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Published on: February 8, 2017
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.
Abstract:
Cannabidiol (CBD) has demonstrated therapeutic potential in treating epilepsy, multiple sclerosis, Alzheimer's, Parkinson's, and Crohn's diseases. Despite its promising effects and analgesic, anti-inflammatory, and anxiolytic properties, oral CBD's full potential is hindered by poor water solubility (0.7-10 μg/mL), low permeability, and chemical instability. This study aimed to enhance CBD's dissolution, stability, and gastrointestinal (GI) permeability by forming a CBD-phospholipid complex (CBD-PLC). We hypothesised that CBD-PLC would enhance CBD's hydrophilicity, thus improving GI barrier permeability. This study involved screening an optimal phospholipid (PL) using a Design of Experiments (DoE) approach to prepare CBD-PLC with nanosized droplets (194.3 nm). Dissolution studies revealed significantly enhanced release rates for CBD-PLC-44.7% at 2 h and 67.1% at 3 h-compared to 0% for pure CBD and 7.2% for a physical mixture (PM). Cellular uptake studies showed that at 30 µM, CBD-PLC exhibited 32.7% higher apparent permeability coefficients (Papp), nearly doubling at 40 µM compared to pure CBD. Cytotoxicity tests confirmed safety over 24 h, while 12-month stability tests demonstrated consistent performance under varied conditions. The results indicate that CBD-PLC improves CBD's solubility, permeability, and stability, offering a promising strategy to address the limitations of oral CBD delivery systems.
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