Strategies for enhancing the oral bioavailability of cannabinoids

Ayala Bar-Hai, Abraham J. Domb, Amnon Hoffman*

*Corresponding author for this work

Research output: Contribution to journalReview articlepeer-review

5 Scopus citations

Abstract

Introduction: Oral administration of cannabinoids is a convenient route of administration in many cases. To enhance the poor and variable bioavailability of cannabinoids, selected strategies utilizing proper delivery systems have been designed. Low solubility in the GI aqueous media is the first and most critical barrier. Thereafter, cannabinoids can reach the systemic blood circulation via the portal vein that is associated with significant hepatic first pass metabolism (FPM) or bypass it via lymphatic absorption. Areas covered: The solubility obstacle of cannabinoids is mainly addressed with lipid-based formulations such as self-nanoemulsifying drug delivery systems (SNEDDS). Certain lipids are used to overcome the solubility issue. Surfactants and other additives in the formulation have additional impact on several barriers, including dictating the degree of lymphatic bioavailability and hepatic FPM. Gastro-retentive formulation is also plausible. Expert opinion: Comparison of the role of the same SNEDDS formulation, cyclosporine vs. cannabinoids, when used to elevate the oral bioavailability of different compounds, is presented. It illustrates some similarities and major mechanistic differences obtained by the same SNEDDS. Thus, the different influence over the absorption pathway illuminates the importance of understanding the absorption mechanism and its barriers to properly select appropriate strategies to achieve enhanced oral bioavailability.

Original languageAmerican English
Pages (from-to)313-322
Number of pages10
JournalExpert Opinion on Drug Metabolism and Toxicology
Volume18
Issue number5
DOIs
StatePublished - May 2022

Bibliographical note

Publisher Copyright:
© 2022 Informa UK Limited, trading as Taylor & Francis Group.

Keywords

  • Absorption enhancer
  • CBD
  • LBDDS
  • SNEDDS
  • THC
  • bioavailability
  • cannabinoids
  • chylomicrons
  • cyclosporine
  • first pass metabolism
  • lymphatic absorption
  • piperine

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