We are the first to offer PEA in a high-quality and directly applicable format for unique end products
PEA in NutraCups
LIPOSOMA proudly announces our newest product range, called NutraCups. For LIPOSOMA’s NutraCups we selected our finest liposome ingredients and placed these in cup cartridges that are designed for standard coffee cup extraction machines, which are present in almost every household. Every NutraCup produces a perfect liposome dispersion upon hot water extraction, containing high-quality active ingredients. This technology is especially well suited for active ingredients that require higher daily doses, like palmitoylethanolamide (PEA), a substance that can be very helpful in peripheral pain relief. PEA requires a high starting dosage of 1200 mg per day, followed after two months by a daily maintenance dosage of 600 mg, which can be provided because of our NutraCup technology. Orally administered PEA in the form of capsules containing conventional powder is poorly absorbed by the body. The warm liposomal PEA dispersion produced with PEA NutraCups ensures PEA is optimally encapsulated in finely dispersed liposome vesicles, facilitating the process of intestinal uptake and leading to more effective concentrations in the body. Moreover, because the actual liposome dispersion is produced at home right before consumption, no preservatives are needed in the product.
What is PEA?
Palmitoylethanolamide (PEA) is an endogenous lipid present in various human tissues including the brain, liver, eyes and muscles. It is produced from membrane phospholipids and exerts a variety of functions, many of which are related to inflammation and pain signalling [1]. Abnormalities in the levels of PEA are associated with chronic inflammation [2] and pain disorders [3,4,5] underlining its importance in these processes.
PEA and pain reduction
A substantial number of preclinical and clinical studies have demonstrated that PEA administration can relieve pain (analgesia). Two meta-analyses of these studies both concluded that PEA treatment was indeed associated with significant pain reduction. Efficacy is reported in lower back pain, Carpal Tunnel Syndrome and pelvic pain [6,7]. More recent clinical studies confirm the analgesic efficacy of PEA in the treatment of patients with bladder pain syndrome [8], chronic pelvic pain [9], chronic orofacial pain [10], (chronic) lower back pain [11-14], Carpal Tunnel Syndrome [15], knee osteoarthritis [16], diabetes [17] and pain after back or spine surgery [18].
Several different mechanisms of action have been suggested to explain the analgesic effects of PEA. Firstly, PEA can modulate the activity of the endocannabinoid system, which plays a key role in the experience of pain [19]. PEA does not directly bind to cannabinoid receptors but modulates their activity indirectly by preserving the natural agonists of these receptors [20,21]. Secondly, PEA reduces inflammation in the peripheral and central nervous system, which also leads to chronic pain relief [22-24].
Limitations of other PEA products
Due to its lipophilic nature and high melting point, PEA is barely soluble in water and other aqueous solvents [25]. Upon oral intake of a typical dose of PEA in conventional powder form, very little is absorbed and enters the blood circulation, leaving only minimal amounts that can reach the target sites in the human body. Several attempts to improve this have been made, but the tendency of PEA molecules to crystallize and precipitate in almost every solubilization attempt, points to the difficulty also the body faces in absorbing the PEA molecules from the intestinal lumen and transporting it to the target sites. Indeed, the bioavailability of PEA in humans seems to be extremely low with only a short-lived presence in blood after oral intake [26, 27].
Benefits of NutraCups
By providing PEA in a liposome, bioavailability can be increased compared to non-liposomal PEA products. To enable successful liposomal encapsulated PEA, LIPOSOMA developed a new technology called NutraCups. With this technology, all ingredients of liposomal PEA are provided in a cup cartridge and liposomes are formed upon extraction of the cups with warm water. The cups are made compatible with standard coffee cup extraction machines, so that the liposomal PEA beverage can be produced at home right before consumption. At LIPOSOMA we discovered that only this way complete dissolution of the PEA molecules in the liposomal vesicles can be ensured and the required dose can be administered. Furthermore, the NutraCups technology has the advantage that no preservatives are needed.
To summarize, with our NutraCups liposomal PEA product we provide you an effective dose of PEA in the best available form to enable your body to benefit from its health effects that have been studied and documented by many scientists all over the world.
“Discover all the benefits of our liposome technology that along with our outstanding ingredients help us to establish valuable relationships with our business partners. “
LIPOSOMA Nutraceuticals; experts in liposomes
LIPOSOMA manufactures branded and white label liposomal supplements.
