Pharmacological Profile of Different Quercetin Formulations

Comparing the Pharmacological Profile of Different Quercetin Formulations in Healthy Volunteers

This study aims to evaluate the pharmacokinetics of quercetin in healthy participants after the administration of different formulations in a single- and multiple-dose phase. In the single-dose study, plasma uptake (AUC0-24 and Cmax) of standard quercetin is compared with that of LipoMicel®-a novel food-grade delivery form of quercetin. In the multiple dose study, accumulating plasma concentrations of formulated quercetin are observed over 72hrs, after repeated doses of LipoMicel treatments (AUC0-72).

At least ten healthy adults participate in an open-label, diet-controlled, crossover, plasma uptake study. Participants receive three different doses (250 mg, 500 mg or 1000 mg) of quercetin aglycone orally.

Study Overview

• Status: Completed
• Conditions: Pharmacokinetics
• Intervention / Treatment: Dietary supplement: Quercetin LipoMicel (250 mg); Dietary supplement: Quercetin LipoMicel (500 mg); Dietary supplement: Quercetin LipoMicel (1000 mg); Dietary supplement: Regular/standard Quercetin (500 mg)

Detailed Description

Objective of this study is to investigate the pharmacokinetic profile of formulated quercetin (LipoMicel®), administered at three different doses, in healthy participants and compare it with that of a standard formulation. The pharmacokinetics of the different quercetin treatments are observed over 24hrs after a single orally administered dose of quercetin (e.g., using AUC0-24 and Cmax). Furthermore, the accumulating plasma concentrations of formulated quercetin are monitored over a 72hr period (e.g., using AUC0-72), following multiple orally administered doses of LipoMicel treatments (250 mg-1000 mg) plus the circulating metabolites of quercetin are determined in the human plasma.

• Study Type: Interventional
• Enrollment (Actual): 10
• Phase: Not Applicable

Contacts and Locations

Study Locations

• Canada
  • British Columbia
    • Burnaby, British Columbia, Canada, V3N4S9
      • ISURA

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 65 years (Adult, Older Adult)
• Accepts Healthy Volunteers: No
• Genders Eligible for Study: All

Description

Inclusion Criteria:

• age 18-65
• healthy, good physical condition

Exclusion Criteria:

• pregnancy or breast-feeding
• gastrointestinal conditions (acute or chronic)
• liver disease (acute or chronic)
• kidney disease (acute or chronic)
• cardiovascular disease (acute or chronic)
• hematological disease
• diabetes
• allergy or intolerance to gluten
• allergy or intolerance to quercetin
• use of any form of nicotine or tobacco, CBD/THC
• alcohol and substance abuse history
• use of medications (e.g., anti-inflammatory)
• use of quercetin supplements
• participation in another investigational study

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: Non-Randomized
• Interventional Model: Crossover Assignment
• Masking: None (Open Label)

