CBD & Bioavailability

How does it works?

Whether you are a new CBD user, or have been using CBD in one form or another for years already, one factor that plays a very large role in how CBD affects you is bioavailability. Phytocannabinoids, including CBD, originate from the botanical kingdom and stimulate your endogenous endocannabinoid system (ECS, for short). The ECS is a complex set of neurotransmitters, neuroreceptors, and cellular enzymes that help to maintain homeostasis in your body. In order to be effective, phytocannabinoids like CBD need to become available to your ECS.

Bioavailability refers to how much, and at what rate, a substance gets absorbed by your bloodstream. You may wonder how much of a CBD product is actually absorbed and used by your ECS. The answer depends largely on two factors, the type of CBD extract (isolate, full spectrum, broad spectrum, etc.) and the delivery method.

Bioavailability of CBD Tinctures

When CBD-rich hemp extract is taken sublingually, held beneath the tongue, or buccally, held between the cheek and gums, CBD has a bioavailability ranging from 13% to 35%. Holding an extract beneath the tongue or on the sides of one’s cheek for 10 to 60 seconds allows enough time for the CBD to be absorbed through the mucous membranes lining the mouth, and to quickly enter directly into the bloodstream. This method offers better bioavailability over oral ingestion since it doesn’t pass through the digestive system, thereby avoiding first pass metabolism, where cannabinoids get broken down by the liver. Since phytocannabinoids are fat soluble, there is evidence that suggests that using CBD in a saturated fat carrier oil, such as MCT oil (medium chain triglyceride oil) can increase the bioavailability. MCT’s are a type of dietary fat with a unique chemical structure compared to longer chain fats, which absorb easily in the body, providing fast energy and quick delivery of cannabinoids to the bloodstream and brain.

Bioavailability of CBD Edibles

Oral ingestion of CBD is another option, and is perhaps the most popular because it involves regular daily activities like eating food, drinking beverages, and swallowing vitamins. Absorption ranges vary widely between 4% to 20% for ingestion. When you orally ingest CBD edibles or supplements, the CBD must pass through your normal digestive and metabolic systems, which filter out a large portion of the CBD before it ever reaches your bloodstream. CBD’s solubility makes it challenging to get past these systems to your bloodstream. CBD is lipophillic, which means it combines with lipids and fat. With this in mind, the bioavailability of a CBD edible can be increased by consuming it with lipids, such as MCT oil or cacao butter. Combining CBD with these natural dietary fats and lipids makes the mixture even more lipophilic (fat-loving), driving absorption to the chylomicron-lymphatic absorption path, which increases the overall bioavailability versus absorption via the hepatic (liver) portal route (system for absorbing hydrophilic [water-loving] substances from the gut to the liver). In one study, consuming a standard breakfast one hour before consuming CBD capsules increased bioavailability.  This study demonstrates how combining CBD with lipid and fat rich foods helps increase the effectiveness of CBD through oral ingestion.  

 Edible options can also be enhanced by combining phytocannabinoids with other functional ingredients. Terpenes are a good example, they’re the natural compounds found throughout the botanical kingdom that help to stimulate the brain’s neurotransmitters. Black pepper, oregano, cinnamon, and clove all contain the terpene beta-caryophyllene, and are known to stimulate the CB2 receptors, which are the same receptors that phytocannabinoids bind to. Foods like galangal, maca root, and chocolate, inhibit fatty acid amide hyrolase (FAAH),which allows the “bliss molecule” known as Anandamide to prolong in your system. Anandamide is a powerful neurotransmitter that carries phytocannabinoids to the ECS receptor sites. Additionally, researchers have recently concluded that natural fats in chocolate facilitate a process called lipid micro-encapsulation. This protects the CBD molecules during digestion, resulting in larger quantities of CBD being delivered to your bloodstream. 

There are also some more cutting edge options that can be employed to increase the bioavailability of orally ingested products containing CBD, such as utilizing nanoparticle technology. Since humans are mostly made up of water, nutrients that are soluble (dissolvable) in water pass more easily to the bloodstream. Phytocannabinoids that are lipophilic (oil-based molecules that are not soluble in water), like CBD, have difficulty dissolving and absorbing in the body versus a water soluble nutrient. Nano-enhanced or biocellular micellization is a way of rendering the particle size of the CBD and other phytocannabinoids into a much smaller or even nano-particle size, then binding it to a liposome. Liposomes are small spherical vessels that transport substances into the body that prevent breakdown by stomach acid and facilitate quicker delivery and higher absorption into the bloodstream.

Bioavailability of CBD Topicals

Topical CBD products such as salve, lotion, cream, spray or roll-ons are best used for targeting specific localized issues on the body. CBD that is applied topically doesn’t actually enter into the bloodstream, so it is difficult to determine how much is absorbed.  Remember, bioavailability refers to how much, and at what rate, a substance gets absorbed by your bloodstream .  Transdermal products, which are often found in the form of patches, are the exception for topicals, as they employ technology for deeper sustained penetration that can reach the bloodstream.  Typically topicals do not go into the bloodstream though, and are instead absorbed into the skin’s surface, interacting with local cannabinoid receptors in the epidermis and subdermal areas.  CBD topicals can benefit from the addition of other therapeutic botanicals found to assist with reducing inflammation, soothing muscle pain, and nourishing the skin.