Development and Characterization of Cannabidiol Self-Emulsifying Drug Delivery System: In Vitro and In Vivo...

Area of Science:

• Pharmacology
• Drug Delivery Systems
• Biopharmaceutics

Background:

• Cannabidiol (CBD) exhibits significant therapeutic potential but suffers from poor oral bioavailability.
• Low aqueous solubility and extensive first-pass metabolism limit CBD's efficacy.
• Food intake variability further complicates CBD absorption and dosing.

Purpose of the Study:

• To develop a self-emulsifying drug delivery system (SEDDS) for enhanced aqueous solubility and oral bioavailability of CBD.
• To identify optimal excipient concentrations for stable CBD formulation under various physiological conditions.
• To evaluate the in vivo performance of promising SEDDS formulations.

Main Methods:

• Formulation of CBD-loaded SEDDS using Caproyl® 90, Tween® 20, and Transcutol® HP.
• Characterization of particle size and in vitro drug release kinetics.
• Assessment of formulation stability under simulated gastrointestinal conditions.
• In vivo pharmacokinetic studies to determine oral bioavailability.

Main Results:

• SEDDS formulations with specific Caproyl® 90 and Tween® 20 ratios yielded nanoparticles below 200 nm.
• High Tween® 20 concentrations (≥65% w/w) achieved over 90% in vitro CBD release.
• Selected formulations (CTT1, CTT4, CTT8) demonstrated stability and maintained CBD solubility post-digestion.
• In vivo studies revealed CTT4 achieved 2.4-fold higher bioavailability compared to CTT8.

Conclusions:

• SEDDS is a viable strategy to overcome the bioavailability challenges of CBD.
• Optimizing surfactant concentration is crucial for enhancing CBD absorption.
• The developed SEDDS formulations show promise for improving oral delivery of cannabidiol.