypothesizes that the bioavailability of micellar curcumin is superior to native curcumin and investigates the potential anti-inflammatory and proprotein convertase subtilisin/kexin type 9 (PCSK9) concentration lowering effects.In this double-blind, randomized, crossover trial, 15 healthy volunteers receive micellar or native curcumin (105 mg day-1 ) for 7 days with a ≥7 days washout period. Curcumin and metabolite concentrations are quantified by high-performance liquid chromatography with fluorescence detection (HPLC-FD), and pharmacokinetics are calculated. To analyze anti-inflammatory effects, blood samples (baseline, 2 h, 7 days) are stimulated with 50 ng mL-1 lipopolysaccharides (LPS). Interleukin (IL)-6, tumor-necrosis factor (TNF-α), and PCSK9 concentrations are quantified. Micellar curcumin demonstrates improved bioavailability (≈39-fold higher maximum concentrations, ≈14-fold higher area-under-the-time-concentration curve, p < 0.001) but does not reduce pro-inflammatory cytokines in the chosen model. Subjects receiving micellar curcumin have significantly lower PCSK9 concentrations (≈10% reduction) after 7 days compared to baseline (p = 0.038).METHODS AND RESULTSIn this double-blind, randomized, crossover trial, 15 healthy volunteers receive micellar or native curcumin (105 mg day-1 ) for 7 days with a ≥7 days washout period. Curcumin and metabolite concentrations are quantified by high-performance liquid chromatography with fluorescence detection (HPLC-FD), and pharmacokinetics are calculated. To analyze anti-inflammatory effects, blood samples (baseline, 2 h, 7 days) are stimulated with 50 ng mL-1 lipopolysaccharides (LPS). Interleukin (IL)-6, tumor-necrosis factor (TNF-α), and PCSK9 concentrations are quantified. Micellar curcumin demonstrates improved bioavailability (≈39-fold higher maximum concentrations, ≈14-fold higher area-under-the-time-concentration curve, p < 0.001) but does not reduce pro-inflammatory cytokines in the chosen model. Subjects receiving micellar curcumin have significantly lower PCSK9 concentrations (≈10% reduction) after 7 days compared to baseline (p = 0.038).Micellar curcumin demonstrates an improved oral bioavailability but does not show anti-inflammatory effects in this model. Potential effects on PCSK9 concentrations warrant further investigation.CONCLUSIONMicellar curcumin demonstrates an improved oral bioavailability but does not show anti-inflammatory effects in this model. Potential effects on PCSK9 concentrations warrant further investigation. Scope : Preclinical models have demonstrated the anti‐inflammatory and lipid‐lowering effects of curcumin. Innovative formulations have been developed to overcome the poor bioavailability of native curcumin. The study hypothesizes that the bioavailability of micellar curcumin is superior to native curcumin and investigates the potential anti‐inflammatory and proprotein convertase subtilisin/kexin type 9 (PCSK9) concentration lowering effects. Methods and results : In this double‐blind, randomized, crossover trial, 15 healthy volunteers receive micellar or native curcumin (105 mg day −1 ) for 7 days with a ≥7 days washout period. Curcumin and metabolite concentrations are quantified by high‐performance liquid chromatography with fluorescence detection (HPLC‐FD), and pharmacokinetics are calculated. To analyze anti‐inflammatory effects, blood samples (baseline, 2 h, 7 days) are stimulated with 50 ng mL −1 lipopolysaccharides (LPS). Interleukin (IL)‐6, tumor‐necrosis factor (TNF‐α), and PCSK9 concentrations are quantified. Micellar curcumin demonstrates improved bioavailability (≈39‐fold higher maximum concentrations, ≈14‐fold higher area‐under‐the‐time‐concentration curve, p < 0.001) but does not reduce pro‐inflammatory cytokines in the chosen model. Subjects receiving micellar curcumin have significantly lower PCSK9 concentrations (≈10% reduction) after 7 days compared to baseline ( p = 0.038). Conclusion : Micellar curcumin demonstrates an improved oral bioavailability but does not show anti‐inflammatory effects in this model. Potential effects on PCSK9 concentrations warrant further investigation. |
