Optimization of trans-Resveratrol bioavailability for human therapy.

Area of Science:

• Pharmacology
• Drug Delivery
• Nutraceuticals

Background:

• Trans-Resveratrol (t-Res) exhibits low oral bioavailability when administered as a dry powder.
• Developing advanced formulations is crucial to enhance t-Res absorption and therapeutic potential.

Purpose of the Study:

• To evaluate the pharmacokinetics, bioavailability, and biological effects of an innovative soluble galenic formulation of t-Res.
• To compare the efficacy and safety of the soluble t-Res formulation against its dry powder form in human volunteers and rodent models.

Main Methods:

• A crossover study in 15 healthy volunteers comparing 40 mg of soluble t-Res (caplets) versus dry powder t-Res (capsules).
• Plasma t-Res concentrations and metabolites analyzed via liquid chromatography-mass spectrometry over 5 hours.
• Assessment of anti-inflammatory effects in mice fed a high-fat diet.

Main Results:

• The soluble t-Res formulation resulted in 8.8-fold higher plasma t-Res levels compared to the dry powder.
• Biologically relevant plasma concentrations (0.1-6 μM) were sustained for several hours with the soluble form.
• The soluble formulation demonstrated robust anti-inflammatory effects in mice, while the dry powder was largely inactive.

Conclusions:

• The soluble galenic formulation significantly improves t-Res bioavailability, efficiency, and anti-inflammatory activity.
• This novel formulation facilitates t-Res human therapy by enhancing absorption and potentially reducing required doses, with no observed toxicity.
• The soluble form overcomes the limitations of dry powder t-Res, paving the way for broader therapeutic applications.