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

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-emu...

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Autores principales: Knaub, Katharina, Sartorius, Tina, Dharsono, Tanita, Wacker, Roland, Wilhelm, Manfred, Schön, Christiane
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6720748/
https://www.ncbi.nlm.nih.gov/pubmed/31426272
http://dx.doi.org/10.3390/molecules24162967
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author Knaub, Katharina
Sartorius, Tina
Dharsono, Tanita
Wacker, Roland
Wilhelm, Manfred
Schön, Christiane
author_facet Knaub, Katharina
Sartorius, Tina
Dharsono, Tanita
Wacker, Roland
Wilhelm, Manfred
Schön, Christiane
author_sort Knaub, Katharina
collection PubMed
description 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 C(max) and a 2.85-/1.70-fold higher AUC(0–8h)/AUC(0–24h) compared to the reference formulation. T(max) 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 (C(max)), favorably enhanced bioavailability (AUC) and fast absorption (T(max)). No safety concerns were noted following either administration.
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spelling pubmed-67207482019-09-10 A Novel Self-Emulsifying Drug Delivery System (SEDDS) Based on VESIsorb(®) Formulation Technology Improving the Oral Bioavailability of Cannabidiol in Healthy Subjects Knaub, Katharina Sartorius, Tina Dharsono, Tanita Wacker, Roland Wilhelm, Manfred Schön, Christiane Molecules Article 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 C(max) and a 2.85-/1.70-fold higher AUC(0–8h)/AUC(0–24h) compared to the reference formulation. T(max) 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 (C(max)), favorably enhanced bioavailability (AUC) and fast absorption (T(max)). No safety concerns were noted following either administration. MDPI 2019-08-16 /pmc/articles/PMC6720748/ /pubmed/31426272 http://dx.doi.org/10.3390/molecules24162967 Text en © 2019 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Knaub, Katharina
Sartorius, Tina
Dharsono, Tanita
Wacker, Roland
Wilhelm, Manfred
Schön, Christiane
A Novel Self-Emulsifying Drug Delivery System (SEDDS) Based on VESIsorb(®) Formulation Technology Improving the Oral Bioavailability of Cannabidiol in Healthy Subjects
title A Novel Self-Emulsifying Drug Delivery System (SEDDS) Based on VESIsorb(®) Formulation Technology Improving the Oral Bioavailability of Cannabidiol in Healthy Subjects
title_full A Novel Self-Emulsifying Drug Delivery System (SEDDS) Based on VESIsorb(®) Formulation Technology Improving the Oral Bioavailability of Cannabidiol in Healthy Subjects
title_fullStr A Novel Self-Emulsifying Drug Delivery System (SEDDS) Based on VESIsorb(®) Formulation Technology Improving the Oral Bioavailability of Cannabidiol in Healthy Subjects
title_full_unstemmed A Novel Self-Emulsifying Drug Delivery System (SEDDS) Based on VESIsorb(®) Formulation Technology Improving the Oral Bioavailability of Cannabidiol in Healthy Subjects
title_short A Novel Self-Emulsifying Drug Delivery System (SEDDS) Based on VESIsorb(®) Formulation Technology Improving the Oral Bioavailability of Cannabidiol in Healthy Subjects
title_sort novel self-emulsifying drug delivery system (sedds) based on vesisorb(®) formulation technology improving the oral bioavailability of cannabidiol in healthy subjects
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6720748/
https://www.ncbi.nlm.nih.gov/pubmed/31426272
http://dx.doi.org/10.3390/molecules24162967
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