It is well-known that cannabis oil is poorly absorbed and many companies have a difficult time separating good ingredients from bad (poorly absorbed) ingredients. To address this, Geocann utilizes an exclusively licensed drug delivery technology, called VESIsorb®, so health conscious consumers receive the maximum benefits from phytocannabinoid compounds. VESIsorb® is the leading delivery system innovation for dramatically improving the bioavailability of poorly absorbed ingredients, like cannabis oil. Since 2007, close to 200 million consumers in all six major continents have safely and effectively used one of the 50+ VESIsorb® formulas.
We are delighted by the number of questions we have received from the medical community, scientists, researchers and health conscious consumers worldwide. Consequently, we have developed this “ADVANCED FAQ” for those interested in gaining a deeper and clearer understanding of why natural actives like phytocannabinoids are better absorbed when delivered in this patented colloidal droplet system.
VESIsorb® is described as a “natural” technology because it mimics the human fat digestion and absorption process. It is known that poor water-soluble drugs, e.g. fat soluble vitamins, are better absorbed when administered after a meal containing fat. One of the reasons for the improved absorption is the enhanced drug solubilization by bile salt mixed micelles which are formed from the digestion products of dietary triglycerides (monoglyceride and fatty acids) and bile - a nanotechnology tool developed by Mother Nature. The task of naturally formed bile salt-mixed micelles, having a size below 10 nanometers, is to transport the lipophilic molecules through the aqueous environment of the GI-tract and across the unstirred water layer to the absorptive epithelium. Individual lipid molecules, and not the micelles per se, are the species that enter the absorptive membrane.
The precise manner by which lipophilic molecules cross the membrane of the enterocytes is uncertain. Until recently it was generally thought that lipids simply diffuse, individually as monomers through the lipid bilayer of the membrane into the cell. Now there is evidence that dietary fatty acids may be transported across the enterocyte membrane by a specific transporter.
Once inside the enterocyte, dietary fatty acids and monoglycerides diffuse to the smooth endoplasmic reticulum, where they are resynthesized into triglycerides. Finally, the resynthesized triglycerides packaged into chylomicrons that are secreted into lymph. It is very important to understand that nano-sized micelles are produced naturally in our bodies each and every day.
On the other hand, there are methods used in nanotechnology that are “top down” which simply means they use energy and force to decrease the size to less than 100 nanometers. They use high-pressure homogenizers or micro-fluidizers. They are, in some cases, fundamentally milling down crystals from microns to much smaller nano-sized hard particles. This never happens in the body, and it is far from a natural occurrence.
VESIsorb®, a lipid-based formulation that naturally self-assembles on contact with an aqueous phase into a colloidal system (so called “association colloid”), mimics this mixed micellar absorption pathway. The improvement of oral drug or natural bioactive bioavailability by this technology is broken down into three steps:
Step 1: Formation of the colloidal delivery system. When mixed with an aqueous system (such as the GI-lumen), this unique lipid-based formulation naturally forms a self-assembling colloidal delivery system containing solubilized phytocannabinoids. A colloidal droplet is typically less than 100nm in diameter and consists of a monolayer with the bioactives in its oil core.
Step 2: Diffusion of the colloidal system across the unstirred water layer.
Step 3: Dissociation of single molecules from the colloidal system and transfer to the absorption epithelium and passive diffusion of single molecules across enterocyte membrane.
Since VESIsorb® mimics the naturally occurring mixed micellar transport system of the human body it can be considered a safe technology to improve the absorption of poorly water soluble drugs.
Micelles are composed of a surfactant or surfactant mixture and the active substance to be solubilized within the center of the micelle. A micelle is like an aggregate of surfactant molecules dispersed in a liquid solution. A surfactant molecule has a hydrophilic part – called “head” – and a hydrophobic part – called “tail”. A typical micelle in an aqueous solution forms an aggregate with the hydrophilic “head” regions in contact with surrounding water (solvent), sequestering the hydrophobic tail regions in the micelle center. In this “hydrophobic tail center,” the active substance is dissolved. A “classical” micelle system does not contain oil and is a surfactant-rich system. If a micelle contains small amounts of oil, they are called “swollen” micelles.
