BIO-AVAILABILITY: WHY NEARLY ALL YOUR CBD IS USELESS

Actually, CBD is a long way from useless, but most likely nearly all that you may be consuming is! 

 

 

So, like millions of others you are taking CBD, that’s great, but don’t for a moment think that all the CBD oil that you consume is being put to positive use by your body, it’s genuinely not as straight forward as that. How effective your body’s interaction with CBD is, depends on many factors and it is probably more complicated than you would imagine.

But if you knew that maybe only 6% of your CBD will actually enter your bloodstream and get to do the job that you are taking it for, would you still be as likely to buy it?

In this blog, we look further into the properties of cannabinoids like CBD, optimal dosing and why benefiting from CBD is not just as simple as taking it.                                                                                                                            

It is difficult to get CBD into the body 

One of the first things to know about cannabidiol (CBD), more so than THC, is that it is actually really difficult to get it absorbed into the body, if you take it orally. For a start, cannabinoids like CBD are hydrophobic (water hating) and are lipophilic (lipid loving) molecules and so do not want to mix with water.  As we are 60-70% water, this is something of a problem in getting the active CBD compounds to our signaling pathways.                                                                                           

Pure CBD is bi-phasic

Like any therapeutic or pharma medicine, taking the right dose is of paramount importance for its effectiveness and this is most definitely true of single molecule cannabinoids like CBD isolate.

Take too little and there is no effect at all, take too much and the benefits can rapidly decrease. Alcohol is biphasic, one too many and you can soon go from having a good time to a bad one (so we have been told). 

Interestingly, when you take an extract (CBD with other components), you get a dose response curve that’s more of a steady slope upward, rather than bell shaped; in other words, you have benefits no matter the dose and you don’t get that drop-off at higher and lower doses.                                                                                          

Dosing - It's not long lasting 

Swallowing a single, large dose (macro-dose), may be ultra-convenient, but it puts the system under pressure to process and metabolise all that CBD and as a result it may overwhelm your endo-cannabinoid system(ECS) and not have the chance to be put to its desired use.

Worthy of note also, is that the peak effects will last for only 3-4 hours and so a single macro-dose may not be sufficient if you are experiencing significant fluctuations in your symptoms.

This is why cannabinoid therapy is most effective in much smaller and more frequent doses taken throughout the day (micro-dosing). This is far easier and more convenient with some consumption routes compared to others; by vaping, for example, you can micro-dose with a few milligrams and because the effects are near instant, you can more easily find your sweet spot and maintain that on an ongoing basis. Gummies on the other hand, may taste good and you will get a fixed dose, but it is impossible to get the same level of control over your experience.                                                                                                              

Single molecule or whole plant?

The Cannabis plant contains over 700 known constituents^[1], CBD being just one of them and depending on the extraction techniques and refining processes applied, the resulting product will generally fall into one of the following categories:

Full spectrum extract: contains the full array of compounds produced by the plant (CBD, THC and other cannabinoids, terpenes etc.). In the UK, legal CBD items can only contain 1mg of THC in the whole product, which is not enough to have any effect.  

Broad spectrum extract: contains the full array of compounds produced by the plant, but with THC removed.

CBD isolate: contains only pure CBD (99%+), with all other compounds having been removed.                                                                                                         

Entourage Effect synergy 

CBD isolate powder is produced on an industrial scale and being by far the cheapest and most stable source of CBD, it’s commonly found in everyday products like edibles and vape in particular.

Whilst CBD has its own recognised properties, twenty years of research suggests that when it is taken alongside other cannabinoids and terpenes also present in the Cannabis plant, they display a therapeutic synergy dubbed the “entourage effect”^[2].

