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

    Yvonne Mödinger / Katharina Knaub / Tanita Dharsono / Roland Wacker / Remo Meyrat / M. Hunter Land / Anthony L. Petraglia / Christiane Schön

    Molecules, Vol 27, Iss 2860, p

    2022  Volume 2860

    Abstract: 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 ... ...

    Abstract 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 AUC 0–12h /AUC 0–24h and a 3.6-fold increase in C max compared to BCP neat oil. Moreover, BCP was absorbed faster from BCP-SEDDS (T max : 1.43 h) compared to BCP neat oil (T max : 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.
    Keywords beta-caryophyllene (BCP) ; bioavailability ; hemp ; Cannabis sativa L ; human ; oral drug delivery system ; Organic chemistry ; QD241-441
    Subject code 610
    Language English
    Publishing date 2022-04-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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

    Katharina Knaub / Tina Sartorius / Tanita Dharsono / Roland Wacker / Manfred Wilhelm / Christiane Schön

    Molecules, Vol 24, Iss 16, p

    2019  Volume 2967

    Abstract: 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. ...

    Abstract 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.
    Keywords bioavailability ; Cannabis sativa ; cannabidiol ; CBD ; hemp extract ; human ; oral drug delivery system ; pharmacokinetic ; SEDDS ; Organic chemistry ; QD241-441
    Language English
    Publishing date 2019-08-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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