CBD the Hydrophobic -Mechanisms behind the absorption of CBD-

When discussing how CBD works in the body, it’s essential to understand the principles of?lipophilicity?and?hydrophilicity—two fundamental properties that govern how substances interact with fat and water-based environments in the body.

Lipophilicity?is derived from two Greek words:?lipos, meaning ‘fat’, and?philia?, meaning ‘love’ or ‘friendship.’ A?lipophilic substance is ‘fat-loving,’ meaning it dissolves well in fats and other lipid-based substances like oils. Substances with this property, such as CBD, mix readily with oils but struggle to dissolve in water. Imagine pouring oil into a glass of water—it doesn’t mix, and instead, the oil floats on top, showing its strong affinity for fats and its aversion to water.

In contrast,?hydrophilicity?comes from?hydro?, meaning ‘water’, and?philia?, meaning ‘love.’?Hydrophilic?substances are ‘water-loving,’ meaning they dissolve well in water-based environments like salt or sugar dissolving easily in a glass of water. Hydrophilic substances mix well in water but not in oils, demonstrating the opposite behaviour of lipophilic substances.

CBD, or cannabidiol, is a highly?lipophilic?molecule. This means it dissolves easily in fats but does not mix well in water-based environments, like most of our body fluids. As a result, CBD struggles to dissolve in water-based products like drinks or tinctures unless specific steps are taken to adjust the formulation. Without these adjustments, the CBD would remain separate from the water and reduce the product’s effectiveness.

This lipophilic nature of CBD has significant implications for how it is absorbed, distributed, and eliminated by the body. Because CBD loves fats, it easily integrates into fatty tissues but faces challenges when it comes to entering the bloodstream, especially when consumed orally. The lipophilicity of CBD not only influences its bioavailability (how much of the substance can be absorbed by the body) but also its distribution and the rate at which it is eliminated from the body.

Challenges of Absorbing CBD: The Role of Lipophilicity

When CBD is consumed orally, such as in oils or capsules, its lipophilic nature makes it difficult to enter the body’s predominantly water-based environment. The digestive system is water-heavy, and CBD, which does not dissolve well in water, has trouble passing through the intestinal wall into the bloodstream. As a result, only a small percentage of the CBD you ingest makes its way into circulation.

In fact, studies show that in a?fasted state, only about?6%?of orally consumed CBD is absorbed. This means that out of every 100 milligrams of CBD taken orally, only about 6 milligrams might actually enter the bloodstream. This low absorption rate is largely due to CBD’s lipophilic nature.

However, the body does have systems in place to absorb fats. When you consume CBD with food, especially foods high in fats, the absorption of CBD improves significantly. The fats in the meal help transport the CBD through the intestinal lining, allowing more of the molecule to enter the bloodstream. This is why experts often recommend taking CBD with a meal rich in fats—such as avocado, nuts, or fish—to increase its absorption.

Overcoming First-Pass Metabolism

Another major hurdle in the oral absorption of CBD is?first-pass metabolism. When CBD is ingested and absorbed through the gut, it enters the bloodstream and is immediately transported to the liver. The liver contains enzymes that begin to break down substances before they can be distributed to the rest of the body. In the case of CBD, up to?75%?of the molecule may be broken down by the liver before it reaches its target receptors. This process dramatically reduces the amount of CBD that makes it into?the systemic circulation?(the bloodstream), further limiting its bioavailability.

First-pass metabolism is a major reason why many people experience reduced effects from oral CBD products compared to other consumption methods. To bypass this process, alternative delivery methods such as?sublingual?administration (placing drops of CBD oil under the tongue) or?inhalation?(via vaping or smoking) offer more direct routes into the bloodstream. These methods avoid the digestive system and liver altogether, allowing more CBD to reach its intended targets in the body.

