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Article

Enhanced Oral Bioavailability of β-Caryophyllene in Healthy Subjects Using the VESIsorb® Formulation Technology, a Novel Self-Emulsifying Drug Delivery System (SEDDS)

1
BioTeSys GmbH, Schelztorstraße 54-56, 73728 Esslingen, Germany
2
Interlabor Belp AG, Aemmenmattstrasse. 16, 3123 Belp, Switzerland
3
Osage Research and Development, 734 Cutter Ct., Kure Beach, NC 28449, USA
4
Division of Neurosurgery, Rochester Regional Health, Unity Hospital, 1555 Long Pond Rd., Rochester, NY 14626, USA
*
Author to whom correspondence should be addressed.
Academic Editor: Severina Pacifico
Molecules 2022, 27(9), 2860; https://doi.org/10.3390/molecules27092860
Received: 8 April 2022 / Revised: 28 April 2022 / Accepted: 28 April 2022 / Published: 30 April 2022
(This article belongs to the Special Issue Industrial Hemp Chemistry and Nutraceutical Perspectives)
β-Caryophyllene (BCP), a common constituent of many spice and food plants, is gaining increased attention due to recent research identifying numerous potential health benefits. Due to limited oral bioavailability observed in preclinical models, the described benefits of BCP may be maximized by using a suitable delivery system. Additionally, human pharmacokinetics (PK) remain unknown. This study evaluates the relative oral bioavailability of BCP formulated in a self-emulsifying drug delivery system (SEDDS) based on VESIsorb® formulation technology (BCP-SEDDS) compared to BCP neat oil. Hence, a randomized, double-blind, cross-over design, single oral dose study (100 mg BCP) in 24 healthy subjects (12 men/12 women) was performed under fasting conditions. Pharmacokinetic parameters were analyzed from individual concentration-time curves. The data show that BCP-SEDDS resulted in a 2.2/2.0-fold increase in AUC0–12h/AUC0–24h and a 3.6-fold increase in Cmax compared to BCP neat oil. Moreover, BCP was absorbed faster from BCP-SEDDS (Tmax: 1.43 h) compared to BCP neat oil (Tmax: 3.07 h). Gender analysis revealed that there is no significant difference between men and women for both the investigated formulations and all investigated PK endpoints. In conclusion, BCP-SEDDS offers a well-tolerated and effective oral delivery system to significantly enhance the oral bioavailability of BCP in humans. View Full-Text
Keywords: beta-caryophyllene (BCP); bioavailability; hemp; Cannabis sativa L.; human; oral drug delivery system; pharmacokinetic; SEDDS; VESIsorb® formulation technology; endocannabinoid system; nutraceuticals beta-caryophyllene (BCP); bioavailability; hemp; Cannabis sativa L.; human; oral drug delivery system; pharmacokinetic; SEDDS; VESIsorb® formulation technology; endocannabinoid system; nutraceuticals
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MDPI and ACS Style

Mödinger, Y.; Knaub, K.; Dharsono, T.; Wacker, R.; Meyrat, R.; Land, M.H.; Petraglia, A.L.; Schön, C. Enhanced Oral Bioavailability of β-Caryophyllene in Healthy Subjects Using the VESIsorb® Formulation Technology, a Novel Self-Emulsifying Drug Delivery System (SEDDS). Molecules 2022, 27, 2860. https://doi.org/10.3390/molecules27092860

AMA Style

Mödinger Y, Knaub K, Dharsono T, Wacker R, Meyrat R, Land MH, Petraglia AL, Schön C. Enhanced Oral Bioavailability of β-Caryophyllene in Healthy Subjects Using the VESIsorb® Formulation Technology, a Novel Self-Emulsifying Drug Delivery System (SEDDS). Molecules. 2022; 27(9):2860. https://doi.org/10.3390/molecules27092860

Chicago/Turabian Style

Mödinger, Yvonne, Katharina Knaub, Tanita Dharsono, Roland Wacker, Remo Meyrat, M. Hunter Land, Anthony L. Petraglia, and Christiane Schön. 2022. "Enhanced Oral Bioavailability of β-Caryophyllene in Healthy Subjects Using the VESIsorb® Formulation Technology, a Novel Self-Emulsifying Drug Delivery System (SEDDS)" Molecules 27, no. 9: 2860. https://doi.org/10.3390/molecules27092860

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