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Volume 30
Issue 13
10.3390/molecules30132676
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This is an early access version, the complete PDF, HTML, and XML versions will be available soon.
Article

Pharmacokinetics of Cannabidiol in Rat Brain Tissue After Single-Dose Administration of Different Formulations

by
Zuzana Binova
1,
Frantisek Benes
1,
Marie Zlechovcova
1,
Matej Maly
1,
Petr Kastanek
2,
Monika Cahova
3,
Milena Stranska
1 and
Jana Hajslova
1,*
1
Department of Food Analysis and Nutrition, University of Chemistry and Technology, Technická 3, 166 28 Prague, Czech Republic
2
Department of Biotechnology, University of Chemistry and Technology Prague, Technická 5, 166 28 Prague 6, Czech Republic
3
Institute for Clinical and Experimental Medicine, Vídeňská 1958, 140 21 Prague 4, Czech Republic
*
Author to whom correspondence should be addressed.
Molecules 2025, 30(13), 2676; https://doi.org/10.3390/molecules30132676
Submission received: 9 May 2025 / Revised: 15 June 2025 / Accepted: 19 June 2025 / Published: 20 June 2025
(This article belongs to the Special Issue Recent Advances in Cannabis and Hemp Research)
Versions Notes

Abstract

Cannabidiol (CBD), a phytocannabinoid commonly isolated from chemotype III Cannabis sativa plants, is known for its therapeutic potential. However, comprehensive information on its bioavailability is still lacking. The key objective of this study was to investigate the impact of specific formulations on CBD delivery to the site of action and, in particular, the brain of experimental animals. As brain tissue is an extremely complex matrix, a highly sensitive method employing liquid chromatography–tandem mass spectrometry (LC-MS/MS) had to be implemented. To make it applicable for multiple analytes, the method was validated for 17 other phytocannabinoids and selected metabolites. Using this method, a pharmacokinetic study was conducted on 200 brain samples collected from rats that had been administered various CBD formulations (carriers) via oral gavage. The peak concentration in brain occurred within 1–2 h; notably, the highest was reached with carriers containing triacylglycerols with the shortest fatty acid chains (caprylic/capric). In addition to the parent compound, 7-hydroxy-cannabidiol and 7-carboxy-cannabidiol were detected, confirming rapid post-administration metabolism. Overall, this research enhances understanding of CBD distribution in the brain and underscores the impact of specific formulations on its bioavailability, offering insights into optimizing CBD-based therapies to be both effective and ‘patient-friendly’.
Keywords: Cannabidiol; metabolites; brain tissue; bioavailability; LC-MS/MS Cannabidiol; metabolites; brain tissue; bioavailability; LC-MS/MS

Share and Cite

MDPI and ACS Style

Binova, Z.; Benes, F.; Zlechovcova, M.; Maly, M.; Kastanek, P.; Cahova, M.; Stranska, M.; Hajslova, J. Pharmacokinetics of Cannabidiol in Rat Brain Tissue After Single-Dose Administration of Different Formulations. Molecules 2025, 30, 2676. https://doi.org/10.3390/molecules30132676

AMA Style

Binova Z, Benes F, Zlechovcova M, Maly M, Kastanek P, Cahova M, Stranska M, Hajslova J. Pharmacokinetics of Cannabidiol in Rat Brain Tissue After Single-Dose Administration of Different Formulations. Molecules. 2025; 30(13):2676. https://doi.org/10.3390/molecules30132676

Chicago/Turabian Style

Binova, Zuzana, Frantisek Benes, Marie Zlechovcova, Matej Maly, Petr Kastanek, Monika Cahova, Milena Stranska, and Jana Hajslova. 2025. "Pharmacokinetics of Cannabidiol in Rat Brain Tissue After Single-Dose Administration of Different Formulations" Molecules 30, no. 13: 2676. https://doi.org/10.3390/molecules30132676

APA Style

Binova, Z., Benes, F., Zlechovcova, M., Maly, M., Kastanek, P., Cahova, M., Stranska, M., & Hajslova, J. (2025). Pharmacokinetics of Cannabidiol in Rat Brain Tissue After Single-Dose Administration of Different Formulations. Molecules, 30(13), 2676. https://doi.org/10.3390/molecules30132676

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