CBD Dosage forms
The statements regarding CBD have not been evaluated by the Food and Drug Administration.
CBD is not intended to diagnose, treat, cure or prevent any disease.
CBD has become extremely prevalent among tens of millions of Americans. This has happened largely without the blessing or guidance of the FDA. Because of the unique scenario in which the CBD industry finds itself, people purchase CBD for a wide variety of reasons, and there are no empirically determined dosing recommendations. In fact, because the FDA hasn’t approved the off-label use of CBD, it’s federally illegal for a CBD manufacturer or seller to make dosing recommendations.
One caveat to this situation is the FDA-approved usage of Epidiolex®, which is produced by GW Pharmaceuticals and indicated for several childhood seizure disorders. Because this drug – of which cannabidiol is the only active pharmaceutical ingredient – is FDA-approved, and therefore has specific manufacturer-determined doses, the rest of the CBD industry has loosely taken cues in formulating the concentration of their products, without making direct dosing recommendations for users.
While specific measured dosing guidelines cannot be established for off-label or OTC use of CBD, the bioavailability of different dosage form of CBD nonetheless impacts the relative amount of CBD required for each dosage form to achieve the same blood levels of CBD.
NOTE: THIS PAGE IS NOT CALLED DOSING! ANY DOSING CHARTS YOU FIND ONLINE ARE NOT TO BE REGARDED, AS THE FDA AND MEDICAL COMMUNITY HAVE NOT YET ESTABLISHED DOSING GUIDELINES.
Sublingual CBD oils have been until recently the most popular dosage form of CBD. Sublingual CBD products became the most popular because they historically had greater bioavailability than other ingestible dosage forms, but with the advent of patented water soluble oral dosage forms now available, there is competition. Since SL CBD enters the bloodstream directly instead of passing through the digestive tract, It was thought that more CBD is available to be used by the body. Sublingual CBD still achieves only 40-50% bioavailability, which is less than ideal. For that reason, innovative delivery methods have been sought after for more than a decade.
Oral CBD, of course, refers to CBD taken by mouth. However, there are several hurdles to achieving an effective blood level of CBD via the oral route due to extensive first-pass metabolism. For that reason there are several subcategories of Oral CBD in addition to the naked CBD molecules suspended in some lipophilic liquid vehicle within a softgel, or infused into edible products. Molecules comprising vesicle vehicles capable of carrying CBD through the digestive tract are known as mesogens, which are amphiphilic, having both hydrophilic and hydrophobic domains.
CBD delivered with no molecular vehicle
CBD is lipophilic, and therefore hydrophobic. It is not soluble in water or the gastric milieu, and therefore does not readily transit the gastrointestinal wall and continue on to the liver. Furthermore, any CBD that does make it to the liver is extensively broken down via first pass metabolism. Both of these steps result in a minuscule fraction of ingested CBD reaching the systemic bloodstream.
Liposomal or micellar CBD
Liposomal CBD – sometimes referred to as “Nano CBD” or “water soluble CBD,” was one of the first methods to emerge which improved the bioavailability of CBD taken orally. Liposomal drug delivery has been used successfully with several lipophilic legend drugs, including doxorubicin and amphotericin. The successful use of liposomal delivery of these drugs encouraged researchers to consider the use of liposomal technology in the delivery of CBD, which shares the lipophilic characteristic of the two drugs mentioned above.
Liposomal drug delivery involves the use of amphiphilic molecules and emulsifiers, such as lecithin and other fatty acid-derived mesogens, to envelope the CBD molecule and protect it as it passes through the digestive tract. There are two primary forms of amphiphilic mesogens utilized to achieve this, including liposomes and micelles.
A liposome (in an aqueous environment) is a bubble consisting of a bilayer of the amphiphilic molecule, with the hydrophilic domains of the molecules constituting both the outer and inner surfaces of the vehicle membrane. A micelle consists of only one layer of amphiphilic mesogen, with the hydrophilic domain constituting the outer surface of the membrane and the hydrophobic domain constituting the inner surface.
Due to the hydrophilic nature of the outer surface of these structures, both are soluble in aqueous environments, allowing them to pass through the digestive tract and into the bloodstream with ease. Lipophilic drugs like CBD associate with the hydrophobic domains of these structures which protect it from the hydrophilic outer environment. Liposomes carry CBD within the membrane bilayer itself, and micelles carry CBD in the lumen filling the inner volume of the structure.
This is effective for delivering CBD ingested orally into the bloodstream, but it is expensive to produce and also moderately unstable if stored for long periods of time. Furthermore, the structures themselves are 100-1000 nanometers in diameter, which is relatively large for entering the bloodstream via the GI tract.
Given these facts, there still exists an impetus to establish a more efficient method of delivery.
Lyotropic liquid crystalline CBD
Lyotropic liquid crystalline delivery vehicles for CBD are very similar to liposomal structures, with a few key differences. The term lyotropic is used to describe amphiphilic substances with two key characteristics.
- Lyotropic vehicles are self-assembling; they don’t require expensive sonication.
- Lyotropic vehicles have a much smaller diameter than liposomal structures.
You can read more about this new technology on our What’s New page.
Topical CBD delivery systems are different from all other dosage forms in that only a very small portion of their lipophilic and hydrophobic active ingredient achieves systemic circulation. This makes them a poor choice for many indications of CBD, but a superlative choice for other targets, namely the skin, joints, soft tissue, and muscle.
Due to its lipophilic nature, CBD gravitates toward fatty tissue and avoids aqueous environments, relegating it only to target cells in the area adjacent to its site of application. The increased concentration of active ingredient delivered to the target not only improves the effectiveness of the drug, but also allows for a lesser absolute quantity required to achieve the same concentration of active ingredient at the target site.
Ingestible CBD products are favorable for the majority of end users, but inhalable CBD products exhibit the highest bioavailability because of the absorption efficiency of the alveoli. However, many users are averse to using inhalable products because of their association with smoking. In addition, inhalable products contain substances in addition to CBD which can irritate the respiratory tract, as well as cause unwanted systemic side effects. Still, many users prefer this method of delivery in spite of its appropriateness, or lack thereof, in independent pharmacies.