Improving the bioavailability of pterostilbene


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Nutraceutical ingredients are natural compounds, usually extracted and purified from both food and nonfood plants.1 In recent years, nutraceuticals have been experienced an increased interest because their presumed safety and potential therapeutic effects allow health claims as food supplements with a variety of health benefits for humans and animals.

Among the plethora of known nutraceutical compounds, pterostilbene stands out, a phytoalexin found in fruits such as grapes, deerberries, blueberries, peanuts and in wine.3,4 This remarkable nutrient has evidenced properties in the prevention and treatment of a long list of human diseases which include neurological, cardiovascular, metabolic and hematologic disorders due to its antioxidant, anti-inflammatory, and anticarcinogenic properties. Moreover, it has been demonstrated its potential application as a radioprotector to prevent and ameliorate the radiation-induced diseases.5However, the bioavailability of pterostilbene is limited due to its poor solubility in water. This is why we enrolled in a study with the challenge to increase the absorption of this important nutrient. And the objective was accomplished through the discovery of a novel cocrystal with picolinic acid, a naturally occurring derivative of the aminoacid tryptophan. The new pterostilbene/picolinic acid cocrystal shown a 10-fold increase in the oral bioavailability of pterostilbene compared with the commercial form, revealing a great potential to be one of the best oral solid formulations for pterostilbene in humans.6

Pharmacokinetic profiles of pterostilbene in rats following oral administration of pterostilbene and pterostilbene:picolinic acid cocrystal

  • 1. Functional Food Ingredients and Nutraceuticals Processing Technologies. John Shi, CRC Press, Second Edition, Broken Sound Parkwaty, NW, 2015. 
  • 2.  Nutraceuticals and Functional Foods in Human Health and Disease Prevention. Debasis Bagchi, Harry G. Preuss, Anand Swaroop, CRC Press, First Edition, Broken Sound Parkwaty, NW, 2015. 
  • 3. Roupe K. A., Remsberg, C. M., Yanez, J. A., Davies, N. M. Pharmacometrics of stilbenes: seguing towards the clinic. Curr. Clin. Pharmacol. 2006, 1, 81-101.
  • 4. Ruiz, M. J., Fernandez, M., Pico, Y., Manes, J. Dietary Administration of High Doses of Pterostilbene and Quercetin to Mice Is Not Toxic. J. Agric. Food Chem. 2009, 57, 3180-3186.
  • 5. Obrador, E., Salvador-Palmer, R., Pellicer, B., López-Blanch, R., Sirerol, J. A., Villaescusa, J. I., Montoro, A., Dellinger, R. W., Estrela, J. M. Combination of natural polyphenols with a precursor of NAD+ and a TLR2/6 ligand lipopeptide protects mice against lethal γ radiation. Journal of Advanced Research, 2022, In press.
  • 6. Bofill, L., Barbas, R., de Sande, D., Rafols, C., Albertí, J., Prohens, R. A novel, extremely bioavailable cocrystal of pterostilbene. Crystal Growth & Design 2021, 21, 2315-2323.

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