Topicals: Healing Without a High

Pain and inflammation are inconvenient at best, and disabling at their worst. They disrupt our lives and rob us of our ability to thrive. Cannabis-infused topicals have proven to be effective against these disruptions without the often unwanted effects of other delivery methods, like edibles and inhalants.

We each possess an intricate network of receptors and mechanisms that regulate both our nervous system and immune functions – the Endocannabinoid System (ECS). This system can be found in and activated from nearly every nook and cranny of the body, including the skin.

Of course, bodies aren’t perfect. Any number of things can go awry within this primary regulatory system. Cannabis can help. With infused topicals, cannabis can help supplement and control deficiencies and abnormalities within the cutaneous ECS without risk of intoxicating effects.

Healing without a high

Cannabis-based topicals can provide real, lasting, and near immediate therapeutic support without intoxication because they engage with both cannabinoid receptors (i.e. CB1 and CB2) and other mechanisms (i.e. TRPV1, GPR55) found within the epidermis, and not much deeper. Both scientific and anecdotal evidence suggests that topically applied cannabinoids, like THC, cannot easily pass through this outermost layer of the skin without the support of a transdermal delivery system or the presence of mucous membranes, like those in the mouth.

So many choices!

There is an ample assortment of topical products on the market these days. Creams and lotions, balms and salves, oils and massage bars, all containing unique cannabinoid ratios, often mix in aromatherapeutic elements (i.e. lavender, arnica, menthol, bergamot) that also play a role in healing and relief by engaging receptors in the skin. The choices can be overwhelming!

In the end, each of the plant-based cannabinoids we will discuss has demonstrated therapeutic promise in topical treatment and researchers continue to discover revolutionary therapeutic possibilities every day.

Keep in mind, while many of the products you’ll find on the shelves may provide some sense of relief, one might find a little experimentation necessary to discover what works the best for each exceedingly unique individual. Safe and beneficial ingredients, application method and texture (especially absorbability), and scent preference should also be considered when choosing a topical.

THC, CBD, & THCA: the primary players in topicals today

THC

THC is the cannabinoid with which people are most familiar. Taken internally, it’s the primary compound in cannabis that creates intoxication. Topically, it doesn’t. THC can be used to treat a range of inflammatory skin conditions. It can reduce swelling, alleviate allergic reactions, and greatly ease pain and inflammation through site specific application without having to wait for the effects, as with oral ingestion. It can even play a role in the apoptosis (cell death) of carcinomas without harming healthy cells.

CBD

CBD is the darling of cannabis consumption these days. Its benefits are seemingly endless. While CBD hasn’t shown a particularly strong affinity for our primary cannabinoid receptors (CB1/CB2), at least in the absence of strong binders like THC, studies have found that it does work independently through peripheral pathways, both directly and indirectly, many of which can be found within the cells of our skin. TRPV-1, also known as the ‘vanilloid’ receptor, is one of those binding sites with great therapeutic potential, including regulating inflammation and mitigating the sensation of pain.

In tandem with THC, CBD can more effectively engage with CB1/CB2 receptors. Once THC activates, CBD can latch on, modulating the effects of the THC,  and thereby engaging the receptor as a whole, more completely.  This is why you’ll often hear that a “1:1”, or equal ratio of THC to CBD, can be more effective because it hits a wider variety of targets within our cells. Additionally, CB1 and TRPV-1 have been found in cohabitation on skin sensory neurons, suggesting synergistic benefits.

THCA

THCA is the non-intoxicating, acidic precursor to THC (delta-9), found in cannabis before it has been ‘activated’ by heat, light, or time. That being said, it is not, in fact, pharmacologically inactive.

Researchers have argued whether or not THCA effectively binds to CB1/CB2 receptors. Some studies have demonstrated proof of binding, while others have chalked up those effects to the instability of the THCa molecule creating THC, even within lab settings. This instability can be mitigated through oil-based infusions.

Some research has also argued that that the lack of intoxication associated with THCA is proof that it doesn’t have any great fondness for CB1, while others see this as a reason to better understand the differences between CB1 receptors in the Central Nervous System (CNS) and those within the peripheral tissues, like the skin. In fact, research has suggested that THCA taken internally has a greater interest in peripheral receptors than those found in the CNS. If this is the case, it makes sense that THCA works on dermal sites.

Additionally, THCA engages a number of other receptors and pathways within the skin. For instance, it is TRPM-8’s most potent connector, with therapeutic potential against malignant melanoma. And, again, we see the vanilloid receptor, TRPV-1, play an active role in the ability of THCA to relieve pain and inflammation. These TRP-family receptors, as well as a the therapeutic potential of cannabinoids in other enzymatic inhibition and activation, will likely be explored at great length in the years to come.

Regardless of what science has or has not yet discovered in regards to the mechanisms by which cannabinoids work within the skin, the anecdotal evidence is clear: topicals can work.

Dosing

With topicals, it’s all about front-loading applications. Just as you would apply a prescription topical, guidelines for dosing are generally 2-3 times per day, at least at the beginning. Anecdotal evidence demonstrates that many are able to scale-back doses as time passes, but it’s good practice to extend application until well after symptoms have resolved. Much as we do with doctor-prescribed medications. And, again, because there is no intoxication involved, topical cannabis has not shown to create any sense of over-medication, even with heavy use.

