Bioavailability crucial for ingredient success in nutraceutical market, says industry

15 Apr 2020 --- Bioavailability can make or break ingredient formulations due to its crucial role in determining dosage effectiveness and quality. These factors combined are of key concern to formulators, who strive to deliver potent ingredients quickly absorbed by the body to sustain consumer appeal. NutritionInsight speaks with nutraceutical players active in this space on what challenges low bioavailability bring, how they are overcome and how increasing consumer awareness is shaping industry.

Bioavailability is defined by the percentage of a nutrient that is absorbed into the circulating bloodstream after consumption and is able to offer a functional benefit in the body, according to Stephane Vouche, Marketing Manager at Lonza. “A higher bioavailability percentage would suggest that a greater proportion of a nutrient can be absorbed, therefore offering enhanced efficacy and performance once in the bloodstream.” 

“Key factors that influence bioavailability are the physical properties, such as its hydrophobicity and solubility, the formulation or galenic form and whether the formulation is administered in a fed or fasted state gastric emptying rate,” adds Alberto Espinel, Head of R&D, Pharmactive.

The buzz on bioavailability
The effective bioavailability of ingredients is a tool to sustain company sales through customer retention and long-term brand building, according to Maja Orešnik, Science & Research Director at PharmaLinea. “It switches [the focus] from ‘how much of this ingredient will we put in the product’ to ‘how much of this ingredient will the consumer actually receive and be able to readily use.’ The journey of an ingredient and its associated benefits to the consumer is long and bioavailability is a key step in that journey,” she affirms. 

Over at Naturex, part of Givaudan, Pascale Fanca-Berthon, Category Technical Leader in Health Ingredients, knows that increasing the quantities of a particular active does not immediately translate to increased benefits if they aren’t presented in a bioavailable form. “By increasing bioavailability, we can decrease the amount needed for an effective dose. Low effective doses make compliance easier for the consumer and can reduce cost-in-use for end-product manufacturers,” she explains.

Lonza’s proprietary research shows that in France, over 70 percent of consumers in the Millennial and Boomer age groups would like more clinical proof that the nutrients in the supplements they take are being fully absorbed by their bodies. This figure rises to 78 percent for older consumers, Vouche underlines.

Click to EnlargeLow bioavailability can have serious long-term consequences, says Meppem of Pharmako Biotechnologies.A big pill to swallow
In the nutraceutical world, low bioavailability can have serious long-term consequences, says Eric Meppem, Co-Founder and Commercial Director at Pharmako Biotechnologies. These include poor efficacy, low repeat purchase and consumer compliance and consequently brand distrust. “Moreover, higher doses require larger pills to swallow and, ultimately, less opportunity for synergistic formulations.”

Pharmako specializes in improving the bioavailability of lipophilic ingredients. Its customizable, self-micro-emulsifying delivery system AquaCelle is specifically designed and clinically proven to optimize bioavailability while maintaining product stability, the company states. “AquaCelle can facilitate increased absorption, while at the same time reducing or eliminating the effect of food on the absorption of these now bioactive compounds. By including AquaCelle into the formulation, formulators can make smaller doses which can increase compliance and tolerance. It’s easier to swallow a small capsule once a day versus many large capsules several times a day,” 

In the case of collagen peptides, Rousselot is conscious that low bioavailability can hinder the effective digestion and absorption of nutraceutical or nutricosmetic ingredients. Janne Prawitt, Scientific Director Health and Nutrition, identifies the high bioavailability of pure collagen peptides as a “prerequisite” to guarantee the biological efficacy of small bioactive peptides. 

“Collagen’s native form is hard to digest. It needs to be processed into collagen peptides to become highly bioavailable. This is known as hydrolysis and involves the separation of individual collagen strands and the breakdown of long amino acid chains into smaller peptides, which can easily be digested and absorbed by the body,” she explains. 

Orešnik at PharmaLinea also highlights that preserving added-value ingredients throughout its shelf-life is a “more difficult” challenge. To prevent deterioration, it is necessary to create environments to ensure “sometimes very complex combinations of substances [remain bioavailable] and ingredients do not interact or undergo any change that might make them less bioavailable,” she explains.

