CBD oil is traditionally formulated in such a way that leaves the CBD unable to be properly absorbed by the human body. This is both physically and economically wasteful, as well as ineffective at helping the user. There are many reasons for the low efficacy rate and bioavailability of traditionally formulated CBD products. This report aims to examine some factors about these standard processes that cause improper absorption, as well as exploring a solution to these common problems.
Why is the way CBD oil is formulated important?
For bioavailability
Bioavailability refers to the rate at which CBD oil (or other drugs) is absorbed by our bodies and how much of that CBD is actually available for our bodies to put to use. As previously mentioned, CBD oil has a poor absorption rate, simply because our bodies are made mostly of water. Oil and water do not mix, so this means that most of the CBD we ingest does not get used by our bodies. Many CBD oils are not created with water solubility in mind.
Some research shows that oral CBD can have an absorption rate of as low as 6%, meaning that 94% of the CBD you take is not getting used by your body.8 Additionally, there are animal studies exploring the bioavailability of orally administered CBD. Their research showed absorption rates of between 13% and 19%.4 On the one hand, this is much better than the previously mentioned 6%, but it is nowhere near 100% and ultimately, the majority of CBD is still going unused. Proper absorption of oils also requires the optimal function of the liver, pancreas, and a complete digestive tract. Absorption is also affected by the diet, age, and health conditions of the user, so if you have a condition that impacts absorption, your body is using even less CBD.
Referring back to the previously mentioned animal studies, the research showed that CBD undergoes “first-pass metabolism” or pre-systemic metabolism, meaning the concentration of the drug (in this case CBD) is significantly reduced when it is administered orally. CBD’s metabolites (or unused byproducts) are excreted through the kidneys. The study does note, however, that “bioavailability is increased with various lipid formulations.”4
Introducing the right technology, the correct formulation processes, and proper enhancements encourage a better CBD bioavailability. Stronger absorption rates produce better health benefits and, ultimately, save the user money. While it may be more of an investment upfront than traditional CBD oil, the benefits it brings over time are worth every penny.
Other reasons to consider when selecting your CBD oil formulation method is the taste of the final product, the shelf-life of your final product, as well as the stability, it has after it has been manufactured. Different formulation processes can all have an impact on these factors.
Techniques and processes that can improve bioavailability
Creating a water-soluble formula
CBD oil is naturally hydrophobic, it repels water. You can see in the picture below that the water simply sits on the surface of the water, there is no attempt to mix in with the water because its molecular composition does not allow for it. Creating a CBD oil product with an affinity to water is necessary for proper absorption and an incredibly effective way to increase bioavailability.
In order to make CBD oil water-soluble, the particles must essentially explode and disperse into smaller particles that are able to be mixed in with water. This explosion and dispersion change the frequency of the oil so that the CBD becomes attracted to the water in our bodies. Creating hydrophilic (water-loving or water-soluble) oils, in turn, increases the bioavailability and efficacy rate of CBD oil. Our bodies work with the water-soluble formulation to produce the best results.
Choosing the correct level of formulation
There are a few different levels of formulation, with mixing being the least effective way to formulate a CBD oil product.
Mixing or blending
Mixing CBD oil uses heating and blending processes. This has become the CBD industry standard and the end goal is to have a finished product, but not much past that. There is not much consideration for water solubility and bioavailability if the product is mixed or blended.
Mixing produces CBD with very low efficacy – the particle sizes are very large compared to other CBD oils created from different mixing techniques, about 20-50 microns.
Microemulsion
Using microemulsion as a drug delivery system is not a new technique or exclusive to the CBD manufacturing process. It is a widely used technique in the cosmetic, pharmaceutical, and food industries. Looking at the pharmaceutical industry specifically, microemulsion technology is appealing because it has been shown to improve bioavailability in poorly soluble drugs and has appeared in scientific literature since the early 1990s. Microemulsion technology is formulated with surfactants to reduce the surface tension of two liquids.
Microemulsion technology has been shown to help drugs using a peptide and protein delivery system to reach the digestive tract, as well as other kinds of drugs. Protein and peptide therapeutics naturally have low solubility. Some research shows protein and peptide drug delivery systems to have a bioavailability of less than 1%, so the potential for microemulsion technology is quite large.7
One study looked at the drug clopidogrel and how it responded to microemulsion technology. Clopidogrel is an antiplatelet medication that is prescribed to reduce the risk of heart disease and stroke in high-risk individuals. The study found that the solubility of the drug was successfully enhanced 80.66x. The oral solubility of clopidogrel is normally very low, with some studies reporting less than 50% bioavailability.5
Microemulsion heats to an exact temperature and utilizes high-end emulsification equipment to mix CBD and carrier oil at the cellular level. This breaks down the particles to the 2-5 micron range and creates a CBD with 10x bioavailability of standard blending.
