NanoSphere Health Sciences CSO Dr. Richard Kaufman shares his insight on the role of nanotechnology in next-generation drug-delivery methods.
Dr. Richard Kaufman, chief scientific officer for NanoSphere Health Sciences (CSE:NSHS), has developed patented nanoparticle delivery systems that have set him apart as a leader in the medical technology world.
Nanotechnology has the potential to disrupt the medical cannabis industry by providing a solution to poor bioavailability of cannabinoids in the bloodstream via traditional pathways. The technology also has significant potential for applications across a range of sectors, including nutraceuticals, vitamins, NSAIDs, cosmeceuticals and pet care.
Investing News Network: Please explain how cannabinoids are well suited for addressing pain and inflammation in the human body.
NanoSphere Health Chief Scientific Officer Dr. Richard Kaufman: Cannabinoids, primarily THC and CBD, suppress pain through multiple mechanisms that involve both the CB1 and the CB2 cannabinoid receptors located in the peripheral tissues of the spinal area and the brain. In the brain stem and the thalamus there are a lot of CB1 receptors that are keyed mostly for THC and they will block the perception of pain. The cannabinoids working through these CBD receptors can reduce inflammation as well as hyperallergic effects where you have too much response to pain.
But also, the THC, which I consider the heavy carrier for pain relief, works through sensory nerves that are able to decrease the pain signals that would go to the spinal cord and the brain where you interpret pain. So when you take THC in the right delivery system to reach these areas, it can suppress the pain signal processes, called the GABAergic process.
There’s also some other secondary mechanisms involving the pro-inflammatory processes as well as the opium beta endorphin receptors. Terpenes, the essential oils found in the trichromes of the cannabis plant, are also very analgesic and very anti-inflammatory on their own accord. So the cannabinoids suppress the transmission and interpretation of pain in a way that can oftentimes provide an alternative, for example, to opioids, which have a lot of addictive risks and adverse effects.
INN: Poor bio-availability of cannabinoids in the bloodstream via traditional pathways, including oral ingestion, has posed a challenge for the mainstream adoption of the use of this compound in medical treatment. Could you please explain the factors that can influence the bio-availability of cannabinoids in the bloodstream?
RK: The first factor is a matter of delivery. Cannabinoids are lipophilic — they have a decent molecular size, and they are fond of fats but are not water soluble. Depending on the route, you have different levels of absorption into the bloodstream. Bear in mind that absorption in the bloodstream is not a signal of how much actually gets to the receptors of the CB1 and the CB2 receptors of the endocannabinoid system. For example, when you have ingested cannabinoids, there’s a lot of pre-systemic metabolism. First THC will form a highly psychotropic effect through first pass in the liver, and there is a long delay of reaching the bloodstream.
Along the way, you also have the factor that when any of the cannabinoids reach the bloodstream, they tend to be absorbed merely into the fat cells. People that are regular users have more cannabinoids from past use and can show higher levels of bio-availability in the bloodstream. If you have native users as test subjects in a pharmacokinetics study, you may not get the same results vs. regular users. When you smoke cannabis, depending on how you smoke it, your inhalation and side-stream smoke could cause a variation in cannabinoid delivery ranging from 2 to 56 percent.
INN: Please explain to our investor audience the science behind nanotechnology delivery systems and your role in developing this technology.
RK: At NanoSphere, we want to be precise. We’ve developed precision methods of delivering the cannabinoids into the bloodstream. We performed a pharmacokinetics study in which we delivered the cannabinoids of THC between the cheek and the gum, known as buccal delivery. We found that we were getting an estimated 25 to 30 percent delivery of the THC into the bloodstream. We’re also pioneering transdermal delivery where we can deliver cannabinoids directly through the skin, avoiding the GI tract and the lag time while also increasing a higher level of overall regular absorption.
