Oral Bioavailability of Pterostilbene Cocrystal Compared to Its Free Form (BIOPTERO)

NCT05561075 | Completed

• 1 other identifier: BIOPTERO
• Study Type: interventional
• Target: 6
• Locations: 1 country
• Sites: 1

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).

Conditions

Biological Availability

Keywords

Polyphenols; Antioxidant activity; Co-crystallization; Pterostilbene

Outcome Measures

Primary Outcomes (1)

• Bioavailability of Pterostilbene calculated by area under the curve (AUC 0-24) of plasma pterostilbene levels.

  Fasting pterostilbene levels in plasma will be determined before consume the capsule with pterostilbene until 24 hours postprandially at 8 points after consuming the capsule (0.5 hours, 1 hours, 2 hours, 3 hours, 4 hours, 6 hours, 8 hours and 24 hours).

  At week 1 and week 2

Secondary Outcomes (5)

• Maximum plasma concentration (Cmax)

  At week 1 and week 2

• Time for maximum plasma concentration (Tmax)

  At week 1 and week 2

• Half-life (T1/2).

  At week 1 and week 2

• Area Under the Curve (AUC 0-inf) of plasma pterostilbene levels.

  At week 1 and week 2

• Relative oral bioavailability (Frel)

  At week 1 and week 2

Study Arms (2)

Pterostilbene cocrystal

EXPERIMENTAL

Dietary Supplement: Pterostilbene cocrystal

Pterostilbene free form

ACTIVE COMPARATOR

Dietary Supplement: Pterostilbene free form

Interventions

Pterostilbene cocrystal DIETARY_SUPPLEMENT

One capsule with Pterostilbene cocrystal

Pterostilbene cocrystal

Pterostilbene free form DIETARY_SUPPLEMENT

One capsule with Pterostilbene free form

Pterostilbene free form

Eligibility Criteria

• Age: 18 Years - 65 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

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

You may not qualify if:

• 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.

Sponsors & Collaborators

• Fundació Eurecat: lead
• Circe, S.L.: collaborator

Study Sites (1)

Eurecat

Reus, 43204, Spain

Location

Related Links

• Technological Centre of Nutrition and Health. Eurecat\_Reus.

Study Officials

• Antoni Caimari, PhD

  UTNS (Eurecat_Reus)

  PRINCIPAL INVESTIGATOR

Study Design

• Study Type: interventional
• Phase: not applicable
• Allocation: RANDOMIZED
• Masking: QUADRUPLE
• Who Masked: PARTICIPANT, CARE PROVIDER, INVESTIGATOR, OUTCOMES ASSESSOR
• Purpose: OTHER
• Intervention Model: CROSSOVER
• Sponsor Type: OTHER
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: September 27, 2022
• First Posted: September 30, 2022
• Study Start: October 20, 2022
• Primary Completion: November 17, 2022
• Study Completion: November 17, 2022
• Last Updated: March 16, 2023

Record last verified: 2023-03

Data Sharing

• IPD Sharing: Will not share

Locations

ES (1)