One of the fundamental challenges of working with a plant oil extract like cannabidiol (CBD) is its natural lack of water solubility. It's one of the main biological barriers to its absorption into the bloodstream and across the blood-brain barrier. It also limits cannabidiol's potential applications as an ingredient, since in its unprocessed state it can only dissolve in solvents or other oils.
As a hemp-derived substance, it also contains humic acid, a substance found naturally in soil, which helps plants to grow by feeding the microbes around their roots. But when cannabidiol products retain trace amounts of humic acid, it reduces shelf life because of its potential to become a toxic contaminant. The food and pharma sectors have been racing to develop a truly water-soluble form of pure, pharmaceuticalgrade cannabidiol, as well as a shelf-stable version that preserves all its active ingredients.
Cannabidiol, says David Mouser, CEO of formulator and manufacturer at CBDPurUS, can be thought of as a 'fountain of health'. It's in demand for applications as varied as toothpaste, milk, deodorant and skin patches, in a wide range of delivery methods.
While there have still been few official studies into its pharma and medical applications, its target market includes people with mental health problems, chronic pain, mood disorders, arthritis, epilepsy and a long list of other health issues, including opioid addiction, the total cost of which hit $1 trillion in the US last year.
CBDPurUS is one of the oldest companies in the cannabidiol market, and getting in early has enabled it to expand from the US into the UK and Jamaica, with organic farms in the US and Asia, where it grows its own non-GMO cultivars.
It has achieved good manufacturing practice (GMP) certification in the US: an assurance that its products are consistently high in quality and contaminant-free, thus being safe for end-user consumption. Its star products are cannabidiol isolate in a crystallite powder form, which has been certified as pharma-grade - 99.96% pure - by the International Cannabidiol Organisation of Manufacturers and Research (ICOMR), and SDP46, a water-soluble version that can be added directly to food and beverages.
"We are the only reliable source of water-soluble CBD right now," says Mouser. "That's important, because water-soluble CBD will be used for 70% of CBD products by 2020."
Because SDP46 can be measured out with normal kitchen utensils and added to prepared drinks and food, interest from the consumer market is strong.
Pre-made edibles, vapes and drops have fixed delivery strength and a stipulated serving size in order to get the full effect, but with their own supply of a water-soluble, tasteless cannabidiol powder, consumers could choose how to take their supplement and adjust the dosage as needed.
When it was first launched, Mouser recalls, "We had so many people calling to buy the product, we had to set up a consumer-direct webpage. So we call people back and we use the revenue to enhance R&D."
The isolate itself dissolves only in solvents or oil, but it provides the source for the water-soluble SDP46. Both products also go through a patented process to completely remove humic acid: a concern that's top-of-mind for food, supplement and pharma manufacturers with an interest in CBD.
"Responsible companies now have an alternative to avoid potential liability, costly litigation and loss of market reputation regarding the inherent humic acid issues," a CBDPurUS spokesperson said in an official statement. "Humic acid makes a great fertiliser, but is an undesirable contaminant in a commercial product because it encourages growth and chemical changes."
Mouser adds: "CBDPurUS is the only company guaranteeing no product liability regarding shelf life."
This is especially relevant for beverages, since humic acid also reacts with chlorinated drinking water to produce toxic dihaloacetonitriles. The company's humic acid removal process, patented in 2016, involves adding a fourth extraction step to the manufacturing process, after which the liquid product is sprayed into a sealed chamber and dried to a powder with heated gas.
Each gram of the final product contains roughly 100mg of cannabidiol - any higher and the spray-dry process would have to involve solvents, which would reintroduce concerns of toxicity.
The number 46 in SDP46 refers to the bio-enhancers added to make the active ingredient easier for the human body to absorb. The pure isolate, Mouser says, is "like an antique car" and is difficult to combine with bio-enhancers. But a study commissioned by CBDPurUS and ICOMR released in March 2016 found a way to significantly improve the bioavailability of the isolate-derived SDP46 by using additives to bind together two types of cytochrome enzymes - CYP450 and CYP3A4 - that play a key role in metabolising cannabidiol.
Normally, CYP450 enzymes will destroy as much as 40% of a dose of cannabidiol before it reaches the bloodstream, but binding them to CYP3A4 enzymes neutralises the process. The consumer gets a higher dose of CBD at a faster rate, and SDP46 can penetrate the blood-brain barrier in eight minutes.
According to Richard Stallworth, the director of ICOMR, "Higher bioavailability can effectively reduce the amount of CBD necessary for each person to find the amount needed for their individual efficacy."
Achieving a high degree of purity along with solubility in water opened the way for the company to release its own formulated supplement product in November 2017. SeltzerFizz is a powdered drink mix containing SDP46 in the form of nanoparticles, encased in shells that dissolve within two minutes once in the bloodstream. There's a flavour choice of lemon-lime or strawberry lemonade, and the mix dissolves instantly in 6-8oz of water.
SeltzerFizz, which is sold direct to consumer, is targeted at children, the elderly, military veterans and people with motor control disabilities like Alzheimer's. The development process focused on finding a convenient and appealing delivery method for CBD, so Mouser and his team took their inspiration from Alka Seltzer's fizzy tablet system for aspirin. They eventually moved away from the tablet concept as it didn't work well with the existing SDP46 formula, but kept the effervescence.
The SeltzerFizz powder comes in 10 and 30mg sachets to make consumption as simple as possible, and as a bonus, the fizz enhances the speed of absorption so its effects are felt in five to ten minutes. The pre-measured packets also make it easy to tell how much cannabidiol has been consumed and adjust the dosage.
As cannabis and hemp regulations worldwide shift and change, and hemp products gain further ground in the ingredients world, breaking the water-solubility and shelfstability barriers heralds a significant widening of the opportunities for CBD. The SeltzerFizz product demonstrates the potential that truly water-soluble, shelf-stable, high-quality CBD has to reach new markets.
As a tasteless powdered additive, it's highly convenient for food manufacturers in a range of sectors and its opportunities in the world of edibles are significantly expanded.
With as-of-yet unresearched applications in health and wellness, cannabidiol has a bright future ahead in pharma, so it's vital that it comes in accessible, versatile formats that give patients and their carers plenty of options.