Number of Arms

4

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Quercetin LipoMicel (250 mg); Each participant receives their treatment of Quercetin LipoMicel at a total dose of 250 mg quercetin. Treatments are consumed with a glass of water (approx. 200 mL), but with no food (4hr fasting condition). Capillary whole blood samples are collected at time points 0, 0.5, 1, 2, 3, 4, 6, 8, 10, 12, and 24hrs following a single-dose administration of quercetin and at 25, 47, 48, 71 and 72hrs after a repeated oral total dose of 250 mg LipoMicel (once daily for 72hrs). A washout period of at least 7 days between each treatment will be used.	Dietary supplement: Quercetin LipoMicel (250 mg); Quercetin LipoMicel® soft-gels. Total dose of 250 mg of quercetin
Experimental: Quercetin LipoMicel (500 mg); Each participant receives their treatment of Quercetin LipoMicel at a total dose of 500 mg quercetin. Treatments are consumed with a glass of water (approx. 200 mL), but with no food (4hr fasting condition). Capillary whole blood samples are collected at time points 0, 0.5, 1, 2, 3, 4, 6, 8, 10, 12, and 24hrs following a single-dose administration of quercetin and at 25, 47, 48, 71 and 72hrs after a repeated oral total dose of 500 mg LipoMicel (once daily for 72hrs). A washout period of at least 7 days between each treatment will be used.	Dietary supplement: Quercetin LipoMicel (500 mg); Quercetin LipoMicel® soft-gels. Total dose of 500 mg of quercetin
Experimental: Quercetin LipoMicel (1000 mg); Each participant receives their treatment of Quercetin LipoMicel at a total dose of 1000 mg quercetin. Treatments are consumed with a glass of water (approx. 200 mL), but with no food (4hr fasting condition). Capillary whole blood samples are collected at time points 0, 0.5, 1, 2, 3, 4, 6, 8, 10, 12, and 24hrs following a single-dose administration of quercetin and at 25, 47, 48, 71 and 72hrs after a repeated oral total dose of 1000 mg LipoMicel (once daily for 72hrs). A washout period of at least 7 days between each treatment will be used.	Dietary supplement: Quercetin LipoMicel (1000 mg); Quercetin LipoMicel® soft-gels. Total dose of 1000 mg of quercetin
Experimental: Regular/standard Quercetin (500 mg); Each participant receives their treatment of standard/raw Quercetin at a total dose of 500 mg quercetin. Treatments are consumed with a glass of water (approx. 200 mL), but with no food (4hr fasting condition). A standardized lunch and dinner are served after 4h and 8h of product administration. Capillary whole blood samples are collected (after a 10hr overnight fast) at time points 0, 0.5, 1, 2, 3, 4, 6, 8, 10, 12, and 24hrs following a single-dose administration of quercetin. A washout period of at least 7 days between each treatment will be used.	Dietary supplement: Regular/standard Quercetin (500 mg); Total dose of 500 mg of quercetin

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
AUC: the area under the concentration-time curve	To evaluate the plasma uptake of orally ingested quercetin (aglycone) in a novel formulation ("LipoMicel") in healthy adults by comparing the Area under the concentration-time curve (AUC) with that of standard/regular quercetin (aglycone).	0 (baseline; pre-dose), 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48 and 72 hours
Cmax: maximum plasma concentration	To evaluate the plasma uptake of orally ingested quercetin (aglycone) in a novel formulation ("LipoMicel") in healthy adults by comparing the Peak Plasma Concentration (Cmax) with that of standard/regular quercetin (aglycone).	0 (baseline; pre-dose), 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48 and 72 hours
Tmax: the time point of maximum plasma concentration	To evaluate the plasma uptake of orally ingested quercetin (aglycone) in a novel formulation ("LipoMicel") in healthy adults by comparing the time point of maximum plasma concentration (Tmax) with that of standard/regular quercetin (aglycone).	0 (baseline; pre-dose), 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48 and 72 hours

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
AUC: the area under the concentration-time curve (quercetin metabolites)	To determine the plasma concentrations of quercetin metabolites following the oral consumption of LipoMicel® 250 mg, over a period of 72hrs, by calculating AUC.	0 (baseline; pre-dose), 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48 and 72 hours
Cmax: maximum plasma concentration (quercetin metabolites)	To determine the peak plasma concentrations of quercetin metabolites following the oral consumption of LipoMicel® 250 mg, over a period of 72hrs, by calculating Cmax.	0 (baseline; pre-dose), 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48 and 72 hours
Tmax: the time point of maximum plasma concentration (quercetin metabolites)	To determine the time point of maximum plasma concentration of quercetin metabolites following the oral consumption of LipoMicel® 250 mg, over a period of 72hrs, by calculating Tmax.	0 (baseline; pre-dose), 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48 and 72 hours

Collaborators and Investigators

• Sponsor: Factors Group of Nutritional Companies Inc.

Study record dates

Study Major Dates

• Study Start (Actual): January 31, 2022
• Primary Completion (Actual): July 31, 2022
• Study Completion (Actual): October 31, 2022

Study Registration Dates

• First Submitted: November 3, 2022
• First Submitted That Met QC Criteria: November 3, 2022
• First Posted (Actual): November 10, 2022

Study Record Updates

• Last Update Posted (Actual): November 10, 2022
• Last Update Submitted That Met QC Criteria: November 3, 2022
• Last Verified: November 1, 2022

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Physiological Effects of Drugs; Molecular Mechanisms of Pharmacological Action; Protective Agents; Antioxidants; Quercetin
• Other Study ID Numbers: 2021-03-002

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: No

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: No
• Studies a U.S. FDA-regulated device product: No