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Open AccessArticle

A Novel Self-Emulsifying Drug Delivery System (SEDDS) Based on VESIsorb® Formulation Technology Improving the Oral Bioavailability of Cannabidiol in Healthy Subjects

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BioTeSys GmbH, Schelztorstr. 54-56, 73728 Esslingen, Germany
2
Natural and Economic Sciences, Department of Mathematics, Ulm University of Applied Sciences, Albert-Einstein-Allee 55, 89081 Ulm, Germany
*
Author to whom correspondence should be addressed.
Molecules 2019, 24(16), 2967; https://doi.org/10.3390/molecules24162967
Received: 18 July 2019 / Revised: 12 August 2019 / Accepted: 13 August 2019 / Published: 16 August 2019
Cannabidiol (CBD), a phytocannabinoid compound of Cannabis sativa, shows limited oral bioavailability due to its lipophilicity and extensive first-pass metabolism. CBD is also known for its high intra- and inter-subject absorption variability in humans. To overcome these limitations a novel self-emulsifying drug delivery system (SEDDS) based on VESIsorb® formulation technology incorporating CBD, as Hemp-Extract, was developed (SEDDS-CBD). The study objective was to evaluate the pharmacokinetic profile of SEDDS-CBD in a randomized, double-blind, cross-over design in 16 healthy volunteers under fasted conditions. As reference formulation, the same Hemp-Extract diluted with medium-chain triglycerides (MCT-CBD) was used. CBD dose was standardized to 25 mg. Pharmacokinetic parameters were analyzed from individual concentration-time curves. Single oral administration of SEDDS-CBD led to a 4.4-fold higher Cmax and a 2.85-/1.70-fold higher AUC0–8h/AUC0–24h compared to the reference formulation. Tmax was substantially shorter for SEDDS-CBD (1.0 h) compared to MCT-CBD (3.0 h). Subgroup analysis demonstrated a higher bioavailability in women compared to men. This difference was seen for MCT-CBD while SEDDS-CBD mitigated this gender effect. Overall, SEDDS-CBD showed a significant improvement for all determined pharmacokinetic parameters: increased CBD plasma values (Cmax), favorably enhanced bioavailability (AUC) and fast absorption (Tmax). No safety concerns were noted following either administration. View Full-Text
Keywords: bioavailability; Cannabis sativa; cannabidiol; CBD; hemp extract; human; oral drug delivery system; pharmacokinetic; SEDDS bioavailability; Cannabis sativa; cannabidiol; CBD; hemp extract; human; oral drug delivery system; pharmacokinetic; SEDDS
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MDPI and ACS Style

Knaub, K.; Sartorius, T.; Dharsono, T.; Wacker, R.; Wilhelm, M.; Schön, C. A Novel Self-Emulsifying Drug Delivery System (SEDDS) Based on VESIsorb® Formulation Technology Improving the Oral Bioavailability of Cannabidiol in Healthy Subjects. Molecules 2019, 24, 2967.

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