G.E.T. the Facts

The CanncestraTM Success Story

Canncestra targets muscles and joints with unparalleled efficacy. We do so—surprisingly—via topical application to the skin. Our groundbreaking ability to solve the skin’s formidable penetration barriers is the focus of Canncestra’s multiple transformative breakthroughs. 

The Skin

Our skin—our largest organ—is responsible for a spectrum of essential protective functions. It has immune system activity, regulates temperature, prevents excessive fluid loss or gain, and produces vitamin D. Our skin also protects us against trauma and UV damage, and is a formidable barrier to the entry of harmful elements from the environment—pathogens, irritants, allergens, and toxins. But this effective barrier system has a highly frustrating downside when we want to send therapeutic compounds to tissues below the skin. Scientists have been trying for a very long time to eliminate these barriers, and we have finally done it. Our pioneering scientific discoveries have elevated Canncestra’s products to unprecedented levels of effectiveness.  

A summary of the skin’s complex fortifications will highlight the challenges faced in making Canncestra this effective. The skin has three segments. The topmost segment is the 5-layer epidermis, beginning with its most impenetrable layer—the tightly packed cells of the stratum corneum. Below that, the four remaining layers of the epidermis also present an extremely dense physical barrier, including very strong adhesion between cells, to anything that manages to get through the top layer. Below the epidermis lies the two-layer dermis, and then the hypodermis, the skin’s deepest layer. In addition to the formidable penetration challenges, the hydrophilic epidermis and hypodermis welcome water-containing molecules and reject fatty compounds. In contrast, the lipophilic dermis between them welcomes fat-containing compounds, but rejects water-containing molecules. 

Meeting the Challenges

We were determined to overcome the penetration and biochemical challenges that have substantially limited existing topical pain relief products. And that is why and when we partnered with pharmacologist Dr. Victor Silva, whose long-time research efforts include progress in overcoming the skin’s barriers to the penetration of therapeutic treatments. With Victor on our team, we were able to begin our transformative scientific journey.

 With Victor’s inspired new science, Canncestra’s first step was creating products made of the smallest particles possible—nanoparticles—which are 100 nanometers or less. Nanoparticles have been used in cosmetics and pharmacology for improved drug delivery since the 1990s, and Canncestra incorporates this pharmaceutical-grade nanotechnology. Enhancing that technology, we wrapped our nanoparticles in strong, highly flexible protective packages able to carry them on their journey. We also increased the width of their travel route between the cells to give them the room they need, and enabled them to shed layers as they travel, so that they remain compatible with the changing biochemical environment as they move down through the skin’s layers. 

Our scientific breakthroughs work in synchrony to bring Canncestra where it’s needed—to tissues in pain. G.E.T. is Canncestra’s acronym to describe this science.

 G. GlycoXanthin—Creating Room to Travel 

Sugar (glyco-) and caffeine (-xanthine) are not new to skincare formulations. Sugar has been used for drawing moisture to the skin, and to promote wound healing. Caffeine prevents UV-induced skin damage, and has a general anti-inflammatory action. Canncestra’s patented matrix, GlycoXanthinTM, combines them in a way that amplifies their benefits within the skin. They create the lotions’ smooth and hydrating texture and they support skin health. And most importantly, this matrix enables a route down through the skin for our Envisome carriers to travel. 

E. Envisome—The Multifunctional Travel Vehicle

Next we came up with the EnvisomeTM, the ingenious protective, ultra-flexible carrier that brings Canncestra’s nanoparticles effectively and safely through the skin’s layers and delivers them at full strength to the tissues below. 

Our Envisome is a new-and-improved type of ethosome. The ethosome—a novel transdermal delivery carrier—was designed to be a remarkably flexible container. We modified the ethosome using a proprietary ratio of phospholipids, ethanol and propylene glycol. This significantly increases their flexibility and burst-resistance, as they carry our nanoparticles down through the skin’s layers. Our Envisome is also designed to shed layers as it descends, so it remains compatible with the biochemical environment, whether it’s hydrophilic or lipophilic. This is encapsulation science at its newest.