There are a number of factors in the current use of cannabis that block its most bio-available form from reaching the bloodstream and also prevent you from knowing how much you get into the bloodstream for whatever dose you’re taking. Our goal is to prevent this and always deliver precision metered dosages through different routes of delivery, which include going through the nose and directly to the brain — we call it intranasal. Transdermally, the delivery route is from the skin surface to the blood vessels where it goes into the bloodstream, and also between the cheek and the gum, and we have patents on this process involving nanoparticles and we’re very proud to be a leader in this area.
INN: How is nanotechnology changing the landscape for the medical use of cannabinoids? What are the potential treatment indications for cannabinoid-based nanotechnology?
RK: Cannabinoids have a lot of therapeutic potential. But the actual level of research and clinical trials on their therapeutic potential is way behind. Secondly, at NanoSphere, we look at the best route for delivering the different cannabinoids. For certain conditions, you’ll probably need an entourage effect of different cannabinoids, often THC along with CBD and terpenes. Nanotechnology allows you to get more surface area of activity by only having the molecule that’s active placed in what we call a nanosphere with more surface area, which gives it more reactivity and higher levels of bio-availability.
Nanotechnology also allows you to develop what we call smart nanoparticles. In which we can tailor the way the nanoparticles are delivered to the receptors in the target area. In this way, nanotechnology in many cases is very effective. For example, a non-nano-sized and non-encapsulated cannabinoid is going to have a very hard time penetrating the barrier of the skin surface. However, when we surround cannabinoids with a phospholipid membrane made of the same materials that form the membranes around the trillions of cells in the body, it acts much like a Trojan horse and carries the cannabinoids directly through the skin surface and into the bloodstream.
The same process allows us to use nanotechnology in other areas. For example, one of the interesting areas we are pioneering is direct nose-to-brain delivery. Cannabis taken by any method results in only 1 percent of the cannabinoid actually reaching the bloodstream to penetrate past the blood brain barrier; a pitiful amount. By using our technology — which is really on the cutting edge of research for treating brain disorders and other conditions — we can deliver cannabinoids right to the specific part in the nose that goes directly into the brain. The research has shown a bio-availability of maybe two to three times or more than intravenously which is remarkable.
Nanotechnology allows us to create these molecules with more surface area with the greater ability to be transported and directed to where they need to go in the body. That is how the use of nanotechnology is changing the cannabis space over the future by allowing us to deliver precision metered dosage in micro-liter amounts.
INN: Outside of cannabis-related therapeutics, are there any other applications for this technology across other health and wellness markets?
RK: Oh, absolutely. As a company, our delivery system technology is patented for the delivery of nutraceuticals and dietary supplements that can be used by physicians as alternatives and complements to their current medications. We have a pharmaceutical division and have filed IP for the delivery of NSAIDs which will make them safer for daily use without causing, for example, inflammation and gastric erosion. We have a cosmeceutical division to make cosmetics more bio-active and bio-available. And this technology also has applications in pet care. For example, if a pet has to take a medication and oral administration is a problem, the dose can be given intranasally. So across the spectrum, nanotechnology is safe and effective and can change the scope of how medications are delivered, increase their benefits and also be used for a wide range of biotechnology purposes for the future delivery of medications into the 21st century.
INN: How is NanoSphere harnessing nanotechnology to meet its goal of becoming a leader in next-generation delivery methods?
RK: I think it’s very important to state that a lot of the research on nanotechnology is done in a laboratory only. Translating that research into scalable systems that can be manufactured and produced is a challenge. We pride ourselves in having recently received a patent on our core technology for the manufacturing of a scalable universal form of lipid nanoparticles to incorporate a wide range of low bio-availability compounds.
We believe that our delivery system allows us to take a blueprint of all the same systems we have in our primary lab in Colorado and set up shop in another location within the US, or even in Vancouver or Toronto, for example, and be able to produce the same kind of nano-encapsulations we’re pioneering in Denver. And for any kind of compounds, whether from cannabis or pharmaceuticals, in effect changing the way nanotechnology can be used in a universal way. We are at the forefront of leading research in nanotechnology as well as commercial applications around the world.