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

Autor: Tina Sartorius, Roland Wacker, Manfred Wilhelm, Christiane Schön, Tanita Dharsono, Katharina Knaub
Jazyk: angličtina
Rok vydání: 2019
Předmět:
Male
Cannabis sativa
Pharmaceutical Science
Administration
Oral
Pharmacology
030226 pharmacology & pharmacy
Analytical Chemistry
cannabidiol
0302 clinical medicine
Drug Delivery Systems
Oral administration
Drug Discovery
pharmacokinetic
oral drug delivery system
Analgesics
Cross-Over Studies
Fasting
Healthy Volunteers
surgical procedures
operative
Chemistry (miscellaneous)
Area Under Curve
Drug delivery
Lipophilicity
Molecular Medicine
CBD
Female
medicine.drug
Adult
Cmax
Biological Availability
Absorption (skin)
hemp extract
digestive system
Article
lcsh:QD241-441
03 medical and health sciences
Sex Factors
Pharmacokinetics
Double-Blind Method
lcsh:Organic chemistry
medicine
Humans
human
Physical and Theoretical Chemistry
business.industry
Organic Chemistry
digestive system diseases
Bioavailability
Anti-Anxiety Agents
Emulsifying Agents
SEDDS
business
bioavailability
Cannabidiol
030217 neurology & neurosurgery
Zdroj: Molecules, Vol 24, Iss 16, p 2967 (2019)
Molecules
Volume 24
Issue 16
ISSN: 1420-3049
Popis: 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&ndash
8h/AUC0&ndash
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.
Databáze: OpenAIRE
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