As the Envisomes reach their target tissues, our compounds are released. This includes the terpenes, CBD, and other botanicals specially chosen to enhance the unique effectiveness of Canncestra’s spectrum of ingredients.

T. Terpenes, CBD and Other Botanicals 

We amplified Canncestra’s analgesic and anti-inflammatory power by adding terpenes (in addition to those already part of our hemp oil) and a careful selection of other targeted botanical compounds. Our goal is minimizing or eliminating the experience of pain—and ensuring meaningful, reliable relief. We know that pain can be activated by multiple pathways in the body—which we want to turn off, and it can be blocked by others—pathways we want to turn on. This guided our selection.

Terpenes

Terpenes are responsible for the aromatic elements of plants and essential oils, such as in mints, citrus peel, and hemp. They are clinically documented to have anti-pain, anti-anxiety, and anti-inflammatory benefits. Many are also anti-microbial. The hemp plant itself contains a menu of terpenes, many shown to stimulate multiple anti-pain and anti-inflammatory pathways, and Canncestra is made with a full-spectrum hemp oil CBD distillate to ensure that they are present. 

Additionally, we increased the amounts of the hemp plant’s four most effective anti-inflammatory and pain-relieving terpenes—alpha terpinene, beta-myrcene, beta-caryophyllene, and limonene. And we’ve included two non-hemp terpenes—menthol and camphor—to increase even further the formula’s ability to target and turn off pain and inflammation. The camphor and menthol molecules do this by binding with anti-pain receptors similar to those the CBD binds with. Terpenes interact synergistically with cannabinoids to increase their benefits, this is called the “entourage effect.”

CBD (Cannabidiol) 

Canncestra’s full-spectrum hemp oil distillate contains many of the plant’s cannabinoid compounds in addition to terpenes. The predominant one in our lotions is the well-researched cannabidiol (CBD), and we have developed a technique to exponentially maximize the dose that our Envisome carriers transport.  

Cannabinoids are central to the full scope of our body’s functions. The Endocannabinoid System (ECS) includes the body’s largest receptor system, along with the 60–100 endocannabinoids that the body produces, and the enzymes that make them or break them down. As our master regulator of homeostasis, the ECS impacts all of our other systems: nervous, endocrine, cardiovascular, reproductive, metabolic, musculoskeletal, immune, digestive, and cutaneous. This ancient ECS system is so central to function that it is found in nearly all animals, invertebrates included (even worms). Insects and sponges are the primary exception. In addition to the endocannabinoids that our body produces, we are also able to get phytocannabinoids from certain plants, including cannabis/hemp and many others, which fit into our body’s receptors. 

The primary avenue of delivering phytocannabinoids has been by mouth. But this route holds the potential for degradation in the GI tract and the liver. So we chose delivery through the skin to get direct impact on the tissues. We created substantial scientific progress in overcoming the skin’s penetration barriers. A side benefit of our transformational progress is that even the minimal percentage of CBD molecules that remain in the skin have therapeutic benefit. 

Many cannabinoids assist the skin, which is an important component of the ECS. The skin makes nine of its own endocannabinoids, and CBD receptors are found in almost all types of skin cells and structures. In line with this, animal studies have found that CBD—and other endo- and phytocannabinoids—impact the skin, with potential anti-inflammatory, anti-pain, anti-itch, keratin-balancing, anti-aging, and wound-repair benefits. 

CBD and other therapeutic compounds work because, at some point in our ancient past, we developed cell receptors for a great spectrum of plant and inner-derived chemicals. A cell receptor is a protein on or inside a cell. Once the receptor receives signals from a messenger chemical (called a ligand) that binds to it, like a key fitting into a lock, the cell changes-- virtual doors open and the body responds. Research shows that CBD can bind to several pain-relieving receptors, giving it the opportunity to initiate many beneficial actions within.

Although it does not bind to the typical CB-1 or CB-2 receptors (it blocks them, instead), CBD
is still an active phytocannabinoid by increasing the anti-inflammatory, pain-relieving and muscle-relaxing endocannabinoid, anandamide. CBD effectively suppresses pain by preventing anandamide from being broken down.

