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
Conditions
Keywords
6-prenylnaringenin, Bioavailability, Pharmacokinetics, PBMC
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.
Interventions
DIETARY_SUPPLEMENTPlacebo
Mannitol and silicon dioxide capsules
DIETARY_SUPPLEMENTNative 6-prenylnaringenin
250 mg native 6-PN plus mannitol and silicon dioxide capsules
DIETARY_SUPPLEMENTMicellar 6-prenylnaringenin
250 mg 6-PN in a micellar formulation with Tween-80 as adjuvant capsules
Sponsors
Universität Tübingen
University of Hohenheim
Study design
Allocation
RANDOMIZED
Intervention model
CROSSOVER
Primary purpose
BASIC_SCIENCE
Masking
DOUBLE (Subject, Investigator)
Eligibility
Sex/Gender
ALL
Age
18 Years to 45 Years
Healthy volunteers
Yes
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
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| 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 |
| 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 |
| 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 |
| 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 |
| Cell count (dead cells/ml and living cells/ml) of PBMCs after 6-PN administration | 0 h, 6 h, and 24 h post dose | — |
| Cell viability of PBMCs after 6-PN administration | 0 h, 6 h, and 24 h post dose | — |
Secondary
| Measure | Time frame |
|---|---|
| Serum creatinine [mg/dL] | 0 h, 4 h, 24h post-dose |
| Serum total cholesterol [mg/dL] | 0 h, 4 h, 24h post-dose |
| Serum HDL cholesterol [mg/dL] | 0 h, 4 h, 24h post-dose |
| Serum LDL cholesterol [mg/dL] | 0 h, 4 h, 24h post-dose |
| Serum triacylglycerols [mg/dL] | 0 h, 4 h, 24h post-dose |
| LDL/HDL cholesterol ratio | 0 h, 4 h, 24h post-dose |
| Glomerular filtration rate [mL/min] | 0 h, 4 h, 24h post-dose |
| Serum glucose [mg/dL] | 0 h, 4 h, 24h post-dose |
| Serum aspartate transaminase activity [U/L] | 0 h, 4 h, 24h post-dose |
| Mean corpuscular hemoglobin concentration [g/dL] | 0 h, 24 h post-dose |
| Mean corpuscular hemoglobin [pg] | 0 h, 24 h post-dose |
| Mean corpuscular volume [fL] | 0 h, 24 h post-dose |
| Hematocrit [%] | 0 h, 24 h post-dose |
| Erythrocytes [/pL] | 0 h, 24 h post-dose |
| Thrombocytes [/nL] | 0 h, 24 h post-dose |
| Leucocytes [/nL] | 0 h, 24 h post-dose |
| Hemoglobin [g/dL] | 0 h, 24 h post-dose |
| Serum alanine 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 alkaline phosphatase activity [U/L] | 0 h, 4 h, 24h post-dose |
| Serum bilirubin | 0 h, 4 h, 24h post-dose |
| Serum uric acid [mg/dL] | 0 h, 4 h, 24h post-dose |
Countries
Germany
Outcome results
None listed