Our high-end liposomal nutraceuticals are guaranteed by the academic qualifications of our team and its commitment to scientific excellence.
Our liposome technology offers many advantages for nutritional supplement producers, the food sector and consumers. Our liposomal vitamins and other nutraceuticals are available as raw materials, capsules, liquids and many other tailored solutions.
Would you like to learn more? Give us a call at 0031 20 237 36 00
Sources
[1] Iannotti, A., Di Marzo, V., Petrosino, S. (2016). Endocannabinoids and endocannabinoid-related mediators: Targets, metabolism and role in neurological disorders. Progress in Lipid Research 62:107-128.
[2] De Filippis, D., d’Amico, A., Cipriano, M., Petrosino, S., Orlando, P., Di Marzo, V., Iuvone, T., Iuvone, T. (2010). Levels of endocannabinoids and palmitoylethanolamide and their pharmacological manipulation in chronic granulomatous inflammation in rats. Pharmacological Research 61(4):321–328. doi:10.1016/j.phrs.2009.11.005
[3] Ghafouri N, Ghafouri B, Larsson B, Stensson N, Fowler CJ, Gerdle B. (2013). Palmitoylethanolamide and stearoylethanolamide levels in the interstitium of the trapezius muscle of women with chronic widespread pain and chronic neck-shoulder pain correlate with pain intensity and sensitivity. Pain 154(9):1649-1658.
[4] Stensson, N., Ghafouri, B., Gerdle, B., & Ghafouri, N. (2017). Alterations of anti-inflammatory lipids in plasma from women with chronic widespread pain—a case–control study. Lipids Health Dis. 2017;16(1):112.
[5] Stensson, N., Ghafouri, N., Ernberg, M., Mannerkorpi, K., Kosek, E., Gerdle, B., & Ghafouri, B. (2018). The relationship of endocannabinoidome lipid mediators with pain and psychological stress in women with fibromyalgia: a case–control study. J Pain. 2018;19(11):1318-1328.
[6] Artukoglu, B.B., Beyer, C., Zuloff-Shani, A., Brener, E., Bloch, M. (2017). Efficacy of Palmitoylethanolamide for Pain: A Meta-Analysis. Pain Physician 20(5):353-362
[7] Paladini, A., Fusco, M., Cenacchi, T., Schievano, C., Piroli, A., Varrassi, G. (2016). Palmitoylethanolamide, a Special Food for Medical Purposes, in the Treatment of Chronic Pain: A Pooled Data Meta-analysis. Pain Physician 19(2):11-24.
[8] Cervigni, M., Nasta, L., Schievano, C., Lampropoulou, N., Ostardo, E. (2019). Micronized Palmitoylethanolamide-Polydatin Reduces the Painful Symptomatology in Patients with Interstitial Cystitis/Bladder Pain Syndrome. BioMed Research International:9828397. doi: 10.1155/2019/9828397
[9] Stochino Loi, E., Pontis, A., Cofelice, V., Pirarba, S., Fais, M.F., Daniilidis, A., Melis, I., Paoletti A.M., Angioni, S. (2019). Effect of ultramicronized-palmitoylethanolamide and co-micronized palmitoylethanolamide/polydatin on chronic pelvic pain and quality of life in endometriosis patients: An open-label pilot study. International Journal of Women’s Health 11:443-449.
[10] Alshelh, Z., Mills, E.P., Kosanovic, D., Di Pietro, F., Macey, P.M., Vickers, E.R., Henderson, L.A. (2019). Effects of the glial modulator palmitoylethanolamide on chronic pain intensity and brain function. Journal of Pain Research 12:2427-2439. doi: 10.2147/JPR.S209657.
[11] Chirchiglia, D., Paventi, S., Seminara, P., Cione, E., Gallelli, L. (2018). N-palmitoyl ethanol amide pharmacological treatment in patients with nonsurgical lumbar radiculopathy. Journal of Clinical Pharmacology 58(6):733-739.
[12] Cruccu, G., Stefano, G.D., Marchettini, P., Truini, A. (2019). Micronized Palmitoylethanolamide: A Post Hoc Analysis of a Controlled Study in Patients with Low Back Pain – Sciatica. CNS & Neurological Disorders – Drug Targets 18(6):491-495.
