Lipid-based formulations to increase cannabidiol bioavailability: In vitro digestion tests, pre-clinical assessment and clinical trial.

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.

Assessment of In Vitro Biological Activities of Anthocyanins-Rich Plant Species Based on Plinia cauliflora Study Model.

Plinia cauliflora (jaboticaba) is a native fruit tree from Brazilian rainforest widely used in popular medicine to prevent diarrhea, asthma, and infections. Studies have shown that the major therapeutic potential of jaboticaba fruits is on its peel, a rich source of anthocyanins. These secondary metabolites have well-known antioxidant and anti-inflammatory activities and have been claimed to be effective to treat diabetes, cancer, cardiovascular diseases, and stroke. This chapter describes a series of methodologies to evaluate important in vitro biological activities like cytotoxicity, proliferation, and migration of a hydroalcoholic extract of jaboticaba peel on mouse fibroblast L929 line. Assays to assess total phenolic, flavonoid, and anthocyanin contents and antioxidant activities are described as well.