CBD also hooks up with several other receptors that more directly influence pain. Some of these receptors include the TRPV1 (Transient Receptor Potential Vanilloid 1) receptors, MORs (Mu Opioid Receptors), 5-HTRs (Serotonin) receptors, D2 (Dopamine) receptors), plus a major anti-pain pathway, the PPAR (Peroxisome Proliferated-Activated Receptor agonist) receptors, effectively turning off pain. CBD is a pain multi-tasker.

For increased effectiveness, Canncestra succeeded in boosting the CBD-carrying capacity of our Envisomes. Canncestra now provides a whopping 1,500 mg of CBD per ounce—almost three times more than any other topical on the market. 

And Other Botanicals

Combining our decades of healthcare experience working with plants in clinical practice and our knowledge of botanical research, Canncestra selected specific herbs and herbal compounds to boost the actions of the terpenes and cannabinoids in our lotions. We searched for both whole botanicals and isolated compounds that bind with and activate the same groups of anti-pain/anti-inflammatory receptors in the skin, joints, and muscles. 

Our whole botanical choices are: turmeric, boswellia, and devil’s claw. Our isolates choices are: resveratrol, methyl salicylate, and capsaicin. Because each selection has unique benefits, Canncestra takes advantage of both approaches by skillfully combining the whole plant parts with isolates. 

The whole medicinal plant parts: Turmeric root (Curcuma longa) has a multitude of relevant targets that include activating the anti-pain PPAR pathway, and inhibiting at least a dozen inflammatory cytokine and chemokine signals. Turmeric has a long history of successful use in a variety of conditions that include pain, and inflammation. Boswellia resin (Boswellia serrata) also hits multiple targets that include pain-relieving and anti-inflammatory receptors and their pathways (including PPAR). Devil’s claw root (Harpagophytum procumbens) is strongly supported by both traditional use and recent studies for both internal and topical use. It contains a multitude of bioactive compounds that include anti-inflammatory and pain-relieving agents, and it activates cannabinoid CB-2 receptors, among others, adding to the synergy of botanical pain relief. 

The isolates: Resveratrol is found in many plants, with much research documenting its antioxidant, anti-inflammatory, and anticarcinogenic effects. Topically, it also activates the TRPA1 and PPAR pathways for pain inhibition. Methyl salicylate, found in a number of plants, is a topical anti-inflammatory and pain-relieving compound that also acts on TRP pain receptors. It is chemically similar to aspirin, and used in many topical analgesics. Capsaicin—responsible for the intense pungency of chili peppers—not only facilitates absorption of other components it’s paired with, but aids in topical pain relief and improving local circulation. It is curious in its action, as it initially activates the TRPV1 receptors to cause heat pain, and then desensitizes the receptor to stop pain signals, thus relieving pain. Our science enables an increased capsaicin content—benefit without the burn. 

Summary

Using pharmaceutical-grade nanotechnology to prepare the full spectrum of CBD and other hemp compounds, added terpenes, and carefully chosen botanicals for delivery, Canncestra successfully delivers them at full dose—a first—via its innovative technology. The primary advance is our encapsulation science—the creation of our Envisome, an ultra-flexible, adaptable carrier with its nano- particle cargo. Its cargo remains fully protected as it passes through both lipophilic and hydrophilic environments. Also critical is our creation of a navigable pathway for the Envisome’s travel, a result of our GlycoXanthin matrix. And we have achieved a dose of CBD that is almost three times higher than any other topical product on the market. 

By substantially increasing the CBD dose, and by carefully selecting for effect-enhancing terpenes and other botanicals, we created a product that binds with pain and anti-pain receptors in the tissues. Canncestra has designed a significantly more effective delivery system enabling a navigable travel route through the skin. Canncestra has a unique lotion that targets topical pain relief. And as a side benefit, the GlycoXanthin matrix also protects and hydrates the skin. 

G.E.T. It?!

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