| Author | Buchtele, Nina Frank, Jan Schoergenhofer, Christian Derhaschnig, Ulla Jilma, Bernd Grafeneder, Juergen Sus, Nadine Eskandary, Farsad |
| AuthorAffiliation | 2 Department of Clinical Pharmacology Medical University of Vienna Vienna 1090 Austria 4 Department of Medicine I Medical University of Vienna Vienna 1090 Austria 1 Department of Emergency Medicine Medical University of Vienna Vienna 1090 Austria 3 Division of Nephrology, Department of Medicine III Medical University of Vienna Vienna 1090 Austria 5 Department of Food Biofunctionality (140b) Institute of Nutritional Sciences University of Hohenheim Stuttgart Germany |
| AuthorAffiliation_xml | – name: 1 Department of Emergency Medicine Medical University of Vienna Vienna 1090 Austria – name: 3 Division of Nephrology, Department of Medicine III Medical University of Vienna Vienna 1090 Austria – name: 2 Department of Clinical Pharmacology Medical University of Vienna Vienna 1090 Austria – name: 5 Department of Food Biofunctionality (140b) Institute of Nutritional Sciences University of Hohenheim Stuttgart Germany – name: 4 Department of Medicine I Medical University of Vienna Vienna 1090 Austria |
| Author_xml | – sequence: 1 givenname: Juergen orcidid: 0000-0002-3639-0106 surname: Grafeneder fullname: Grafeneder, Juergen organization: Medical University of Vienna – sequence: 2 givenname: Ulla surname: Derhaschnig fullname: Derhaschnig, Ulla organization: Medical University of Vienna – sequence: 3 givenname: Farsad surname: Eskandary fullname: Eskandary, Farsad organization: Medical University of Vienna – sequence: 4 givenname: Nina surname: Buchtele fullname: Buchtele, Nina organization: Medical University of Vienna – sequence: 5 givenname: Nadine surname: Sus fullname: Sus, Nadine organization: University of Hohenheim – sequence: 6 givenname: Jan surname: Frank fullname: Frank, Jan organization: University of Hohenheim – sequence: 7 givenname: Bernd surname: Jilma fullname: Jilma, Bernd email: bernd.jilma@meduniwien.ac.at organization: Medical University of Vienna – sequence: 8 givenname: Christian surname: Schoergenhofer fullname: Schoergenhofer, Christian organization: Medical University of Vienna |
| BackLink | https://www.ncbi.nlm.nih.gov/pubmed/36101515$$D View this record in MEDLINE/PubMed |
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| Snippet | Scope: Preclinical models have demonstrated the anti‐inflammatory and lipid‐lowering effects of curcumin. Innovative formulations have been developed to... Scope : Preclinical models have demonstrated the anti‐inflammatory and lipid‐lowering effects of curcumin. Innovative formulations have been developed to... Preclinical models have demonstrated the anti-inflammatory and lipid-lowering effects of curcumin. Innovative formulations have been developed to overcome the... |
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| SubjectTerms | Active control Anti-Inflammatory Agents - pharmacology Bioavailability Biomarkers blood Cross-Over Studies Curcumin Curcumin - metabolism Cytokines Double-blind studies fluorescence food research Healthy Volunteers High-performance liquid chromatography Humans Inflammation Inflammation - drug therapy Interleukin-6 Interleukins Kexin Lipids lipopolysaccharide Lipopolysaccharides Liquid chromatography Metabolites Micelles nutrition PCSK9 Pharmacokinetics Pharmacology Proprotein Convertase 9 Proprotein convertases Subtilisin TNF‐α Tumor necrosis factor Tumors |
| Title | Micellar Curcumin: Pharmacokinetics and Effects on Inflammation Markers and PCSK‐9 Concentrations in Healthy Subjects in a Double‐Blind, Randomized, Active‐Controlled, Crossover Trial |
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