LEARN

Administering CBD Through The Skin Can Bypass First-pass Metabolism of Cannabinoids

CBD (cannabidiol) is a cannabinoid that is present in high concentrations in the plant cannabis sativa. CBD is one of the 400+ different compounds present in the plant. It is also one of the 60+ cannabinoids found in the plant.

CBD’s popularity as a therapeutic drug has encouraged the creation of a range of CBD-based beauty and wellness products.

The prominence of CBD as a therapeutic drug is well-founded. There are many initial studies that support the potential of CBD as a therapeutic drug for many health issues. There is strong evidence that CBD can address childhood epilepsy efficiently. In particular, CBD is showing promising results for treating two of the most notorious forms of childhood epilepsy – the Lennox-Gastaut and Dravet syndromes.

The positive effects of CBD on the above syndromes were studied in some cases. It was found that CBD reduced the frequency of seizures, and in some cases stopped them altogether, in children suffering from childhood epilepsy.

CBD for Insomnia, Anxiety and Chronic Pain

CBD is also being used to address symptoms of insomnia and anxiety. When patients of insomnia used CBD, they slept better. They also stayed asleep for a longer time than they would do otherwise.

Another condition that CBD is helping address is chronic pain. A study on animal models showed that CBD could reduce inflammation and pain related to arthritis. CBD was administered on the skin of animals in this study.

There is also proof that CBD can reduce neuropathic and inflammatory pain. Neuropathic pain is caused by damage to the nervous system. Experts consider these two types of pain as one of the most difficult forms of chronic pain to treat.

By addressing even such pain effectively, CBD is proving to be one of the most promising therapeutic drugs. More studies are being carried out to understand the potential of CBD for therapy.

CBD is Non-Psychoactive

A key reason that has been encouraging researchers to continue studies on CBD is its non-psychoactive property. CBD, unlike THC (another cannabinoid found in sativa plant), does not cause a heightened state in the patient.

According to the World Health Organization, pure CBD has not been known to cause any health issues in people. There is also no proof to indicate that CBD promotes substance dependence in human beings.

CBD products are more popular than ever among public. The awareness that CBD can address symptoms without making you “high” is a major reason for the popularity.

Patients suffering from pain have a range of pain relief CBD products to choose from, to manage their symptoms. These products are available in many convenient forms. The list includes pain relief cream, pain relief spray, and pain relief roll-on.

Wellness product range includes body oil, recovery lotion, sleeping mask and more. Some product lines such as CBD Plus and CBD Must are highly research-based. In addition to pain relief and wellness products, these brands offer skin health improvement products. The skin range includes eye serum, glow oil, facial cream, anti aging facial serum, facial serum and face cream.

CBD Administration through Skin

Even though CBD is efficient in addressing a range of health conditions, poor bio-availability of the cannabinoid in oral administration prevents optimal utilization of CBD-based drugs. Bio-availability is the degree of ready availability of CBD to the body. A high bio-availability indicates that the drug is readily absorbed by the body and reaches the blood stream faster.

Study shows that CBD has very low bio-availability when administered orally. Researchers are now studying other methods of administering CBD to counter this challenge. Transdermal administration – administering CBD via the skin – is increasingly being seen as an efficient alternative of drug delivery.

Cannabinoids, including CBD are lipophilic

by nature. This means, CBD dissolves faster in fats than in water. This nature makes the cannabinoid apt for transdermal delivery.

Why CBD Bio-availability is Important?

• Good CBD bio-availability is important for the formulation to perform its intended purpose . A CBD drug is more efficient with greater bi-availability.
• Low bio-availability increases drug wastage. Poor bio-availability causes only a small amount of CBD to reach the patient’s body. In fact, taking CBD orally, or by inhaling, can cause 98% of the ingredients of a CBD formulation to go unused by the body.
• CBD’s dosage depends on bio-availability. Poor bio-availability of oral CBD products results in an increase of dosage. CBD formulation is not made available to the body as it needs to be, to produce results. As a result, dosage has to be increased significantly.
• Poor bio-availability makes it difficult for health professionals to prescribe accurate dosage for the patient. This inability makes medical practitioners wary of the drug even though CBD has proved to be a safe and effective medicine in various cases.
• Patients fail to derive the true intended value of CBD drugs due to the poor bio-availability factor.

How CBD Delivery through the Skin (Transdermal Delivery) Works?

In transdermal CBD delivery, CBD formulation is introduced into the body through the skin. The skin serves as an effective medium for transdermal delivery because of its large surface area. There is a lot of space for the CBD drug to be infused into the body through the skin.

CBD’s administration through skin is a painless form of delivering the drug. CBD-based drug formulation is applied on the skin for systemic absorption into the body. Systemic absorption is a method in which CBD is made available to the whole body (instead of one single part) by infusion into the circulatory system.

CBD is applied on healthy skin in transdermal method. When applied this way, the formulation enters deep into the skin, passing through its epidermal and dermal layers. The formulation does not accumulate in the dermal layer though. Upon reaching the dermal layer, CBD becomes ready for absorption into the entire body.

Benefits of CBD Delivery through Skin

• Transdermal delivery is a non-invasive method, which endears the procedure to patients with an aversion for needles.
• With the largest body organ – the skin – as its medium, transdermal delivery gives generous drug administration space for healthcare providers. Patients can use any location on their skin for placement of CBD formulations.

Transdermal formulations are mostly available as patches, which are convenient to use. Patients need to pull off the adhesive layer to stick the patch anywhere on the skin. Patches are applied on the wrists, ankles and neck, and other areas where veins are nearer to the skin. Doing so makes drug absorption into the blood stream faster.

