Benefits of CBD

In 2017, retail sales of hemp-derived CBD products reached an astounding $350 million; by 2020, CBD is projected to be a billion-dollar market.[1],[2] What exactly is CBD, and why has it taken the wellness world by storm? Read on to learn about the evidence-based health benefits of CBD and why liposomal formulations are the optimal delivery system for this potent healing compound.

What is CBD?

Cannabidiol (CBD) is one of over 100 compounds known as phytocannabinoids found in Cannabis sativa and a variety of other species distributed throughout the plant kingdom. CBD accumulates in Cannabis trichomes, small crystalline structures on the plant’s leaves and buds that serve as “factories” for a multitude of beneficial compounds and as a defense mechanism against pests and pathogens.[3]

Unlike its famous sister phytocannabinoid, tetrahydrocannabinol (THC), CBD is non-psychoactive. In fact, CBD attenuates several of the undesirable psychological effects of THC, including anxiety and paranoia.[4] A growing body of research also indicates that CBD is the dominant phytocannabinoid for creating healing states in the body.

CBD and the Endocannabinoid System

The endocannabinoid system (ECS) is a complex network of receptors and signaling molecules that regulate many aspects of our physiology, including appetite, cognition, immune function, inflammation, pain, and sleep. The ECS produces two endocannabinoids, anandamide and 2-arachidonoylglycerol, that interact with its G-protein-coupled CB1 and CB2 receptors. The ECS also harbors several enzymes that control endocannabinoid synthesis and degradation, including fatty acid amide hydrolase (FAAH).[5]

While THC directly interacts with CB1 and CB2 receptors, CBD’s relationship with the ECS is more complex. Rather than interacting directly with CB1 and CB2 receptors, CBD indirectly influences their activity by modulating their responsivity to endocannabinoids. CBD thus enhances endocannabinoid tone, improving the function of the downstream systems regulated by the ECS, including the central nervous system, gastrointestinal tract, and immune system.

CBD Effects Beyond the ECS

CBD’s effects are not limited to the endocannabinoid system; it also influences a variety of non-ECS signaling pathways and cell receptors.

Non-ECS Receptors and Signaling Pathways

CBD interacts with a wide variety of non-ECS signaling pathways and receptors, including the 5-HT1a serotonin receptor, peroxisome-proliferator-activated receptors (PPAR), TRP channels, the G-protein-coupled receptor GPR55, and the wnt-beta-catenin signaling pathway.[6],[7],[8],[9],[10] These interactions mediate CBD’s diverse array of physiological, effects ranging from antidepressant to analgesic actions.

Inhibition of endocannabinoid breakdown

CBD also inhibits the breakdown and reuptake of anandamide and 2-arachidonoylglycerol, increasing their levels in circulation and potentiating their natural anti-inflammatory and analgesic effects.[11]

Allosteric receptor modulation

CBD is an allosteric receptor modulator, meaning it can either amplify or reduce the responsiveness of receptors to their corresponding signaling molecules, resulting in an altered biological response.[12] For example, CBD acts as a negative allosteric receptor modulator at CB1 receptors, inhibiting the adverse effects of excessive CB1 stimulation such as anxiety, increased appetite, and paranoia.[13]

The Health Benefits of CBD

With all the attention CBD has received in the media in recent years, it has gained a reputation as a panacea. Are the purported health benefits of CBD too good to be true, or does it live up to the hype? A growing body of research indicates that CBD is indeed a remarkable healing compound! CBD’s impressive health benefits are attributed to its profound homeostatic effects on the neurological, endocrine, and immune systems.

Brain function

CBD offers an abundance of health benefits to the brain. It inhibits multiple processes involved in the development of neurodegenerative diseases, including glutamate excess, amyloid-beta-induced microglial cell activation, and tau hyperphosphorylation.[14],[15],[16]

CBD facilitates recovery from traumatic brain injury (TBI) by inhibiting neuroinflammation and central pain sensitization. It also increases levels of neuroprotective endocannabinoids, fortifying the body’s resistance against brain damage.[17],[18]

CBD has profound implications for mental health, alleviating depression and anxiety with efficacy equivalent to that of the pharmaceutical drugs ipsapirone and diazepam. It also shows promise in the management of PTSD, a notoriously difficult-to-treat condition, by potentiating neurological processes involved in the extinction of aversive memories.[19]

Sleep

The balancing activity of CBD on excitatory and calming neurotransmission gently induces deep, restorative sleep.[20] Unlike benzodiazepines and anti-anxiety drugs, it does not interfere with a healthy sleep-wake cycle or cause next-morning drowsiness.[21] CBD may benefit sleep the most when combined with a low level of THC.

Pain and Inflammation

CBD is a potent anti-inflammatory agent. It downregulates pro-inflammatory genes and upregulates anti-inflammatory genes, alleviating chronic neuropathic pain and osteoarthritic pain.[22],[23] It also reduces inflammation in the gastrointestinal tract, ameliorating symptoms of inflammatory bowel disease.[24]

Enhanced Bioavailability of CBD in Liposomes

While CBD is available in many forms, including tinctures, capsules, and sprays, its bioavailability is optimized when it is administered with lipids, or what is known as liposomal delivery.[25] There are certain liposomal formulations that deliver CBD and a spectrum of other beneficial hemp-based compounds in specialized nanoparticles that bypasses first-pass metabolism, thereby gaining immediate access to the lymphatic system and rapidly delivering the healing properties of CBD to the cells.

