Clinical trial NCT05561075: Oral Bioavailability of Pterostilbene Cocrystal Compared to Its Free Form (BIOPTERO)
Official title: Evaluation of the Oral Bioavailability of Pterostilbene Cocrystal Compared to Its Free Form in Healthy Volunteers. Crossover, Randomized, Double-Blind Study (BIOPTERO)
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: NA
Conditions: Biological Availability
Keywords: Polyphenols
Antioxidant activity
Co-crystallization
Pterostilbene
Lead sponsor: Fundació Eurecat
Sponsor class: OTHER
Collaborators: name: Circe, S.L.
First posted: 2022-09-30
Enrollment: 6
Sex: ALL
Minimum age (years): 18
Maximum age (years): 65
Standard ages: ADULT
OLDER_ADULT
Accepts healthy volunteers: yes
Allocation: RANDOMIZED
Intervention model: CROSSOVER
Primary purpose: OTHER

Brief summary: Oxidative stress and reactive oxygen species (ROS) can seriously affect cells, tissues and organs. The human body is capable of counteracting ROS production by stimulating antioxidant defense systems and consequently adapting to the oxidative challenge.

Several transcription factors are involved in the induction of antioxidant genes. Activators of nuclear factor derived from erythroid 2 (NRF2), a protein that controls the expression of certain genes, are considered agents capable of inducing antioxidant capacity and to alleviate ROS. There are some food bioactive compounds, including polyphenols, capable of activating NRF2.

Pterostilbene (PT) is a stilbenoid found in many natural sources, and is emerging as an antioxidant due to its potential preventive and therapeutic properties in a long list of diseases. Despite its apparent properties, the water solubility and bioavailability of PT are low.

The co-crystallization of nutraceuticals is a recent strategy based on crystal engineering to overcome their low solubility and, therefore, their low oral bioavailability. It has been identified and characterized a cocrystal of pterostilbene that can increase oral bioavailability in animals by up to 10 times compared to the commercial free base PT.

The main objective of the study is to evaluate the oral bioavailability of the crystallized form of pterostilbene (ccPT) compared to its commercial free base form (pterostilbene (PT).

The secondary objectives of the study are to determine the pharmacokinetic parameters:

* Relative oral bioavailability (Frel)
* Maximum concentration (Cmax).
* Maximum time (Tmax).
* Half life time (T1/2).

During the study there will be 3 visits: a preselection visit (V0), a visit for the first postprandial study (V1) and after one week washing period, a visit for the second postprandial study (V2).


Eligibility criteria: Inclusion Criteria:

* Men and women between 18 and 65 years of age.
* Sign the informed consent form.
* Know how to read, write and speak Spanish

Exclusion Criteria:

* Take supplements or multivitamin supplements or phytotherapeutic products (especially infusions) that interfere with the treatment under study up to 30 days before the start of the study.
* Be lacto-vegetarian, lacto-ovo-vegetarian, or vegan.
* Present intolerances and/or food allergies related to pterostilbene.
* Be a smoker.
* Having received antibiotic treatment up to 30 days before the start of the study.
* Present values of body mass index ≤ 18kg/m\^2 or ≥ 35 kg/m\^2.
* Present some chronic disease with clinical manifestations: coronary heart disease, cardiovascular disease, diabetes, celiac disease, Crohn's disease, chronic kidney disease, cancer, autoimmune diseases (such as fibromyalgia), respiratory and/or gastrointestinal diseases that may compromise the absorption of the compound.
* Clinical history of anemia.
* Being pregnant or intending to became pregnant.
* Be in breastfeeding period.
* Being unable to follow the study guidelines.
* Participate in or have participated in a clinical trial or nutritional intervention study in the last 30 days before inclusion in the study.

Primary outcomes:
measure: Bioavailability of Pterostilbene calculated by area under the curve (AUC 0-24) of plasma pterostilbene levels.
timeFrame: At week 1 and week 2
Secondary outcomes:
measure: Maximum plasma concentration (Cmax)
timeFrame: At week 1 and week 2
measure: Time for maximum plasma concentration (Tmax)
timeFrame: At week 1 and week 2
measure: Half-life (T1/2).
timeFrame: At week 1 and week 2
measure: Area Under the Curve (AUC 0-inf) of plasma pterostilbene levels.
timeFrame: At week 1 and week 2
measure: Relative oral bioavailability (Frel)
timeFrame: At week 1 and week 2
Other outcomes:
Locations:
city: Reus
country: Spain
facility: Eurecat
Study officials:
affiliation: UTNS (Eurecat_Reus)
name: Antoni Caimari, PhD
role: PRINCIPAL_INVESTIGATOR
References: