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Optimising Cannabidiol Delivery: Improving Water Solubility and Permeability Through Phospholipid Complexation.
Thabata Muta1, Riya Khetan1, Yunmei Song1
1Centre for Pharmaceutical Innovation (CPI), Clinical & Health Science, University of South Australia, Adelaide, SA 5000, Australia.
International Journal of Molecular Sciences
|March 27, 2025
Summary
This study developed a cannabidiol-phospholipid complex (CBD-PLC) to overcome poor oral delivery. CBD-PLC significantly enhances CBD
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Biochemistry
Background:
- Cannabidiol (CBD) shows therapeutic promise for various conditions, including neurological and inflammatory diseases.
- Oral administration of CBD is limited by poor water solubility, low permeability, and chemical instability.
- Existing delivery systems struggle to fully exploit CBD's therapeutic potential due to these physicochemical barriers.
Purpose of the Study:
- To enhance the dissolution, chemical stability, and gastrointestinal (GI) permeability of cannabidiol (CBD).
- To develop a novel CBD-phospholipid complex (CBD-PLC) to improve oral delivery.
- To investigate the potential of CBD-PLC in overcoming the limitations of conventional CBD formulations.
Main Methods:
- Utilized a Design of Experiments (DoE) approach to screen and identify an optimal phospholipid (PL).
- Prepared CBD-phospholipid complex (CBD-PLC) with optimized nanosized droplets (194.3 nm).
- Conducted dissolution, cellular uptake (permeability), cytotoxicity, and stability studies to evaluate CBD-PLC performance.
Main Results:
- CBD-PLC demonstrated significantly enhanced dissolution rates compared to pure CBD and physical mixtures.
- Cellular uptake studies showed markedly increased apparent permeability coefficients (Papp) for CBD-PLC.
- CBD-PLC exhibited excellent safety profiles in cytotoxicity tests and maintained consistent performance over 12 months.
Conclusions:
- The developed CBD-phospholipid complex (CBD-PLC) effectively improves CBD's solubility, permeability, and stability.
- CBD-PLC represents a promising strategy to enhance oral cannabidiol delivery systems.
- This approach addresses key limitations, paving the way for more effective therapeutic applications of CBD.
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