Abstract
BackgroundThis study describes the design, optimization, and stress-testing of a novel phytocannabinoid nanoemulsion generated using high-pressure homogenization. text {QNaturale}^{circledR }, a plant-derived commercial emulsifier containing quillaja saponin, was used to stabilize the lipid phase droplets in water. Stress-testing was performed on this nanoemulsion in order to evaluate its chemical and colloidal stability under the influence of different environmental factors, encompassing both physical and chemical stressors.MethodsExtensive optimization studies were conducted to arrive at an ideal nanoemulsion formulation. A coarse emulsion containing 16.6 wt% CBD-enriched cannabis distillate and 83.4 wt% carrier (soybean) oil dispersed in 10 wt% text {QNaturale}^{circledR } (1.5 wt% quillaja saponin) solution after 10 homogenization cycles at a pressure of 30,000 psi produced a stable nanoemulsion. This nanoemulsion was then subjected to the stress studies.ResultsThe optimized nanoemulsion had an average droplet diameter of ca. 120 nm and average droplet surface ζ potentials of ca. -30 mV. It was imaged and characterized by a variety of protocols. It proved to be stable to droplet agglomeration and phase separation upon storage under ambient conditions for 6 weeks, as well as under a variety of physical stressors such as heat, cold, dilution, and carbonation. pH values ≤2 and moderately high salt concentrations (> 100 mM), however, destabilized the nanoemulsion, eventually leading to phase separation. Cannabis potency, determined by HPLC, was detrimentally affected by any changes in the nanoemulsion phase stability.ConclusionsQuillaja saponin stabilized cannabidiol(CBD)-enriched nanoemulsions are stable, robust systems even at low emulsifier concentrations, and are therefore significant from both a scientific as well as a commercial perspective.
Highlights
This study describes the design, optimization, and stress-testing of a novel phytocannabinoid nanoemulsion generated using high-pressure homogenization
For the High-performance liquid chromatography (HPLC) analysis, 1 mg/mL stock solution of each of the following cannabinoids was obtained from Cerilliant: cannabidiolic acid (CBD-A), tetrahydrocannabinolic acid (THC-A), cannabidiol (CBD), cannabigerolic acid (CBG-A), cannabigerol (CBG), cannabichromene (CBC), cannabinol (CBN), and delta-9 tetrahydrocannabinol (THC)
It is to be noted that the droplet sizes recorded by us matches well with the values recorded by Leibtag et al for their olive oil/CBD/quillaja saponin nanoemulsion produced by a sonication method, indicating a lower bound for quillaja saponin stabilized CBD/carrier oil droplets in the aqueous phase of a nanoemulsion, regardless of the emulsion preparation method or carrier oil type (Leibtag and Peshkovsky 2020)
Summary
This study describes the design, optimization, and stress-testing of a novel phytocannabinoid nanoemulsion generated using high-pressure homogenization. As the therapeutic benefits of cannabis become scientifically established, and the use of nutraceutical and recreational cannabis products is decriminalized in countries such as Argentina, Belgium, Georgia, Uruguay, South. Cannabis is a highly complex mixture, consisting of over 120 phytocannabinoids with related chemical structures, along with a variety of terpenes and flavonoids (Turner et al 2017). As many of these natural products interact with the central nervous system (CNS) receptors (Zou and Kumar 2018), cannabis could prove to be an exceedingly promising source for pharmacophore discovery. Other promising biological effects of cannabinoids include antiobesity and antidiabetic effects of tetrahydrocannabivarin (THCV) (Abioye et al 2020) and in developing fluorideand alcohol-free anti-bacterial mouthwash and oral care products (Vasudevan and Stahl 2020)
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