[13] Passavanti, M.B., Fiore, M., Sansone, P., Aurilio, C., Pota, V., Barbarisi, M., Fierro, D., Pace, M.C. (2017). The beneficial use of ultramicronized palmitoylethanolamide as add-on therapy to Tapentadol in the treatment of low back pain: a pilot study comparing prospective and retrospective observational arms. BMC Anesthesiology 17(1):171. doi: 10.1186/s12871-017-0461-9.
[14] Scaturro, D., Asaro, C., Lauricella, L., Tomasello, S., Varrassi, G., Letizia Mauro G. (2019). Combination of Rehabilitative Therapy with Ultramicronized Palmitoylethanolamide for Chronic Low Back Pain: An Observational Study. Pain and Therapy. doi: 10.1007/s40122-019-00140-9. [Epub ahead of print]
[15] Evangelista, M., Cilli., De Vitis, R., Militerno, A., Fanfani, F. (2018). Ultra-micronized Palmitoylethanolamide Effects on Sleep-wake Rhythm and Neuropathic Pain Phenotypes in Patients with Carpal Tunnel Syndrome: An Open-label, Randomized Controlled Study. CNS & Neurological Disorders – Drug Targets 17(4):291-298. doi: 10.2174/1871527317666180420143830.
[16] Steels, E., Venkatesh, R., Steels, E., Vitetta, G., Vitetta, L. (2019). A double-blind randomized placebo controlled study assessing safety, tolerability and efficacy of palmitoylethanolamide for symptoms of knee osteoarthritis. Inflammopharmacology 27(3):475-485.
[17] Semprini R, Martorana A, Ragonese M, Motta C. (2018). Observational clinical and nerve conduction study on effects of a nutraceutical combination on painful diabetic distal symmetric sensory-motor neuropathy in patients with diabetes type 1 and type 2. Minerva
Medica 109(5):358-362.
[18] Paladini, A., Varrassi, G., Bentivegna, G., Carletti, S., Piroli, A., Coaccioli, S. (2017). Palmitoylethanolamide in the treatment of failed back surgery syndrome. Pain Research and Treatment 2017:1486010.
[19] Woodhams, S.G., Chapman, V., Finn, D.P., Hohmann, A.G., Neugebauer, V. (2017). The cannabinoid system and pain. Neuropharmacology 124:105-120. doi: 10.1016/j.neuropharm.2017.06.015.
[20] Di Marzo, V., Melck, D., Orlando, P., Bisogno, T., Zagoory, O., Bifulco, M., Vogel, Z., De Petrocellis, L. (2001). Palmitoylethanolamide inhibits the expression of fatty acid amide hydrolase and enhances the anti-proliferative effect of anandamide in human breast cancer cells. The Biochemical Journal 358:249–255.
[21] Petrosino, S., Schiano Moriello, A., Cerrato, S., Fusco, M., Puigdemont, A., De Petrocellis, L. Di Marzo, V. (2016). The anti-inflammatory mediator palmitoylethanolamide enhances the levels of 2-arachidonoylglycerol and potentiates its actions at transient receptor potential vanilloid type-1 channels. British Journal of Pharmacology 173:1154–1162.
[22] Couch, D., Tasker, C., Theophilidou, E., Lund, J.N., O’Sullivan, S.E. (2017). Cannabidiol and palmitoylethanolamide are anti-inflammatory in the acutely inflamed human colon. Clinical Science (London, England) 131(21):2611-2626. doi: 10.1042/CS20171288.
[23] Huh, Y., Ji, R.R., Chen, G. (2017). Neuroinflammation, Bone Marrow Stem Cells, and Chronic Pain. Frontiers in Immunology 21;8;1014. doi: 10.3389/fimmu.2017.01014.
[24] Ji, R.R., Chamessian, A., Zhang, Y.Q. (2016). Pain regulation by non-neuronal cells and inflammation. Science 354(6312):572-577.
[25] Lambert, D. M., Vandevoorde, S., Diependaele, G., Govaerts, S. J., and Robert, A. R. (2001). Anticonvulsant activity of N-palmitoylethanolamide, a putative endocannabinoid, in mice. Epilepsia 42, 321–327. doi: 10.1046/j.1528-1157.2001.41499.x
[26] Gabrielsson, L., Mattson, S. & Fowler, C.J. (2016). Palmitoylethanolamide for the treatment of pain: pharmacokinetics, safety and efficacy. British Journal of Clinical Pharmacology 82, 932-942.