Nanoemulsion
Nanoemulsion technology can break down CBD particles to be as small as under 1 micron or 1,000 nanometers. Research positions nanoemulsion technology as appealing because less surfactant is needed for nanoemulsion than microemulsion, usually less than 10% surfactant is used while microemulsion uses about 50% surfactant. Like microemulsion technology, this formulation process also increases the bioavailability of the drug clopidogrel. Correctly formulated nanoemulsion products are said to have a shelf-life of two to five years. It is important to source high-quality products, as those using incorrect nanoemulsion techniques are meta-stable, meaning they will not store well and are more susceptible to a phenomenon called Ostwald ripening.2
Both nano and microemulsion technology are also able to be formed into products that have multiple routes of administration, such as creams or drops for topical products – an ideal scenario for topical CBD products.
Opting for liposomal encapsulation
Encapsulating CBD particles with liposomes is an effective way to increase the bioavailability of CBD oil. There is a substantial amount of evidence to prove liposomes as an effective way to increase the bioavailability and enhancement of oral drugs with a traditionally poor rate of absorption.
According to research, “The application of liposomes to assist drug delivery has already had a major impact on many biomedical areas. They have been shown to be beneficial for stabilizing therapeutic compounds, overcoming obstacles to cellular and tissue uptake, and improving the biodistribution of compounds to target sites in vivo. This enables the effective delivery of encapsulated compounds to target sites while minimizing systemic toxicity. Liposomes present as an attractive delivery system due to their flexible physicochemical and biophysical properties, which allow easy manipulation to address different delivery considerations.”6 In other words, the liposomal delivery method is non-toxic, durable, and can overcome obstacles, as well as being extremely flexible with where in the body it can go and what it can do. Research shows that liposomes are able to protect the drug it encapsulates as the drug makes its way through the digestive tract.1 Drug surviving the digestive tract is a common concern because stomach acids and the metabolic processes of the body can break the drug down before it reaches its target.
Arguably one of the most important points for creating CBD with a liposomal delivery system is their unique ability to be able to entrap both lipophilic (having a tendency to dissolve in lipids or fats) and hydrophilic (an attraction for water) compounds. This creates a unique opportunity for liposomal technologies to be applied to a diverse range of drugs, including CBD oil.
Using water-soluble Vitamin E as an enhancer
D α-tocopheryl polyethylene glycol 1000 succinate is the water-soluble derivative of the natural form of vitamin E, D α-tocopheryl. For clarity, it will be referred to as “TPGS”.
There is significant research supporting the use of TPGS in many drug therapies. It was suggested in 1960 as a solubilizing agent for oil-soluble vitamins. TPGS shows a hydrophilic head and lipophilic tail, allowing TPGS to be compatible with fats and water. Biopharmaceutical studies suggest that it can be used as a safe, effective absorption enhancer for poorly absorbed drugs such as cyclosporine and protease inhibitors. According to this research, TPGS can “be applied as a solubilizer, absorption and permeation enhancer, emulsifier as well as surface stabilizer in drug delivery. It has been widely used in fabricating nano-drugs or other formulations for many poorly water-soluble or permeable drugs.”9
TPGS is widely recognized as providing many advantages to drug therapy. But possibly the most groundbreaking is TPGS’ tendency to show anticancer activity. According to the research, TPGS targets the mitochondria of cancer cells and induces apoptogenic (death of cells) behavior. The study also notes that TPGS can kill these tumor cells and not cause any harm to healthy cells and tissues.9
In addition, TPGS is approved by the FDA.
In conclusion:
Pivoting from traditionally manufactured CBD oil water-soluble will greatly increase the bioavailability of CBD oil. Not only will the molecular composition of the CBD oil change and become compatible with water, but the enhancers will also boost the rate of absorption, too. The research on these methodologies is not new. Liposomal technology and TPGS have a substantial amount of evidence to prove their effectiveness. It is simply a matter of applying them to CBD manufacturing processes.