In terms of delivery formats that best facilitate high bioavailability, Espinel of Pharmactive states that generally, coated galenic forms can better preserve actives in ingredients. Moreover, solubilized formulas, such as effervescent tablets and some soft-gels, can favor the absorption at the intestine. 

Click to EnlargeLicaps clear capsule with fluid.Turmeric: A textbook example
A textbook example of poor bioavailability is turmeric, which is known for being poorly absorbed by the body. However, nutraceutical companies have found different solutions for this R&D headache. Naturex developed TurmiPure Gold, a patented colloidal suspension turmeric in a 100 percent natural formulation, which enhances bioavailability and water dispersibility of curcuminoids. “With TurmiPure Gold, there’s no need to take a high daily dose of turmeric. A dosage of 300 mg of TurmiPure Gold delivers the same amount of curcuminoids as an effective high dose of market standards,” explains Fanca-Berthon.

Meanwhile, by partnering with NovaSOL Curcumin in its latest applications, Lonza has been able to bring this highly bioavailable liquid form together with its liquid-filled, hard Licaps capsules. “Licaps capsules are hermetically sealed with a proprietary fusion sealing technology, which ensures that they can safely and securely deliver a wide variety of potential high bioavailability liquid fills. In fact, two Licaps capsules with the patented, dissolved NovaSOL Curcumin offer equivalent benefits to 27 standard curcumin tablets,” Vouche notes.

Industry impacted by increased consumer awareness
Just as responsible consumers have driven demand for the plant-based, clean label supplements, they have also encouraged the need for high-quality, sustainable supplement solutions, which are efficacious and backed by science. “As such, we work with our partners to help them prepare for a future in which bioavailability is an even bigger priority for the modern consumer,” adds Vouche. 

Meanwhile, Fanca-Berthon says that Naturex’s customers are also well aware of the issues surrounding bioavailability. “Beyond the notion of bioavailability, bio-equivalence is becoming the new go-to measure for determining product performance because it can be used to compare bioavailability across products. Bio-equivalence is when two products can be equivalent for a specific effect, for example the amount of curcuminoids that is absorbed by the body. In the case of TurmiPure Gold, you would need to take 1922 mg of standard turmeric extract to reach the same level of curcuminoids in blood as just 300 mg of TurmiPure Gold,” she explains.

Click to EnlargeIncreasing clinical studies is the ticket to consumer education.  Despite business awareness of the topic growing, Meppem affirms that many consumers are still confused about bioavailability. The real challenge is supporting brand customers with published, credible data to inform and convince consumers about enhanced bioavailability. 

“Clinical results are more meaningful for consumers and companies need to provide credible evidence on enhanced absorption. Comparisons of a bioavailable nutrient to another from studies with different controls only exacerbate this confusion,” he emphasizes. Tackling this, Pharmako relies on comparing absolute measures, such as the actual measure of an active in nanograms per ml of blood plasma. 

Both Prawitt of Rousselot and Pharmactive’s Espinel rally behind the clinical studies banner. “After studying Peptan, Rousselot has invested further in fundamental research that analyzes Peptan’s bioavailability, taking a first step towards explaining the mechanism of action behind the health benefits of collagen peptides,” Prawitt notes. Pharmactive also prioritizes the “proper communication” of the results of its pharmacokinetic studies. “Should any factor affect one of our ingredients, we recommend to our clients which formulations or formulas should be used. [It is important to] educate the final consumer and show information about the ingredient on the packaging,” adds Espinel.

Regardless of the progress made in challenging industry to improve ingredient absorption and better inform end-consumers, Orešnik from PharmaLinea concludes that delivering ingredients in the promised amount and state is far from easy and still not highlighted enough in the industry. “We have a dual role. Not only do we continue investing in our expertise in stable product development, we also keep educating the industry’s NPDs and business development managers.” In the meantime, education through the media and trade shows is gradually picking up momentum and slowly but surely clarifying “the entire story of bioavailability.”

By Anni Schleicher

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