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CompletedNCT03286777Updated Oct 10, 2018

Increasing the Oral Bioavailability of 6-prenylnaringenin by Micellar Solubilization

An interventional study of Placebo and Native 6-prenylnaringenin in Safety of Native vs. Micellar 6-PN After Oral Intake, Pharmacokinetics of Native vs. Micellar 6-PN After Oral Intake and PBMC Activity After Native vs. Micellar 6-PN Oral Intake, sponsored by University of Hohenheim. Completed at 2 sites in Germany. Open to participants aged 18 Years to 45 Years, including healthy volunteers. Per ClinicalTrials.gov, last updated 2018-10-10.

Sponsored by University of Hohenheim · Not applicable, Interventional, and Basic science

Phase
Not applicable
Study type
Interventional
Enrollment
6
Allocation
Randomized
Ages
18 Years to 45 Years
Sex
All
01

Study 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.

02

Conditions studied

  • Safety of Native vs. Micellar 6-PN After Oral Intake
  • Pharmacokinetics of Native vs. Micellar 6-PN After Oral Intake
  • PBMC Activity After Native vs. Micellar 6-PN Oral Intake

Keywords

  • 6-prenylnaringenin
  • Bioavailability
  • Pharmacokinetics
  • PBMC
03

Who can participate

Ages eligible
18 Years to 45 Years
Sexes eligible
All
Accepts 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

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
04

Study design

Phase
Not applicable
Primary purpose
Basic science
Allocation
Randomized
Intervention model
Crossover assignment
Masking
Double (Participant, Investigator)
Enrollment
6 participants (actual)

Study arms

  • Placebo comparator
    Placebo

    Mannitol and silicon dioxide

    Dietary Supplement: Placebo

  • Experimental
    Native 6-prenylnaringenin

    250 mg native 6-PN plus mannitol and silicon dioxide

    Dietary Supplement: Native 6-prenylnaringenin

  • Experimental
    Micellar 6-prenylnaringenin

    250 mg 6-PN in a micellar formulation with Tween-80 as adjuvant

    Dietary Supplement: Micellar 6-prenylnaringenin

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

05

What researchers measure

Primary outcomes

  1. 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

  2. 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

  3. 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

  4. 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

  5. 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

  6. Cell viability of PBMCs after 6-PN administration

    Time frame: 0 h, 6 h, and 24 h post dose

Secondary outcomes

  1. Serum aspartate transaminase activity [U/L]

    Time frame: 0 h, 4 h, 24h post-dose

  2. Serum alanine transaminase activity [U/L]

    Time frame: 0 h, 4 h, 24h post-dose

  3. Serum gamma-glutamyl transferase activity [U/L]

    Time frame: 0 h, 4 h, 24h post-dose

  4. Serum alkaline phosphatase activity [U/L]

    Time frame: 0 h, 4 h, 24h post-dose

  5. Serum bilirubin

    Time frame: 0 h, 4 h, 24h post-dose

  6. Serum uric acid [mg/dL]

    Time frame: 0 h, 4 h, 24h post-dose

  7. Serum creatinine [mg/dL]

    Time frame: 0 h, 4 h, 24h post-dose

  8. Serum total cholesterol [mg/dL]

    Time frame: 0 h, 4 h, 24h post-dose

  9. Serum HDL cholesterol [mg/dL]

    Time frame: 0 h, 4 h, 24h post-dose

  10. Serum LDL cholesterol [mg/dL]

    Time frame: 0 h, 4 h, 24h post-dose

  11. Serum triacylglycerols [mg/dL]

    Time frame: 0 h, 4 h, 24h post-dose

  12. LDL/HDL cholesterol ratio

    Time frame: 0 h, 4 h, 24h post-dose

  13. Glomerular filtration rate [mL/min]

    Time frame: 0 h, 4 h, 24h post-dose

  14. Serum glucose [mg/dL]

    Time frame: 0 h, 4 h, 24h post-dose

  15. Hemoglobin [g/dL]

    Time frame: 0 h, 24 h post-dose

  16. Mean corpuscular hemoglobin concentration [g/dL]

    Time frame: 0 h, 24 h post-dose

  17. Mean corpuscular hemoglobin [pg]

    Time frame: 0 h, 24 h post-dose

  18. Mean corpuscular volume [fL]

    Time frame: 0 h, 24 h post-dose

  19. Hematocrit [%]

    Time frame: 0 h, 24 h post-dose

  20. Erythrocytes [/pL]

    Time frame: 0 h, 24 h post-dose

  21. Thrombocytes [/nL]

    Time frame: 0 h, 24 h post-dose

  22. Leucocytes [/nL]

    Time frame: 0 h, 24 h post-dose

06

Study locations

2 sites
  • University of Hohenheim
    Stuttgart, Baden-Württemberg 70599, Germany
  • Eberhard Karls University Tuebingen
    Tübingen, Baden-Württemberg 72076, Germany
07

References and documents

08

Registry details

Key details

Study ID
NCT03286777
Lead sponsor
University of Hohenheim
Collaborators
Universität Tübingen
Responsible party
Sponsor
First posted
Sep 18, 2017
Start date
Jun 22, 2017
Primary completion
Dec 31, 2017
Completion
Jul 1, 2018
Last update
Oct 10, 2018

Study contacts

Jan Frank, Prof. Dr.
principal investigator · University of Hohenheim
Sascha Venturelli, Dr. med. Dr. rer. nat.
principal investigator · University Hospital, Eberhard Karls University Tuebingen, Germany
Christian Busch, Dr. med.
principal investigator · University Hospital, Eberhard Karls University Tuebingen, Germany

Oversight

FDA-regulated drug
No
FDA-regulated device
No
View the source record on ClinicalTrials.gov ↗

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