This multiple compound synergy is not available when taking single molecule products, which means some of the most powerful and potent properties of the plant are going to be lost if your CBD is from isolate.                                                                          

Raw material & manufacturing 

High quality raw material, impeccable and meticulous extracting and refining techniques, state of the art engineering and rigid quality control will all impact on the quality of your CBD. It’s essential you are starting out with the best possible product, that’s backed up by comprehensive laboratory tests.                                      

Delivery & bio-availability 

Finally and of vital importance is how you choose to consume your CBD, as this will have the single biggest impact on how effective your CBD interaction is going to be. This is because of the difference in bio-availability (BA) afforded to each delivery method.

BA refers to how much of a given substance is absorbed into your bloodstream and is made available for use. Your body can never utilise 100% of any given compound, some will always be lost. 

When cannabinoids and terpenes are consumed orally, which is how people tend to take their CBD, absorption is slow, erratic and variable with a BA estimated to be just 6%^[3]. Typically, onset time is one to two hours, but can be as much as six. 

The reason for this loss and delay is that a compound taken orally has to go through the entire digestive system before it gets metabolised in the liver, during this time the vast majority of any cannabinoids are degraded before they even have a chance of entering the bloodstream^[4].

This is known medically as the first pass effect and all orally consumed CBD has this fate, giving it the lowest BA of any delivery system, however it may last the longest in the body.                                 

Topicals

The use of plant preparations applied direct to the skin is as old as time and indeed research has shown that a plant’s terpenes can readily cross the skin's barrier. The same cannot, unfortunately, be said for CBD, a resinous molecule, which can’t penetrate through the multiple, dermal layers so easily and will not be able to make its way into the bloodstream when applied to the skin.

That is not to say massaging a problem joint or muscle with the eucalyptol, menthol and camphor terpenes that are most likely in any topical CBD balm will not provide some relief.                                                                                                               

Inhalation - Optimal delivery 

By far the most efficient and effective way of consuming cannabinoids and terpenes is by inhalation, where BA can hit 60%^[5], and the effects are almost instant. This is because the plant molecules rapidly enter the blood stream directly from the lungs, thus avoiding the digestive system and first past metabolism. In this way much less CBD is lost and far more gets through to the endocannabinoid system, other key receptors and messaging systems throughout the body^[6].                               

Bio-availability will determine the real price of your CBD 

Because of the differences in BA, your chosen consumption method will have a direct impact on how much you ultimately have to pay per milligram of useable CBD. For example, a 10mg gummie or oil dose will likely deliver less than 1mg of useful CBD and if a product has only 10% BA, you’re essentially paying six times more for your CBD than if you used a product which is at 60% BA.                                                                                                           

CBD product	Bioavailability	Onset to peak (mins)
Gummies/Edibles	6%	60 to 240
CBD oil	10%	60 to 120
Distillate inhalation	60%	1 to 10

As previously discussed in this blog, there are numerous factors that can affect your CBD experience, but nothing has more impact on a product’s bio-availability, than how it’s taken. It’s one subject that many CBD oil brands tend to gloss over, maybe because they know nearly all their CBD will ultimately go to waste, but now so do you!

And it’s a subject that’s worth thinking about when deciding on your own CBD products, including their efficacy and ultimate cost, otherwise you may well find you are, quite literally, just pissing it all away.                                                   

NECTR is a highly effective way to benefit from CBD 

We designed our products with all of the above and much more in mind. Our functional, botanical vapour cartridges are not only the most effective and bio-available way to maximise your body’s uptake of cannabinoids, but they deliver individual effects in an instant.

 

 

References

[1] Backes M – Interview, Future Cannabis Project (2020).
[2] Russo E - Taming THC: Potential cannabis synergy and phytocannabinoid-terpenoid entourage effects, British Journal of Pharmacology (2011).
[3] The World Health Organisation - Cannabidiol (CBD): Critical Review Report (2018).
[4] Lucas C - The pharmacokinetics and the pharmacodynamics of cannabinoids, British Journal of Pharmacology (2018).
[5] Bruni N et al - Cannabinoid delivery systems for pain and inflammation treatment, Molecules (2018).
[6] Russo E et al - Agonistic properties of cannabidiol at 5-HT1a receptors, Neurochemical Research (2005).