Aenova spotlights softgels for optimizing CBD bioavailability and user appeal

16 Dec 2021 --- Softgel capsules are an ideal dosage form for cannabinoids like CBD, according to Aenova. In a new white paper, the Germany-based company details that this format offers better bioavailability, as well as being preferable from a regulatory and convenience standpoint.

“There are only advantages using softgels for cannabinoids because they protect the cannabinoids from light and oxygen, which cause degradation compared, for example, to pure liquid formulations,” Dr. Mario Arangio, head of pharmaceutical development at Aenova, tells NutritionInsight. 

Cannabinoids have good permeability and poor water solubility. Additionally, they must be presented in the gastrointestinal tract in an already stabilized form.Cannabinoids are used in various areas of application, including pain, appetite and nausea. 

Bioavailability concerns
The poor bioavailability is not only due to the poor gastrointestinal solubility but also to a significant first path metabolism that occurs in the liver following gastrointestinal absorption. 

“This is the main reason that cannabinoids are ideal for lipid-based drug delivery systems (LBDDS) in soft gelatin capsules. Some recent studies have shown that THC and CBD oral bioavailability have increased threefold (from 3­8% to almost 30%) thanks to the use of LBDDS,” states the white paper. 

Once the soft gelatin capsule is ingested by a patient, the capsule ruptures within 5 to 10 minutes and the cannabinoid is released in the GI tract and absorbed into the bloodstream.

The absorption process can be influenced by the diet of the patient or by the excipients of the capsule. By choosing the right lipid excipients, digestion – via lipases and bile salts – can lead to mixed micelles that are absorbed through the enterocytes.

Patient appeal
For pharmaceutical purposes, several different dosage forms have been considered for the formulation of cannabinoids. These include oral, nasal, sublingual, transcutaneous and rectal, for example. 

Oral administration is often preferred because of its ease of use and lower regulatory hurdles, notes Aenova. Within this, it states that softgel capsules are particularly suitable as the preferred dosage form because of their specific properties.

Beyond technical advantages, softgel capsules are associated with better patient compliance. 

Aenova argues that liquid forms, which are often popular for CBD, often feature syringes, which can be inconvenient. 

Additionally, soft gelatin capsules can easily mask ingredients’ smells and tastes, and the capsules can be customized to a wide variety of shapes and sizes. They are also chewable and can be used for sublingual applications, thus appealing to people who may be unable to swallow pills. 

Earlier this month, Cannaray CBD rolled out its supplements in British supermarket chain Waitrose, offering a choice of capsules, drops or gummies.
Aenova argues there are numerous advantages to softgel capsules for cannabinoids. 

What’s next for capsules? 
Arangio flags that there is still “plenty of idle capacity” for soft gels available. 

“Companies differentiate by innovation, customer service and quality excellence, which reveals the preferred partners.”

Looking ahead, he anticipates that trends in the capsule industry are set to include vegetarian and vegan capsules, as well as enteric capsules with shell properties to avoid coating, 

“Another popular feature will be bioavailability enhancement by lipid matrices,” he predicts. 

He also acknowledges that the nutrition industry has a “huge variety” of delivery formats, which include drops, tablets, chewing gums, teas and cereals. “Here, it is more a question of taste.”

Indeed, alternative delivery formats have been a key area of innovation across industry as consumers fight off “pill fatigue.” At Vitafoods Europe 2021, exhibitors presented a mixed picture of attitudes toward capsules. 

By Katherine Durrell