Like micelles, VESIsorb® is an aqueous dispersion. However, the dispersed phase is composed of both surfactant AND oil, and belongs to the systemic group of micro-emulsions. The dispersed phase of VESIsorb® can be envisioned as nano-droplets composed of an oily core (oil components/active ingredients) surrounded by a hydrophilic shell (emulsifiers). Compared to a micellar system, the VESIsorb® contains lower amounts of surfactant (which is highly desirable) and high amounts of oil (lipophilic core/center where the active substance is dissolved).
Aqueous VESIsorb® dispersion, like micro-emulsions, act like real solutions that are in a thermodynamic equilibrium and thus, cannot be accountable to the classical image of an emulsion. It is a “colloidal” solution with extremely tiny (< 100nm), highly flexible associates.
Liposomes are vesicles and composed of a phospholipid bi-layer membrane surrounding an aqueous core. Fat-soluble active substances can only be solubilized within the bi-layer membrane, thus the loading capacity is limited and lower compared to VESIsorb®.
VESIsorb® has been designed to function and perform in the human body at body temperature (37°C). This system ensures 100% active ingredient solubility at body temperature both in the VESIsorb® fill mass and in the aqueous body environment. For example, when combined with VESIsorb®, phytocannabinoids completely dissolve at body temperature (37°C) but not necessarily at room temperature (so called temperature dependent solubility). Thus, by cooling down the system below body temperature, the clear solution may become oversaturated and the system becomes semi-solid to solid. By re-warming the system to body temperature of 37°C, it completely liquefies again and then rebuilds in contact with the gastric/GI fluids in the colloidal delivery system.
The patented VESIsorb® self-assembling colloidal droplet delivery system is technologically advanced and more scientifically sophisticated than other so called “enhanced absorption systems.” The superiority of the delivery system has consistently been demonstrated in well-designed pilot and peer reviewed published pharmacokinetic absorption and bioavailability studies.
The colloidal droplet system must be customized to each active or combinations of actives. Successful VESIsorb® formulations are optimized for droplet conversion performance using dynamic light scattering analysis. The goal is 100% solubilized actives, in a completely homogeneous system with mean droplet size of less than 100nm. Meeting these criteria confirms that the VESIsorb® self-assembling colloidal droplet system is working. What is also important to understand is that the system is not only built around the unique molecular characteristics of the phytocannabinoids but designed for optimal performance in the body. When mixed with an aqueous system, such as the GI-fluids, this unique lipid-based formulation naturally forms a self-assembling colloidal droplet delivery system containing solubilized phytocannabinoids.
It is simple to say that all one needs to do is dissolve fat soluble actives in an applicable oil and just fill it into a soft gel capsule. Within the capsule (oil environment) it is indeed dissolved but NOT in an aqueous environment. As soon as the oil, containing the active in a dissolved form, comes in contact with water, the solution medium (oil) gets diluted and is not stable or mixable with water because the “linking molecules” (emulsifier) are missing. So, immediately upon losing its oil solubility feature, the former solved active starts crystallizing in the water environment (e.g. GI-tract). When this occurs, there is poor dissolution, poor absorption, and little effect.
VESIsorb®, on the other hand, is a carrier system which keeps water-insoluble, respectively fat-soluble, molecules in a hydrophilic environment (e.g. water, gastric fluids, etc.) in solution. It is a “colloidal”-scale solubilized system. VESIsorb® does not change a molecule chemically. It is a solubilization vehicle comprised of oils and monolayer forming agents (emulsifiers). Emulsifiers, due to their nature (hydrophobic tail and hydrophilic head) – arrange in an aqueous environment at the interface between oil and water. Without these linking molecules, it is not possible to get a stable oil/water mixture (e.g. emulsion). A stable emulsion is able to keep fat-soluble molecules dissolved in a water environment. Upon adding VESIsorb® to an aqueous environment, it naturally self-assembles into a “colloidal emulsion,” where no energy is required to build up the emulsion droplets. These “colloidal droplets” are not static systems. They are dynamic, meaning their molecules (emulsifiers, oils and actives) could move by a so-called perpetual “flip-flop” effect from one droplet to another or to other membranes (e.g. enterocytes).
