Natural sesame oil is superior to pre-digested lipid formulations and purified triglycerides in promoting the intestinal lymphatic transport and systemic bioavailability of cannabidiol

Eur J Pharm Biopharm. 2021 May:162:43-49. doi: 10.1016/j.ejpb.2021.02.013. Epub 2021 Mar 5.

Abstract

Lipid-based formulations play a significant role in oral delivery of lipophilic drugs. Previous studies have shown that natural sesame oil promotes the intestinal lymphatic transport and oral bioavailability of the highly lipophilic drug cannabidiol (CBD). However, both lymphatic transport and systemic bioavailability were also associated with considerable variability. The aim of this study was to test the hypothesis that pre-digested lipid formulations (oleic acid, linoleic acid, oleic acid with 2-oleoylglycerol, oleic acid with 2-oleoylglycerol and oleic acid with glycerol) could reduce variability and increase the extent of the intestinal lymphatic transport and oral bioavailability of CBD. The in vivo studies in rats showed that pre-digested or purified triglyceride did not improve the lymphatic transport and bioavailability of CBD in comparison to sesame oil. Moreover, the results suggest that both the absorption of lipids and the absorption of co-administered CBD were more efficient following administration of natural sesame oil vehicle compared with pre-digested lipids or purified trioleate. Although multiple small molecule constituents and unique fatty acid compositions could potentially contribute to a better performance of sesame oil in oral absorption of lipids or CBD, further investigation will be needed to identify the mechanisms involved.

Keywords: Cannabidiol; Intestinal lymphatic transport; Lipid-based formulation; Natural sesame oil.

Publication types

  • Comparative Study

MeSH terms

  • Administration, Oral
  • Animals
  • Area Under Curve
  • Biological Availability
  • Cannabidiol / administration & dosage
  • Cannabidiol / chemistry
  • Cannabidiol / pharmacokinetics*
  • Drug Compounding / methods*
  • Excipients / chemistry*
  • Intestinal Absorption*
  • Intestinal Mucosa / metabolism
  • Linoleic Acid / chemistry
  • Lymphatic Vessels / metabolism
  • Male
  • Models, Animal
  • Oleic Acid / chemistry
  • Rats
  • Sesame Oil / chemistry*
  • Tissue Distribution
  • Triolein / chemistry

Substances

  • Excipients
  • Triolein
  • Cannabidiol
  • Oleic Acid
  • Sesame Oil
  • Linoleic Acid