Using in vitro and in vivo models to evaluate the oral bioavailability of nutraceuticals

Yuwen Ting, Qin Zhao, Chunxin Xia, Qingrong Huang

Research output: Contribution to journalReview articlepeer-review

31 Scopus citations


Nutraceuticals are the bioactive compounds found in many dietary sources. Numerous publications have reported their ability to prevent the development of degenerative diseases through modulation of physiological and physiochemical processes in living systems. Having sufficient concentration at the target site of action is the most critical factor for nutraceuticals to deliver the health benefits. For consumers, it is commonly accepted to ingest these bioactive components through oral delivery route because it is convenient and cost-efficient and allows flexible dosing schedule. Thus, it is important to understand the oral bioavailability of nutraceuticals to evaluate their qualifications as disease preventive agents and to calculate the required ingestion dosages. To predict the oral bioavailability of nutraceuticals, many in vitro and in vivo models have been developed to reduce the need for frequent human pharmacokinetic studies, which are costly and time-consuming and involve ethical complications. These models evaluate one or more of the influential factors that contribute to the oral bioavailability and are efficient screening techniques with the potential of predicting the pharmacokinetic process in humans. To accurately predict human oral bioavailability, further research is required to develop not only a better correlation between the in vitro and in vivo models but also an accurate scaling factor that takes into account interspecies variations.

Original languageEnglish (US)
Pages (from-to)1332-1338
Number of pages7
JournalJournal of agricultural and food chemistry
Issue number5
StatePublished - Feb 11 2015

All Science Journal Classification (ASJC) codes

  • Chemistry(all)
  • Agricultural and Biological Sciences(all)


  • Caco-2
  • TIM-1
  • bioaccessibility
  • bioavailability
  • in vitro digestion
  • lipolysis
  • metabolism
  • nutraceutical
  • pharmacokinetics

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