Cannabidiol (CBD) has been shown to have numerous medical benefits. However, it is highly lipophilic, with oral bioavailability of only 6% in the human body. One way to improve its bioavailability is by entrapment of CBD molecules inside various nano-scale clusters of lipids to provide sustainable solubility in water, thereby increasing bio-accessibility. In this study, we developed a novel solid lipid nanoparticle (SLN) preparation of CBD and studied its stability, shelf life, and entrapment efficiency. SLNs are essentially colloids of nanoparticles constituted by lipids in a solid phase at room temperature, hence the name solid lipid. Lipids with melting points near the melting point of CBD, low toxicity, and effective interaction with CBD are ideal candidates for synthesizing SLNs. Candidates of different lipids, surfactants, and compositions were tested under different homogenization rates and synthesis temperatures. It was found that a synthesis temperature of 70°C under a high-pressure homogenization (HPH) rate of 10’000rpm (for 15 minutes), followed by 10 minutes of ultrasonication, provided an ideal standard preparation procedure. After several trial-and-error of different formulations, the CBD, Witepsol W35, Span 80, sodium lauryl sulfate (SLS), Poloxamer (P188) at the relative weights of 100, 400, 170, 15.5, and 15.5 in water showed to have the highest shelf life (at least four months). Based on the particle surface charge (zeta potential values), it was found that including SLS in the formulation has the highest contribution to surface charge, thereby higher stability. The optimized formulation is the first reported CBD-loaded SLN offering 24% in-vitro release with an entrapment efficiency of 86±4.8%. Overall, SLNs were found to be promising solutions for increasing of bioavailability of CBD as a medical commodity.

Development of solid lipid nanoparticles of cannabidiol (CBD): A brief survey of formulation ingredients

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ACS Fall 2022

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