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

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

Cannabidiol (CBD), a phytocannabinoid compound of <i>Cannabis sativa</i>, 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 limitatio...

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Main Authors: Katharina Knaub, Tina Sartorius, Tanita Dharsono, Roland Wacker, Manfred Wilhelm, Christiane Schön
Format: Article
Language:English
Published: MDPI AG 2019-08-01
Series:Molecules
Subjects:
bioavailability
<i>Cannabis sativa</i>
cannabidiol
CBD
hemp extract
human
oral drug delivery system
pharmacokinetic
SEDDS
Online Access:https://www.mdpi.com/1420-3049/24/16/2967
id doaj-fa17261ecde94997879722eadebbb7e3
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spelling doaj-fa17261ecde94997879722eadebbb7e32020-11-25T01:12:22ZengMDPI AGMolecules1420-30492019-08-012416296710.3390/molecules24162967molecules24162967A Novel Self-Emulsifying Drug Delivery System (SEDDS) Based on VESIsorb<sup>®</sup> Formulation Technology Improving the Oral Bioavailability of Cannabidiol in Healthy SubjectsKatharina Knaub0Tina Sartorius1Tanita Dharsono2Roland Wacker3Manfred Wilhelm4Christiane Schön5BioTeSys GmbH, Schelztorstr. 54-56, 73728 Esslingen, GermanyBioTeSys GmbH, Schelztorstr. 54-56, 73728 Esslingen, GermanyBioTeSys GmbH, Schelztorstr. 54-56, 73728 Esslingen, GermanyBioTeSys GmbH, Schelztorstr. 54-56, 73728 Esslingen, GermanyNatural and Economic Sciences, Department of Mathematics, Ulm University of Applied Sciences, Albert-Einstein-Allee 55, 89081 Ulm, GermanyBioTeSys GmbH, Schelztorstr. 54-56, 73728 Esslingen, GermanyCannabidiol (CBD), a phytocannabinoid compound of <i>Cannabis sativa</i>, 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<sup>&#174;</sup> 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<sub>max</sub> and a 2.85-/1.70-fold higher AUC<sub>0&#8722;8h</sub>/AUC<sub>0&#8722;24h</sub> compared to the reference formulation. T<sub>max</sub> 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<sub>max</sub>), favorably enhanced bioavailability (AUC) and fast absorption (T<sub>max</sub>). No safety concerns were noted following either administration.https://www.mdpi.com/1420-3049/24/16/2967bioavailability<i>Cannabis sativa</i>cannabidiolCBDhemp extracthumanoral drug delivery systempharmacokineticSEDDS
collection DOAJ
language English
format Article
sources DOAJ
author Katharina Knaub
Tina Sartorius
Tanita Dharsono
Roland Wacker
Manfred Wilhelm
Christiane Schön
spellingShingle Katharina Knaub
Tina Sartorius
Tanita Dharsono
Roland Wacker
Manfred Wilhelm
Christiane Schön
A Novel Self-Emulsifying Drug Delivery System (SEDDS) Based on VESIsorb<sup>®</sup> Formulation Technology Improving the Oral Bioavailability of Cannabidiol in Healthy Subjects
Molecules
bioavailability
<i>Cannabis sativa</i>
cannabidiol
CBD
hemp extract
human
oral drug delivery system
pharmacokinetic
SEDDS
author_facet Katharina Knaub
Tina Sartorius
Tanita Dharsono
Roland Wacker
Manfred Wilhelm
Christiane Schön
author_sort Katharina Knaub
title A Novel Self-Emulsifying Drug Delivery System (SEDDS) Based on VESIsorb<sup>®</sup> Formulation Technology Improving the Oral Bioavailability of Cannabidiol in Healthy Subjects
title_short A Novel Self-Emulsifying Drug Delivery System (SEDDS) Based on VESIsorb<sup>®</sup> Formulation Technology Improving the Oral Bioavailability of Cannabidiol in Healthy Subjects
title_full A Novel Self-Emulsifying Drug Delivery System (SEDDS) Based on VESIsorb<sup>®</sup> Formulation Technology Improving the Oral Bioavailability of Cannabidiol in Healthy Subjects
title_fullStr A Novel Self-Emulsifying Drug Delivery System (SEDDS) Based on VESIsorb<sup>®</sup> 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<sup>®</sup> Formulation Technology Improving the Oral Bioavailability of Cannabidiol in Healthy Subjects
title_sort novel self-emulsifying drug delivery system (sedds) based on vesisorb<sup>®</sup> formulation technology improving the oral bioavailability of cannabidiol in healthy subjects
publisher MDPI AG
series Molecules
issn 1420-3049
publishDate 2019-08-01
description Cannabidiol (CBD), a phytocannabinoid compound of <i>Cannabis sativa</i>, 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<sup>&#174;</sup> 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<sub>max</sub> and a 2.85-/1.70-fold higher AUC<sub>0&#8722;8h</sub>/AUC<sub>0&#8722;24h</sub> compared to the reference formulation. T<sub>max</sub> 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<sub>max</sub>), favorably enhanced bioavailability (AUC) and fast absorption (T<sub>max</sub>). No safety concerns were noted following either administration.
topic bioavailability
<i>Cannabis sativa</i>
cannabidiol
CBD
hemp extract
human
oral drug delivery system
pharmacokinetic
SEDDS
url https://www.mdpi.com/1420-3049/24/16/2967
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