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What is Cannabinoid Bioavailability, and What Does it Mean for Formulation?

Cannabinoid bioavailability is a crucial consideration in cannabis product formulations. If the cannabinoids in a product formulation are not sufficiently bioavailable, the product will not deliver the full dose and will not have its intended effects.

What does bioavailability mean, and why is it essential in optimizing cannabis product formulations? Keep reading to learn the science behind cannabinoid bioavailability and how to achieve truly water-soluble formulations.

What is Cannabinoid Bioavailability?

Bioavailability is a scientific term to describe the extent to which a substance reaches its intended site of physiological action.

In pharmacokinetics, the study of drug movement through the body, the acronym ABCD stands for:

  • Administration: the route of administration (e.g., oral, topical, inhalation) and dose of a drug

  • Bioavailability: the proportion of a drug that enters circulation so it can have an active effect

  • Clearance: the physiological removal of the active form of the drug from the bloodstream

  • Distribution: how widely a drug can travel to fluid compartments of the body once consumed

Cannabinoid pharmacokinetic processes are dynamic, may change over time, and are affected by the frequency and magnitude of cannabinoid consumption.

What Affects Cannabinoid Bioavailability?

In simple terms, bioavailability is determined by two main factors: the route of administration and the dose of a cannabinoid.

How Does Route of Administration Affect Cannabinoid Bioavailability?

The route of administration refers to how a drug is consumed or ingested, such as:

  • Oral

  • Sublingual

  • Topical

  • Inhalation

  • Intranasal

  • Injection

  • Rectal

  • Vaginal

If the same dose of a cannabinoid is given with different routes of administration, it will have different bioavailability.

For example, inhaled cannabinoids are delivered rapidly through absorption across the large surface area of the lungs and respiratory tract epithelium, where they directly enter the bloodstream. The inhalation route bypasses first-pass metabolism by the liver. Inhaled THC has a bioavailability of up to 56%. Therefore, an inhaled THC dose of 10 mg would result in 5.6 mg reaching the bloodstream.

On the other hand, the bioavailability of orally consumed cannabinoids will depend on the amount of drug absorbed across the intestinal epithelium. It will also be subject to first-pass metabolism, where liver metabolism diminishes the drug concentration before it has a chance to reach the bloodstream. As a result, the oral bioavailability of THC is estimated to be only 6% to 20%. Therefore, if 10 mg of THC is ingested orally, only 0.6 mg to 2 mg reaches the bloodstream.

How Does Dose Affect Cannabinoid Bioavailability?

The dose of a cannabinoid is indirectly proportional to its bioavailability.

This means that if a cannabinoid has a low bioavailability, a larger dose is required to reach the minimum concentration threshold for effectiveness.

If a cannabinoid has a high bioavailability, a lower dose is needed to reach the same threshold for effectiveness.

For example, a 10 mg dose of THC results in only 0.6 mg to 2 mg reaching the bloodstream; however, if bioavailability is brought to 100% through cannabis product formulation, the entire 10 mg dose is delivered.

How Does Cannabinoid Water Solubility Affect Bioavailability?

Reliable medical efficacy in cannabis product formulation depends on the ability of the formulation to deliver a consistent dose to the intended physiological site of action.

Cannabinoids are naturally water-insoluble molecules. Therefore, cannabinoid bioavailability in cannabis product formulation depends on how effectively formulators can solubilize them.

For example, in topical formulations, such as cannabinoid-infused pain creams, if cannabinoids are not water solubilized, they cannot effectively penetrate the skin.

In oral cannabinoid product formulations, increasing the water solubility of cannabinoids improves bioavailability by increasing the dose of cannabinoids absorbed into the bloodstream. In effect, improving the water solubility of cannabinoids makes the same amount of an ingredient go further.

Learn more about How to Use Water-Soluble Cannabinoids.

How Can the Bioavailability of Cannabinoids Be Improved in Product Formulations?

Formulators can improve bioavailability in product formulations by increasing the water solubility of cannabinoids.

Traditional methods to improve the water solubility of cannabinoids include sonication, liposomes, and micelles. Nanotechnology refers to the dispersion or emulsion of tiny oil droplets in water. However, with these methods, cannabinoids are still not truly water soluble at the molecular level.

The bioavailability of cannabinoids will be adversely affected if a water solubilizing method is not fully effective. A less effective method means formulators will need greater amounts of cannabinoid ingredients to meet the same threshold for physiological effectiveness, resulting in diminished profitability.

Furthermore, without achieving true water solubility, ingredients will separate out of the product, form cloudiness, and settle to the bottom. These issues adversely affect the taste, smell, and shelf life of cannabis product formulations.

Truly Water-Soluble Bioavailable Cannabinoids

Synergy Life Science’s flagship ingredient CannaSorb CB Active is made by chemically reacting a fat-soluble compound to convert it into a water-soluble compound. We start with a hemp-derived CBD isolate to create a fully reacted biopolymer, resulting in an opaque liquid that dilutes quickly, easily, and fully into water at all concentrations to create a clear, stable, and permanent solution.

CannaSorb CB Active is fully bioavailable in the body, with emulsifying action that improves the water-solubility of other components, thereby enhancing their uptake in the body. Unlike other cannabis compounds that claim to be water-soluble yet only have 10% to 25% activity, CannaSorb SB Active is 100% active, so you need less of the ingredient to achieve better results. Our process dramatically increases the bioavailability of CBD isolate. Multiple safety and toxicity studies have received very favorable results.

Traditional methods to improve water solubility in cannabis formulations have varying effectiveness, quality, bioavailability, and actual cost. The innovative ingredient formulation in CannaSorb CB Active goes beyond nanotechnology to deliver true water-solubility that produces a stable, consistent product, making it an ideal platform for a wide range of advanced products with improved efficacy and increased profitability.

You're in the right place if you seek high-value cannabis formulation ingredients and white-label opportunities. Our industry know-how and expert support at Synergy Life Science will help you get your high-quality products on the retail shelves efficiently and affordably. Contact us here to find out more.

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