Topicals may improve:

Pain, inflammation, itch, arthritis, psoriasis, acne, headaches, migraines, cramping, tension, stiffness, bruising, wound recovery, tumor growth, basal and squamous cell carcinomas and melanoma, neuropathic pain, nerve injury, seizure, unwanted hair growth and follicular conditions like Alopecia, dry skin, dermatitis, systemic sclerosis, hormone regulation (i.e. Vitamin D family), and other cutaneous malignancies.

Products we carry:

Empower

Physic

Peak

Hana Medicinals

Sacred Herb Medicinals

Andrea Sparr-Jaswa, co-director of education

Resources:

1. LI S-S, WANG L-L, LIU M, et al. Cannabinoid CB2 receptors are involved in the regulation of fibrogenesis during skin wound repair in mice. Molecular Medicine Reports. 2016;13(4):3441-3450. doi:10.3892/mmr.2016.4961.

2. Caterina MJ. TRP Channel Cannabinoid Receptors in Skin Sensation, Homeostasis, and Inflammation. ACS Chemical Neuroscience. 2014;5(11):1107-1116. doi:10.1021/cn5000919.

3. Malfitano AM, Basu S, Maresz K, Bifulco M, Dittel BN. What We Know and Don’t Know About the Cannabinoid Receptor 2 (CB2). Seminars in immunology. 2014;26(5):369-379. doi:10.1016/j.smim.2014.04.002.

4. Mariam Alaverdashvili & Robert B. Laprairie (2018) The future of type 1 cannabinoid receptor allosteric ligands, Drug Metabolism Reviews, 50:1, 14-25, DOI: 10.1080/03602532.2018.1428341

5. Eric A Voight & Michael E Kort (2010) Transient receptor potential vanilloid-1 antagonists: a survey of recent patent literature, Expert Opinion on Therapeutic Patents, 20:9, 1107-1122, DOI: 10.1517/13543776.2010.497756

6. McPartland JM, MacDonald C, Young M, Grant PS, Furkert DP, Glass M. Affinity and Efficacy Studies of Tetrahydrocannabinolic Acid A at Cannabinoid Receptor Types One and Two. Cannabis and Cannabinoid Research. 2017;2(1):87-95. doi:10.1089/can.2016.0032.

7. Moreno-Sanz G. Can You Pass the Acid Test? Critical Review and Novel Therapeutic Perspectives of Δ9-Tetrahydrocannabinolic Acid A. Cannabis and Cannabinoid Research. 2016;1(1):124-130. doi:10.1089/can.2016.0008.

8. De Petrocellis L, Ligresti A, Moriello AS, et al. Effects of cannabinoids and cannabinoid-enriched Cannabis extracts on TRP channels and endocannabinoid metabolic enzymes. British Journal of Pharmacology. 2011;163(7):1479-1494. doi:10.1111/j.1476-5381.2010.01166.x.

9. Jorge, Liliana & C Feres, Caroline & Ep Teles, Vitor. (2011). Topical preparations for pain relief: Efficacy and patient adherence. Journal of pain research. 4. 11-24. 10.2147/JPR.S9492.

10. Cairns, B.E.. (2009). Peripheral Receptor Targets for Analgesia: Novel Approaches to Pain Management. 10.1002/9780470522226.
11. Tubaro, Aurelia & Giangaspero, Anna & Sosa, Silvio & Roberto, Negri & Grassi, Gianpaolo & Casano, Salvatore & Della Loggia, Roberto & Appendino, Giovanni. (2010). Comparative topical anti-inflammatory activity of cannabinoids and cannabivarins. Fitoterapia. 81. 816-9. 10.1016/j.fitote.2010.04.009.

12. Ruhaak, Lucia & Felth, Jenny & Christina Karlsson, Pernilla & Rafter, Joseph & Verpoorte, Robert & Bohlin, Lars. (2011). Evaluation of the Cyclooxygenase Inhibiting Effects of Six Major Cannabinoids Isolated from Cannabis sativa. Biological & pharmaceutical bulletin. 34. 774-8. 10.1248/bpb.34.774.

13. Peppin JF, Albrecht PJ, Argoff C, et al. Skin Matters: A Review of Topical Treatments for Chronic Pain. Part Two: Treatments and Applications. Pain and Therapy. 2015;4(1):33-50. doi:10.1007/s40122-015-0032-z.

14. Tüting, T., & Gaffal, E. (2017). Regulatory Role of Cannabinoids for Skin Barrier Functions and Cutaneous Inflammation. In Handbook of Cannabis and Related Pathologies (pp. 543-549).

15. Pertwee, Roger G. Targeting the endocannabinoid system with cannabinoid receptor agonists: pharmacological strategies and therapeutic possibilities. Phil. Trans. R. Soc. B 2012 367 3353-3363; DOI: 10.1098/rstb.2011.0381.

16. Mounessa, Jessica S. et al. The role of cannabinoids in dermatology. Journal of the American Academy of Dermatology , Volume 77 , Issue 1 , 188 – 190