If you are looking to optimize your brain health, quench inflammation, and balance hormonal and immune activity, Cannabidiol is one nutraceutical you won’t want to miss out on! As our scientific understanding of CBD continues to grow, we may discover even more health benefits of this unassuming but potent healing compound! 

 

References

  1. “Total U.S. cannabidiol (CBD) consumer sales from 2014 to 2022 (in million U.S. dollars).” Statista. 2019. https://www.statista.com/statistics/760498/total-us-cbd-sales/.
  2. Borchardt D. Hemp cannabis product sales are projected to hit $1 billion in three years. Forbes. 2017. https://www.forbes.com/sites/debraborchardt/2017/08/23/hemp-cannabis-product-sales-projected-to-hit-a-billion-dollars-in-3-years/#6e354fe4474c.
  3. Andre CM, et al. Cannabis sativa: The plant of the thousand and one molecules. Front Plant Sci. 2016; 7:19.
  4. Niesink RJM, et al. Does cannabidiol protect against adverse psychological effects of THC? Front Psychiatry. 2013; 4:130.
  5. Ahn K, et al. Enzymatic pathways that regulate endocannabinoid signaling in the nervous system. Chem Rev. 2008; 108(5): 1687-1707.
  6. Resstel LBM, et al. 5-HT1A receptors are involved in the cannabidiol-induced attenuation of behavioral and cardiovascular responses to acute restraint stress in rats. Br J Pharmacol. 2009; 156(1): 181-188.
  7. O’Sullivan SE. An update on PPAR activation by cannabinoids. Br J Pharmacol. 2016; 173(12): 1899-1910.
  8. Muller C, et al. Cannabinoid ligands targeting TRP channels. Front Mol Neurosci. 2018; 11:487.
  9. Ryberg E, et al. The orphan receptor GPR55 is a novel cannabinoid receptor. Br J Pharmacol. 2007; 152(7): 1092-1101.
  10. Vallee A, et al. Effects of cannabidiol interactions with Wnt/β-catenin pathway and PPARγ on oxidative stress and neuroinflammation in Alzheimer’s disease. ActaBiochim Biophys Sin (Shanghai). 2017; 49(10): 853-866.
  11. Bisogno T, et al. Molecular targets for cannabidiol and its synthetic analogs: effect on vanilloid VR1 receptors and on the cellular uptake and enzymatic hydrolysis of anandamide. Br J Pharmacol. 2001; 134(4): 845-852.
  12. Tham M, et al. Allosteric and orthosteric pharmacology of cannabidiol and cannabidiol‐dimethylheptyl at the type 1 and type 2 cannabinoid receptors.
Br J Pharmacol. 2019; 176(10): 1455-1469.
  13. Straiker A, et al. Cannabidiol inhibits endocannabinoid signaling in autaptic hippocampal neurons. Mol Pharmacol. 2018; 94(1): 743-748.
  14. Martin-Moreno AM, et al. Cannabidiol and other cannabinoids reduce microglial activation In vitro and in vivo: relevance to Alzheimer’s disease. Mol Pharmacol. 2011; 79(6): 964-973.
  15. Janefjord E, et al. Cannabinoid effects on β amyloid fibril and aggregate formation, neuronal and microglial-activated neurotoxicity in vitro. Cell Mol Neurobiol.
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  16. Esposito G, et al. The marijuana component cannabidiol inhibits beta-amyloid-induced tau protein hyperphosphorylation through Wnt/beta-catenin pathway rescue in PC12 cells. J Mol Med (Berl). 2006; 84(3): 253-258.
  17. Belardo C, et al. Oral cannabidiol prevents allodynia and neurological dysfunctions in a mouse model of mild traumatic brain injury. Front Pharmacol. 2019; [online].
  18. Schurman LD, Lichtman LH. Endocannabinoids: A promising impact for traumatic brain injury. Front Pharmacol. 2017; 8: 69.
  19. Blessing EM, et al. Cannabidiol as a potential treatment for anxiety disorders. Neurotherapeutics. 2015; 12(4): 825-836.
  20. Shannon S, et al. Cannabidiol in anxiety and sleep: A large case series. Perm J. 2019; 23: 18-041.
  21. Linares IMP, et al. No acute effects of cannabidiol on the sleep-wake cycle of healthy subjects: A randomized, double-blind, placebo-controlled, crossover study. FrontPharmacol. 2018; 9:315.
  22. Mucke M, et al. Cannabis-based medicines for chronic neuropathic pain in adults. Cochrane Database Syst Rev. 2018; 3:CD012182.
  23. Philpott HT, et al. Attenuation of early phase inflammation by cannabidiol prevents pain and nerve damage in rat osteoarthritis. Pain. 2017; 158(12): 2442-2451.
  24. Swaminath A, et al. The role of cannabis in the management of inflammatory bowel disease: A review of clinical, scientific, and regulatory information: Commissioned by the Crohn’s and Colitis Foundation. Inflamm Bowel Dis. 2019; 25(3): 427-435.
  25. Zgair A, et al. Dietary fats and pharmaceutical lipid excipients increase systemic exposure to orally administered cannabis and cannabis-based medicines. Am J Transl Med. 2016; 8(8): 3448-3459.

 

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