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Numerous studies have demonstrated the health-promoting benefits of resveratrol and its close derivatives in various aspects of disease prevention and management, yet due to their highly conjugated 1,2-diphenylethylene structural skeleton, the in vivo application of stilbenoids could be limited. Therefore, the metabolic profiles of these stilbene compounds warrant further attention and investigation. The bioavailability of a nutrient or a drug is significantly influenced by ADME (absorption, distribution, metabolism and excretion). In this review, we summarize the study results of drug metabolism and pharmacokinetics (DMPK) profiles of resveratrol and its close oligomeric derivatives, including oxyresveratrol, piceatannol, pterostilbene, rhaponticin, rhapontigenin and 2,3,5,4′-tetrahydroxystilbene-2-O-β-glucopyranoside (THSG). This review also addressees explored delivery strategies, such as stilbenoids-loaded nanoparticles or Pickering emulsions, to enhance their aqueous solubility, stability, and thus bioavailability.

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