• CBD delivery through the skin ensures that the movement of the drug in the body is consistent without any major dosage peaks. As a result, the risk of harmful drug-peaking side effects is minimized.
• Delivery through the skin makes CBD available to the body for a longer duration. This increase in duration decreases the need for frequent dosing.
• This method of delivery through skin helps maintain uniform plasma levels in the body. Uniform plasma levels are important to ensure efficient drug functioning and reduced side effects.

Transdermal delivery helps maintain uniform plasma levels till the last segment of the dosing interval ends. As a result, drug efficiency is improved and side effects are minimized. Oral CBD forms are not capable of maintaining such uniform plasma levels. The levels decrease as the dosage progresses.

The vital benefit of transdermal delivery of CBD is improved bio-availability, which makes this method more efficient than oral and inhalation delivery routes.

First Pass Effect Decreases Bio-Availability of CBD in Non-Transdermal Administration

First Pass effect is a bodily reaction to drugs. In the First Pass process, the drug undergoes metabolism (the drug is broken down into simpler ingredients for easy elimination from the body) at a certain location in the body.

Metabolism decreases the concentration of the CBD formulation that enters the body. The drug becomes lesser in volume when it reaches the part of the body where it is required to act. If the drug was meant for systemic release into the body, then the amount dispersed becomes lesser because of the First Pass effect.

The metabolism site for the First Pass effect is usually the liver. Cannabinoids, including CBD, need to pass through the liver and undergo metabolism before they serve their intended purpose. This is because the enzymes that are essential for drug metabolism are present in the liver.

But First Pass metabolism can also occur in the lungs, gastrointestinal tract, or in other tissues that are capable of such metabolic activity.

Oral CBD products fail to deliver their potential therapeutic efficiency due to this First Pass phenomenon.

Another route for CBD administration – inhaling – does offer better results than oral CBD with regard to bio-availability. But this method too comes with its own drawbacks.

When inhaled, CBD reaches the circulatory system through the lungs. CBD is then pushed into the blood stream. But CBD can still be absorbed from the blood stream and moved to fat cells for storage. This process again reduces the amount of CBD that reaches the target site or the blood stream.

A study based on animal model supports the low bio-availability of CBD when administered orally. Oral bio-availability was in the range of 13 to 19% in the study. The study also found that CBD underwent extensive First Pass metabolism. The elimination of the resultant metabolites was found to be through the kidneys.

In another study, it was found that oral administration of CBD resulted in only 6% absorption into the body. The study cited CBD’s poor water solubility and its tendency to undergo extensive First Pass metabolism as reasons for its poor bio-availability.

Transdermal administration or administering CBD through the skin offers a precision method for CBD administration.

CBD Delivery through Skin Improves Bio-Availability by Preventing First Pass Metabolism

Transdermal delivery helps overcome this drawback of CBD’s First Pass Effect by preventing the process altogether. In transdermal drug delivery, cannabinoids, and in particular CBD, pass through the skin. But CBD does not reach liver or the gastrointestinal tract as it usually does. As a result, the occurrence of First Pass effect is prevented.

As CBD does not undergo First Pass metabolism, the time taken for breaking down the cannabinoid, is reduced.

Some transdermal delivery systems use membranes that facilitate improved movement of cannabinoids within the body. With improved movement, chances of fat cells absorbing CBD from the bloodstream are minimized.

While administration of CBD in the transdermal way is effective and faster, skin resistance is a major challenge.

The top layer of the skin, called the stratem corneum, acts as a natural barrier, preventing foreign substances from entering the body. This layer consists of a lipid matrix, which stops most compounds from passing through the skin.

This challenge is overcome through the use of permeation enhancers. These substances temporarily increase the penetration capability of the skin so that the CBD formulation is well-absorbed.

Substances that can serve as permeation enhancers are selected carefully. They are tested for their compatibility with the CBD formulation. They undergo rigorous testing for indications of any unfavorable pharmacological activity within the body.

Other testing parameters include solubility, chemical and physical stability, and lack of taste, color and odor. These substances must not cause any damage to the skin’s original characteristics. The skin usually retains its natural barrier mechanism once the enhancers are removed.

Permeation enhancers are non-toxic and without side effects.

CBD Patches – A Popular Transdermal CBD Product

Given the efficacy of CBD delivery through skin, there are more transdermal CBD products being made available in the market. Transdermal CBD patches are a popular mode of transdermal delivery.

These patches are very much like nicotine patches or patches for birth control. They are convenient to use and discreet as well.

CBD patches contain the formulation in an isolated form of an oil, gel or solution. The molecules of the formulation get activated when the patch is fixed to the skin. As the patch is high in CBD content, the particulates within show a tendency to move to a low-CBD area, which is your skin. This difference in CBD content activates the movement of CBD in your body.

CBD patches can be matrix or reservoir type.

Matrix CBD patches facilitate continuous CBD delivery to the skin. Matrix CBD patches consist of an adhesive polymer matrix layer, which holds the formulation. The matrix layer is responsible for releasing CBD steadily into the skin.

Dosage of drug through matrix CBD patches is based on the quantity of formulation in the matrix layer and the area of the skin covered by the patch.

A reservoir patch contains a membrane, which controls the rate at which CBD is delivered into the skin. If you are looking for greater control on dosage, then a reservoir patch is the best alternative.

In Conclusion

Experts believe transdermal drug delivery to be an effective alternative to oral administration of cannabinoids, including CBD. The major benefit of precise dosage delivery is what sets transdermal delivery apart from other routes of CBD administration. This ability of transdermal delivery is expected to encourage more CBD-based product lines aimed at making people’s lives better and ailment-free.