Ingredients to increase solubility, stability, bioavailability, and more
The cannabis market continues to burgeon, both domestically and globally. As of 2019, North America holds the largest revenue share at 88.4%, but the global legal marijuana market size is expected to reach USD $73.6 billion by 2027, according to Grand View Research.1 And although the global market is slated to expand at a compound annual growth rate (CAGR) of 18.1%, the market still faces hurdles when it comes to formulating new cannabis products.
Many factors affect formulation—from efficacy to taste—and much of it depends on the delivery form. For example, edibles have the issue of taste. Masking the taste of actives or minimizing the taste of surfactants and emulsifiers presents a challenge. Another factor is that different cannabinoids exhibit their own formulating characteristics. For instance, cannabidiol (CBD) and tetrahydrocannabinol (THC)—full- and broad-spectrum CBD and THC—will formulate similarly; however, the other bioactives found in cannabis extracts, such as terpenes, sterols, fiber, etc., may strongly impact the formulations and their functionality, solubility, and taste. But overall, according to Alice Hirschel, PhD, nutritional business director at ABITEC, the two major challenges that product developers face are improving solubility and ensuring absorption of the cannabis actives.
“Cannabis extracts, including all forms of CBD and THC, are hydrophobic, meaning they are not soluble in water,” Dr. Hirschel explains. “This creates a challenge when formulating a variety of delivery forms.”
To overcome this, emulsions are used to solubilize cannabis extracts so they can be included in more delivery forms, including edibles, functional beverages, gummies, personal care products, etc. For example, data supports ABITEC’s CAPTEX® 8000, a caprylic acid medium-chain triglyceride oil, achieving up to 40% w/w solubility of CBD. Its CAPMUL® GMO-50 and CAPMUL® MCM C8 ingredients have a high capacity to solubilize cannabis extracts, and they also function as emulsifiers. Moreover, CAPMUL® ingredients function as food preservatives due to their ability to provide protection, stability, and increase shelf-life.
Beyond solubility is bioavailability. “As lipophilic (lipid-loving) actives, cannabis extracts need to be solubilized in lipids, and these lipids may also facilitate in their absorption upon ingestion,” Dr. Hirschel says. “Lipid delivery systems have been used for decades to deliver hydrophobic actives in easy-to-use, convenient delivery forms that also support absorption.”
ABITEC’s SENDS™ formulations—which include a solubilizer, an emulsifier, and a surfactant and/or co-surfactant—enhance solubility and promote emulsification of active nutraceutical ingredients (ANIs), such as cannabis extracts, leading to greater bioavailability.
“The combination of these ingredients and steps for formulating a SENDS™ will vary based on the ingredients of the end-use product,” Dr. Hirschel explains. “Each SENDS™ formulation is custom designed to optimize the ANI. Optimization can include increased bioavailability, enhanced formulation efficiency to reduce dose, and protection of the ANI during processing and in the gastrointestinal environment while reducing food effect.”
Transdermal Penetration and Lymphatic Transfer
Topical applications present a unique challenge to absorption. “Transdermal-penetrating formulations require the optimized concentration of carrying excipients and penetration-enhancing excipients to produce the desired flux across the stratum corneum (the outer layer of the skin) to the site of release,” says John Tillotson, RPh, PhD, pharmaceutical and nutraceutical technical business director at ABITEC. Many of ABITEC’s CAPMUL® ingredients can increase transdermal penetration by hydrating the stratum corneum, allowing for the transdermal administration of CBD and THC.
For oral products, “To increase bioavailability, some or all of the active ingredients may need to be driven into the lymphatic system to avoid first-pass metabolism,” Dr. Tillotson says. Long-chain lipids, such as CAPTEX® GTO and CAPMUL® GMO-50 from ABITEC, help drive lymphatic transport of CBD and THC, leading to decreased first-pass metabolism and improved bioavailability.
As companies like ABITEC continue to create solutions for solubility and bioavailability in cannabis formulations, product developers are using these solutions to engineer new, innovative delivery forms and label-friendly formulations that satisfy consumers’ needs and growing market demands.
Grand View Research. “Legal Marijuana Market Size Worth $73.6 Billion by 2027 | CAGR 18.1%.” Published February 2020.