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Updated: Oct 17, 2025

Self-Nanoemulsification of Healthy Oils to Enhance the Solubility of Lipophilic Drugs
Published on: July 27, 2022
Lipid-based formulations to increase cannabidiol bioavailability: In vitro digestion tests, pre-clinical assessment
Manuel A A De Prá1, Renata Vardanega1, Carla G Loss1
1Entourage Phytolab, R. Tabapuã 111, 04533-010 São Paulo, SP, Brazil.
Abstract:
Herein, medium-chain triglycerides (MCT), glyceryl monolinoleate (GML), and a self-emulsifying drug delivery system (SEDDS) for cannabidiol (CBD) delivery were compared using in vitro and in vivo (mouse and human) studies. In vitro digestion tests showed that SEDDS yielded the highest CBD recovery in the aqueous phase (86 ± 2%), followed by GML (13 ± 2%) and MCT (5.6% ± 0.8%). In vivo tests (mouse) revealed that SEDDS promoted the highest CBD exposure, exhibiting an area under the plasma concentration-time curve (AUC0-6h) 1.48 times greater than GML and 3.97 times greater than that of the MCT formulation. A single-dose, open-label, crossover study performed in 11 volunteers showed that SEDDS increased CBD AUC0-12h by 1.12 and 1.48 times in relation to GML and MCT, respectively. The in vitro-in vivo correlation was r2 0.75 for mice and r2 0.66 for humans. The AUC correlation between mice and humans was 0.98. Collectively, these results indicate that the lipid profile substantially influences CBD delivery and highlights the potential of the SEDDS and GML formulations as candidate solutions for increasing CBD AUC and bioavailability.
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