The peer-reviewed journal, “Alternative Therapies in Health and Medicine,” published the results of a double-blind study comparing the bioavailability of patented CoQsource® (coenzyme Q10 in a VESIsorb® formulation) Bio-Enhanced CoQ10 to that of other bio-enhanced formulations. The study, entitled, “Relative Bioavailability Comparison of Different Coenzyme Q10 Formulations with a Novel Delivery System,” appears in the March/April, 2009 issue, Volume 15, Number 2.
“These are the most compelling clinically proven absorption results of any CoQ10 formulation that have been published to date.”
Dr. Zheng-Xian Liu
The graph below provides a vivid illustration of the difference in CoQsource® (the orange line) which is coenzyme Q10 in the VESIsorb® delivery system versus the three other “bio-enhanced” coenzyme Q10 products in plasma concentration levels over time. CoQsource® (coenzyme Q10 in the VESIsorb® delivery system) not only has higher plasma concentration levels after one hour, but continues to increase dramatically before reaching Cmax at about 4 hours. The plasma concentration of CoQsource®remains well above levels for the 3 other treatments throughout the 24 hour period.
A pharmacokinetic pilot study in humans comparing Kaneka QH™ Ubiquinol to the same Kaneka QH™ Ubiquinol in the VESIsorb® delivery system demonstrated an increase of 696% in peak blood levels of Ubiquinol. The relative bioavailability calculated using the area under the curve was also increased by 485%.
A pharmacokinetic pilot study in humans comparing OmegaChoice® 90 Concentrated Omega-3 EPA to the same OmegaChoice® 90 in the VESIsorb® delivery system demonstrated an increase of 567% in peak blood levels of EPA. The relative bioavailability calculated using the area under the curve was also increased by 487%.
VESIsorb® has successfully been applied to the most popular science-backedbioactive ingredients like concentrated omega-3 EFAs, coenzyme Q10, QH ubiquinol Q10, vitamin K2, curcumin, phytocannabinoids, vitamin D, pterostilbene, palm tocotrienols, diindolylmethane (DIM), gamma tocopherols, citrus polymethoxylated flavones (PMFs), resVida®, resveratrol, krill oil, algal DHA, vitamin A (retinoids), phospholipids (PC, PS), terpenes (e.g. beta-caryophyllene), among others.
These natural ingredients are notoriously poorly absorbed, and VESIsorb® has dramatically improved their absorption, solubility and application in nutritional supplements, food and beverages, and personal care products.
The advantages of the patented VESIsorb® delivery system go well beyond absorption and bioavailability. VESIsorb® broadens the applications for certain bioactive ingredients into food products, drink mixes, beverages and personal care products. Success in this area has come by addressing issues such as water solubility, oxidative stability, shelf life and uniformity of dispersion in the delivery medium. The VESIsorb®system is easy to work with in production and effectively improves many production systems.
“Natural” is normally linked with purity and safety. Nanotechnology is a broad and complex field that needs to be discussed under certain rules of nomenclature and distinguishing aspects. Experts agree it is critically important to differentiate between solid “nano- particles” versus “nano-size” fluid droplets as well as differentiating between those that disintegrate in vivo and those that do not.
The VESIsorb® naturally self-assembling association colloidal droplets disintegrate within the GI-tract into the single components; thus the formed droplets are of transient nature and considered safe by the experts. In contrast, solid, non-disintegrating nano-particles such as carbon nano-tubes, are an example of nanotechnology that has raised concerns about safety.
However, aside from the mentioned aspects, many other factors can influence the safety of nano-systems. Various scientific expert groups are discussing this complex issue and are trying to establish guidelines for the safe use of nanotechnology. A recent and excellent report published by the IRCG (International Risk Governance Council; “Risk Governance of Nanotechnology Applications in Food and Cosmetics”) summarizes some of the activities regarding safety of nanotechnology.
The Geocann cannabis technology platform for growth is the culmination of the unmatched Intellectual Property (IP) portfolio that SourceOne Global Partners has
acquired and developed over the past 15 years. While VESIsorb® is the most recognized component of this IP portfolio, Geocann also utilizes DPTechnology™ and VESIsorb® VEDD Delivery System to improve the performance of key phytocannabinoids where applicable.
Please submit additional questions or comments, and a member of our team will promptly respond personally to your inquiry.