Enhancing Cannabidiol Bioavailability: Development and Evaluation of an Amorphous Cannabidiol Powder Formulation.

Abstract

Despite the various beneficial properties of cannabidiol (CBD), such as antioxidant, anti-inflammatory, analgesic, antidepressant, and anxiolytic activities, its clinical utility is limited due to its notably low bioavailability (BA). To address this issue, we developed an amorphous CBD powder formulation using solvent shift method, which only uses materials approved for food-grade applications. In a pharmacokinetic study in male Sprague-Dawley rats, we orally administered 10 mg/kg of CBD isolate powder with a crystalline structure and our developed amorphous CBD powder formulation. The C_max values demonstrated a 3.9-fold increase for the amorphous CBD powder formulation containing polyvinylpyrrolidone (PVP) as a polymer (F3) and a 3.0-fold increase for the amorphous CBD powder formulation containing hydroxypropyl methylcellulose (HPMC) as a polymer (F4) compared to the CBD isolate powder. Furthermore, the AUC_0-6h values for F3 and F4 were 5.3- and 5.2-fold higher than those for CBD isolate powder, respectively, indicating a significant enhancement. The T_max values were also significantly shorter for F3 and F4, at 0.9±0.1 h and 0.8±0.1 h, respectively, compared to >6.0 h for CBD isolate powder. These findings demonstrate the superior BA of the amorphous CBD formulation. Based on these results, the amorphous CBD formulation is expected to be a highly absorbable CBD formulation, thereby advancing its use in food and supplements.