Increasing the Oral Bioavailability of 6-prenylnaringenin by Micellar Solubilization

Not Applicable

Completed

• Conditions: PBMC Activity After Native vs. Micellar 6-PN Oral Intake; Pharmacokinetics of Native vs. Micellar 6-PN After Oral Intake; Safety of Native vs. Micellar 6-PN After Oral Intake
• Interventions: Dietary Supplement: Placebo; Dietary Supplement: Micellar 6-prenylnaringenin; Dietary Supplement: Native 6-prenylnaringenin

• Registration Number: NCT03286777
• Lead Sponsor: University of Hohenheim

Brief Summary

Micellar encapsulation will be tested to increase the oral bioavailability in humans of 6-prenylnaringenin (6-PN) from hops (Humulus lupulus). The study follows a single dose (250 mg 6-PN), placebo controlled, randomized, double-blind, three armed crossover study design with ≥2-week washout periods. Plasma, urine and PBMC samples will be collected at intervals up to 24 h after intake of the native compound, the micellar formulation or placebo. The safety, pharmacokinetics and impact of oral prenylflavonoids on PBMC survival will be investigated.

Detailed Description

Not available

Study Timeline

• Study Start: 2017-06-22
• Study First Submitted: 2017-09-14
• Study First Submitted QC: 2017-09-14
• Study First Posted: 2017-09-18
• Primary Completion: 2017-12-31
• Study Completion: 2018-07-01
• Status Verified: 2018-10
• Last Update Submitted: 2018-10-09
• Last Update Posted: 2018-10-10

Recruitment & Eligibility

• Status: COMPLETED
• Sex: All
• Target Recruitment: 6

Inclusion Criteria

• Healthy volunteers with blood chemistry values within normal ranges
• Age: 18-45 years
• BMI: 19-25 kg/m2

Exclusion Criteria

• Pregnancy or lactation
• Alcohol and/or drug abuse
• Use of dietary supplements or any medications, except contraceptives
• Any known malignant, metabolic and endocrine diseases
• Previous cardiac infarction
• Dementia
• Participation in a clinical trial within the past 6 weeks prior to recruitment
• Physical activity of more than 5 h/wk

Study & Design

• Study Type: INTERVENTIONAL
• Study Design: CROSSOVER

Arm && Interventions

Group	Intervention	Description
Placebo	Placebo	Mannitol and silicon dioxide
Micellar 6-prenylnaringenin	Micellar 6-prenylnaringenin	250 mg 6-PN in a micellar formulation with Tween-80 as adjuvant
Native 6-prenylnaringenin	Native 6-prenylnaringenin	250 mg native 6-PN plus mannitol and silicon dioxide

Primary Outcome Measures

Name	Time	Method
Mean maximum plasma concentration (Cmax) of total 6-PN [nmol/L]	0 h, 0.5 h, 1 h, 2 h, 4 h, 6 h, 8 h and 24 h post dose	Total 6-PN determined after deconjugation with beta-glucuronidase/sulphatase
Mean area under the curve (AUC) of plasma concentration vs. time of total 6-PN [nmol/L*h]	0 h, 0.5 h, 1 h, 2 h, 4 h, 6 h, 8 h and 24 h post dose	Total 6-PN determined after deconjugation with beta-glucuronidase/sulphatase
Cell count (dead cells/ml and living cells/ml) of PBMCs after 6-PN administration	0 h, 6 h, and 24 h post dose
Time to reach maximum plasma concentration (Tmax) of total 6-PN [h]	0 h, 0.5 h, 1 h, 2 h, 4 h, 6 h, 8 h and 24 h post dose	Total 6-PN determined after deconjugation with beta-glucuronidase/sulphatase
Cell viability of PBMCs after 6-PN administration	0 h, 6 h, and 24 h post dose
Cumulative urinary excretion of total 6-PN [nmol/g creatinine]	0 h - 24 h post dose	Total 6-PN determined after deconjugation with beta-glucuronidase/sulphatase

Secondary Outcome Measures

Name	Time	Method
Serum HDL cholesterol [mg/dL]	0 h, 4 h, 24h post-dose
Serum glucose [mg/dL]	0 h, 4 h, 24h post-dose
Serum alanine transaminase activity [U/L]	0 h, 4 h, 24h post-dose
Serum aspartate transaminase activity [U/L]	0 h, 4 h, 24h post-dose
Serum gamma-glutamyl transferase activity [U/L]	0 h, 4 h, 24h post-dose
Serum bilirubin	0 h, 4 h, 24h post-dose
Serum LDL cholesterol [mg/dL]	0 h, 4 h, 24h post-dose
Serum total cholesterol [mg/dL]	0 h, 4 h, 24h post-dose
LDL/HDL cholesterol ratio	0 h, 4 h, 24h post-dose
Mean corpuscular hemoglobin concentration [g/dL]	0 h, 24 h post-dose
Hematocrit [%]	0 h, 24 h post-dose
Erythrocytes [/pL]	0 h, 24 h post-dose
Serum alkaline phosphatase activity [U/L]	0 h, 4 h, 24h post-dose
Serum triacylglycerols [mg/dL]	0 h, 4 h, 24h post-dose
Mean corpuscular hemoglobin [pg]	0 h, 24 h post-dose
Serum uric acid [mg/dL]	0 h, 4 h, 24h post-dose
Serum creatinine [mg/dL]	0 h, 4 h, 24h post-dose
Glomerular filtration rate [mL/min]	0 h, 4 h, 24h post-dose
Hemoglobin [g/dL]	0 h, 24 h post-dose
Mean corpuscular volume [fL]	0 h, 24 h post-dose
Thrombocytes [/nL]	0 h, 24 h post-dose
Leucocytes [/nL]	0 h, 24 h post-dose

Trial Locations

Locations (2)

Eberhard Karls University Tuebingen; 🇩🇪 Tübingen, Baden-Württemberg, Germany

University of Hohenheim; 🇩🇪 Stuttgart, Baden-Württemberg, Germany