Levagen+ (PEA) – the CBD alternative, By: Mariko Hill (Product Development Executive)
The demand for CBD and its potential therapeutic benefits has driven sales of the extract to an all-time high with market predictions of $57 billion by 2027. However, with this growth, comes confusion around cannabis, cannabidiol (CBD), and hemp. In the U.S. it reached a tipping point when the 2018 Farm Bill federally legalized the production of industrial hemp-derived CBD containing less than .03 percent of THC (tetrahydrocannabinol). Most states, though, have not been able to update their laws to match this new federal law, leaving them without answers to CBD’s legalities. Similar confusion is taking place in Europe. In January 2019, the European commission added extracts of cannabis sativa, including CBD, to the Novel Food catalogue, therefore requiring pre-market authorization. European Food Standards Agency (EFSA) has yet to approve any CBD supplier.
So, what is CBD and is it worth the potential risk? In the 1990s, scientists discovered endocannabinoids, the natural cannabis-like molecules produced on demand by the body. The endocannabinoid system (ECS) has been found to help to balance and maintain many physiological systems such as memory, pain, mood, appetite, stress, sleep, immune function and more.
The ECS consists of the endocannabinoids (e.g. Anandamide [AEA]), cannabinoid receptors, and the enzymes that synthesize and degrade endocannabinoids. Two receptors, called CB1 and CB2, mediate many effects of endocannabinoids within the central nervous system. Phytocannabinoids are also known to act on these receptors, as they are a naturally occurring plant. This may be why the cannabis plant, mainly CBD, has recently emerged as a promising therapy for a number of ailments.
Today, there are various other barriers proving the CBD market to be a ‘grey area’ such as the lack of clinical evidence, emerging toxicity studies and products found to contain more than the legal amount of THC (this can be detrimental a professional athlete’s career). Thus, ingredients that similarly influence the endocannabinoid pathways should be sought out.
Fortunately, for those concerned about the potential risks, there is palmitoylethanolamide or PEA for short. PEA is a relatively new supplement with research beginning to surface highlighting its analgesic, anti-inflammatory and neuro-protective benefits.
What is it?
PEA is a fatty acid amide that is naturally produced by the body in response to stress, pain and inflammation as a repair mechanism. It is categorised as part of the extended endocannabinoid family and research has demonstrated its benefits for inflammation, pain, sleep and exercise performance.
PEA was first discovered in 1957 from isolating from egg yolk and was found to be the compound that gave eggs their anti-inflammatory properties. In the mid-1960’s, researchers established PEA to be an endogenous compound naturally present in all mammalian tissues (muscle, brain, heart etc).
How does it work?
PEA operates through multiple pathways and mechanisms within the body to provide its beneficial analgesic and anti-inflammatory effects. It has the ability to work both directly and indirectly within the ECS.
Directly, PEA reduces inflammation locally by inhibiting the secretion of pro-inflammatory molecules (e.g. histamine) via the PPAR-a receptors. Furthermore, on a cellular level, PEA stimulates a cascade of reactions that ultimately leads to regulating the expression of proteins that reduce inflammation.
Indirectly, PEA enhances the levels of other anti-inflammatory compounds that can regulate pain, such as AEA (often dubbed as the ‘bliss molecule’ or the body’s own ‘natural THC’). This is done by inhibiting the enzyme fatty acid amide hydrolase (FAAH), which breaks down AEA. This mechanism is known as the ‘entourage effect’. AEA’s ability to bind on to both CB receptors and TRPV-1 channels helps combat pain and increase relaxation.
Importance of PEA?
Levels of PEA naturally decrease with age. Moreover, when an individual encounters painful and/or inflammatory stimuli (e.g. exercise-induced inflammation from running), PEA levels drop precipitously as they start binding on to PPAR-a receptors. Exogenous supplementation is therefore needed in order to restore levels of PEA in the body.
PEA vs CBD?
PEA resembles CBD in that both substances have anti-inflammatory and neuro-protective properties. However, CBD is not produced by the human body unlike PEA, which is endogenously produced as a direct response and repair mechanism to inflammation and pain.
CBD also has yet to be proven effective and safe, as studies have only shown its benefits for certain diseases such as epilepsy. PEA on the other hand has a wealth of safety and efficacy studies in the areas of managing discomfort, supporting joint health and enhancing recovery.
More relevant in the realm of sport, PEA is an excellent supplement for professional athletes. Whilst THC levels in CBD supplements is highly regulated and will only be found in very small concentrations, both compounds occur naturally in the hemp plants, thus is not possible to remove THC completely. This provides issues for professional athletes who are regularly drug tested.
PEA can provide many of the same benefits as those anecdotally claimed for CBD (i.e. pain, inflammation, sports recovery and sleep), yet removes the concern around THC trace levels which are banned by the World Anti-Doping Agency in competing athletes.
The superior PEA – Levagen+
Due to PEA being lipid in nature, it does not dissolve well in water, reducing both the absorption and bioavailability in the digestive system. In order to overcome this issue, Gencor has developed a branded form of PEA, Levagen+. Levagen+ utilizes the novel, award-winning LipiSperse delivery technology, created by Pharmako Biotechnologies, that helps increase bioavailability and functionality of PEA.
One study showed an approximate 1.8 increase in PEA blood levels when comparing 300mg of Levagen+ to 300mg of standard PEA formulation. This increase in absorption and bioavailability leads to a higher active concentration of PEA and suggests that lower dosages will have the same efficacy when compared to standard PEA.
Moreover, with the ability of Levagen+ to disperse freely in water, formulators are able to develop various formats beyond capsules and tablets, which standard PEA is only limited to. These innovative formats include: RTD shots, effervescent, gels etc.
What can PEA help with?
Reducing acute and chronic soreness/inflammation: through the mechanisms described previously, PEA has been shown to reduce acute and chronic soreness and decrease inflammation across a number of different ailments. A meta-analysis by Berker et al (2017) showed that PEA was associated with significantly greater pain reduction compared to control conditions.
Exercise performance & recovery: whilst currently there is limited data around the efficacy of PEA in exercise performance and recovery, the preliminary findings of a recent trial by Gencor demonstrated promising results. After supplementing with PEA, subjects had lower lactate levels than the control group signifying increased aerobic energy metabolism and decreased anaerobic energy metabolism, allowing for a higher level of intensity for a longer period of time. Participants also resulted in lower levels of myoglobin post exercise – a marker of muscle damage. Therefore, PEA could potentially lead to decreased muscle damage, increasing sports performance.
Sleep: PEA can help promote restful sleep through activation of CB1 receptors which increases a calming effect inducing sleep. By activating TRPV-1 channels, PEA may also increase REM sleep – our deep phase of sleep.
Immune boosting: There is a wealth of evidence demonstrating PEA’s role lowering symptoms of cold, fever, headaches and sore throats, thus may be a potential immune-boosting ingredient.
General wellbeing: Endocannabinoids helps to regulate mood, emotion, pleasure perception and much more. PEA may also be able to reduce anxiety and stress through its ability to enhance the levels and actions of anandamide. Further, those with higher levels of PEA in their blood also showed to have a higher stress tolerance.
All in all, there is a tremendous amount of evidence demonstrating the benefits of PEA in various segments. Branded ingredients, such as Levagen+, presents ingredient manufacturers a solution to the demands of consumers and regulators for a safer, more efficacious CBD-alternative. Levagen+ is GRAS, approved by Health Canada as an NHP, and accepted as a dietary supplement in U.S., Europe, Australia and India.