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.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
BASIC_SCIENCE
Masking
DOUBLE
Enrollment
6
Mannitol and silicon dioxide capsules
250 mg native 6-PN plus mannitol and silicon dioxide capsules
250 mg 6-PN in a micellar formulation with Tween-80 as adjuvant capsules
University of Hohenheim
Stuttgart, Baden-Wurttemberg, Germany
Eberhard Karls University Tuebingen
Tübingen, Baden-Wurttemberg, Germany
Mean area under the curve (AUC) of plasma concentration vs. time of total 6-PN [nmol/L*h]
Total 6-PN determined after deconjugation with beta-glucuronidase/sulphatase
Time frame: 0 h, 0.5 h, 1 h, 2 h, 4 h, 6 h, 8 h and 24 h post dose
Mean maximum plasma concentration (Cmax) of total 6-PN [nmol/L]
Total 6-PN determined after deconjugation with beta-glucuronidase/sulphatase
Time frame: 0 h, 0.5 h, 1 h, 2 h, 4 h, 6 h, 8 h and 24 h post dose
Time to reach maximum plasma concentration (Tmax) of total 6-PN [h]
Total 6-PN determined after deconjugation with beta-glucuronidase/sulphatase
Time frame: 0 h, 0.5 h, 1 h, 2 h, 4 h, 6 h, 8 h and 24 h post dose
Cumulative urinary excretion of total 6-PN [nmol/g creatinine]
Total 6-PN determined after deconjugation with beta-glucuronidase/sulphatase
Time frame: 0 h - 24 h post dose
Cell count (dead cells/ml and living cells/ml) of PBMCs after 6-PN administration
Time frame: 0 h, 6 h, and 24 h post dose
Cell viability of PBMCs after 6-PN administration
Time frame: 0 h, 6 h, and 24 h post dose
Serum aspartate transaminase activity [U/L]
Time frame: 0 h, 4 h, 24h post-dose
Serum alanine transaminase activity [U/L]
Time frame: 0 h, 4 h, 24h post-dose
Serum gamma-glutamyl transferase activity [U/L]
Time frame: 0 h, 4 h, 24h post-dose
Serum alkaline phosphatase activity [U/L]
Time frame: 0 h, 4 h, 24h post-dose
Serum bilirubin
Time frame: 0 h, 4 h, 24h post-dose
Serum uric acid [mg/dL]
Time frame: 0 h, 4 h, 24h post-dose
Serum creatinine [mg/dL]
Time frame: 0 h, 4 h, 24h post-dose
Serum total cholesterol [mg/dL]
Time frame: 0 h, 4 h, 24h post-dose
Serum HDL cholesterol [mg/dL]
Time frame: 0 h, 4 h, 24h post-dose
Serum LDL cholesterol [mg/dL]
Time frame: 0 h, 4 h, 24h post-dose
Serum triacylglycerols [mg/dL]
Time frame: 0 h, 4 h, 24h post-dose
LDL/HDL cholesterol ratio
Time frame: 0 h, 4 h, 24h post-dose
Glomerular filtration rate [mL/min]
Time frame: 0 h, 4 h, 24h post-dose
Serum glucose [mg/dL]
Time frame: 0 h, 4 h, 24h post-dose
Hemoglobin [g/dL]
Time frame: 0 h, 24 h post-dose
Mean corpuscular hemoglobin concentration [g/dL]
Time frame: 0 h, 24 h post-dose
Mean corpuscular hemoglobin [pg]
Time frame: 0 h, 24 h post-dose
Mean corpuscular volume [fL]
Time frame: 0 h, 24 h post-dose
Hematocrit [%]
Time frame: 0 h, 24 h post-dose
Erythrocytes [/pL]
Time frame: 0 h, 24 h post-dose
Thrombocytes [/nL]
Time frame: 0 h, 24 h post-dose
Leucocytes [/nL]
Time frame: 0 h, 24 h post-dose
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