Enhancing CBD Bioavailability with New Formulations

To address the challenges posed by CBD’s lipophilicity and first-pass metabolism, researchers and manufacturers have developed innovative formulations designed to improve CBD absorption and bioavailability.

One such formulation is the use of?self-emulsifying drug delivery systems (SEDDS). Self-emulsifying drug delivery systems (SEDDS) are an effective technology for improving the solubility and bioavailability of lipophilic substances like CBD, which have poor water solubility. These systems are composed of oils, surfactants, and sometimes co-solvents. When in contact with gastrointestinal fluids, SEDDS form small oil-in-water emulsions, facilitating the absorption of lipophilic compounds in the digestive system. CBD is a compound derived from Cannabis sativa with recognised therapeutic properties, but its oral bioavailability is limited due to its poor water solubility and first-pass metabolism in the liver. SEDDS has proven to be an effective solution, significantly increasing plasma CBD levels and improving its absorption. Additionally, SEDDS help CBD to be absorbed more quickly, reducing the time needed to reach maximum blood concentration (Tmax) to 1 hour, which is beneficial in treatments requiring rapid action, such as for seizures or acute pain. Despite their advantages, SEDDS must be specifically designed for each drug, and studies have also shown variability in absorption between individuals. Factors such as body weight and metabolism influence how CBD is processed by the body, and further studies are needed to optimize SEDDS according to the characteristics of each patient.

Another promising technology is?nanoemulsion. Nanoemulsions break CBD into tiny, easily absorbed particles, making it easier for the body to transport the molecule through water-based environments like the digestive system and bloodstream. Nanoemulsions help CBD pass through barriers that would otherwise prevent its absorption, increasing the amount of CBD that can enter the systemic circulation.

These advancements in formulation are making CBD products more effective by overcoming the natural barriers posed by CBD’s lipophilic nature.

CBD Storage in Fat Cells: Long-Term Implications

Because CBD is lipophilic, it tends to bind with and be stored in fat cells (adipose tissue) in the body. Once stored, CBD can remain in the body for extended periods, slowly releasing as fat cells are broken down. This can result in a?build-up of CBD in the system for regular users, which could lead to sustained therapeutic effects even after discontinuing use.

However, this also means that CBD remains in the system longer than water-soluble substances. It’s important for regular users to be aware of this, as the gradual release of CBD from fat cells could influence long-term effects and overall usage patterns.

The Future of CBD Bioavailability: Innovative Approaches

As CBD continues to grow in popularity, the field of?bioavailability?is rapidly evolving. Emerging technologies such as?liposomal encapsulation,?water-soluble CBD, and further advances in?nanoemulsions?are improving how efficiently CBD can be absorbed and used by the body. These innovations aim to maximize the potential benefits of CBD by addressing its natural limitations as a lipophilic substance.

In the future, consumers can expect to see even more advanced formulations that make CBD easier to absorb, more effective at lower doses, and ultimately more convenient for a wider range of uses.

Conclusion

Understanding CBD’s?lipophilic?nature is crucial to grasping how it works in the body. Since CBD dissolves in fats but not in water, it faces unique challenges when consumed orally, including low bioavailability and first-pass metabolism. However, by pairing CBD with fatty foods, choosing alternative delivery methods, and taking advantage of new formulations like nanoemulsions and SEDDS, consumers can significantly improve how much CBD enters their bloodstream.

As the science of CBD formulation continues to evolve, the future looks promising, with more efficient products allowing users to fully benefit from the therapeutic potential of this remarkable molecule.

Disclaimer

This article provides general information and discussions about health and related subjects, as well as discussions on the scientific/pharmaceutical landscape in selected areas of interest to us. The information and other content provided here or in any linked materials are not intended and should not be considered or used as a substitute for medical advice, diagnosis or treatment. If you or any other person has a medical concern, you should consult with your healthcare provider or seek other professional medical treatment immediately. Never disregard professional medical advice or delay in seeking it because of something that you have read here or in any linked materials.