Cannabidiol (CBD) is the second most dominant cannabinoid derived from the cannabis sativa plant, after tetrahydrocannabinol (THC). Innovation in the CBD drug development space is gaining worldwide momentum due to increasing scientific data demonstrating the molecule’s promising therapeutic potential in human health. Because of ongoing clinical research, CBD is being considered as a possible treatment in a number of therapy areas, including central nervous system (CNS) diseases1, pain disorders2, cancer3 and more. However, while there is a remarkable opportunity for the development of CBD-based therapies in the aforementioned areas, there are still significant barriers to overcome in relation to the ingredient’s formulation.
CBD has low oral bioavailability, due to the molecule’s lipophilic nature and limited solubility, only 6% of the drug is absorbed into the circulation after oral administration.4 Therefore, to achieve a positive therapeutic outcome, higher doses of the active pharmaceutical ingredient (API) are required – which could bring unwanted problems. DSM is keen to address ways to optimize bioavailability and innovate the market with enhanced CBD-based therapies. As part of this work, DSM has benchmarked formulation technologies against each other to uncover the optimal balance between physico-chemical properties, pharmacokinetic performance and patient compliance. Click on the button below to keep reading our exclusive learnings.
1. Ożarowski, M., Karpiński, T. M., Zielińska, A., Souto, E. B., & Wielgus, K. Cannabidiol in Neurological and Neoplastic Diseases: Latest Developments on the Molecular Mechanism of Action. International journal of molecular sciences, 22(9), 4294 (2021).
2. Argueta, D. A., Ventura, C. M., Kiven, S., Sagi, V., & Gupta, K. A Balanced Approach for Cannabidiol Use in Chronic Pain. Frontiers in pharmacology, 11, 561 (2020).
3. O'Brien K. Cannabidiol (CBD) in Cancer Management. Cancers, 14(4), 885 (2022).
4. Perucca & Bialer. Critical aspects affecting cannabidiol oral bioavailability and metabolic elimination, and related clinical implications. Cannabinoids in Neurology and Psychiatry, vol. 34, pg. 795-800, (2020).
5. Perucca & Bialer. Critical aspects affecting cannabidiol oral bioavailability and metabolic elimination, and related clinical implications. Cannabinoids in Neurology and Psychiatry, vol. 34, pg. 795-800, (2020).
Low and variable bio-accessibility of CBD presents formulation challenges for the pharmaceutical industry. DSM is exploring drug delivery technologies to increase the molecule's pharmacokinetic profile. In-vitro studies reveal a strong correlation between bio-accessibility, physical state, stability, solubility, and particle size. Ongoing in-vivo work investigates excipients and formulation technology to identify candidates for clinical validation and product development. Learn how new research expands on the therapeutic benefits of CBD for the pharmaceutical industry.