Absorbing ingredients: Bioavailability trends and research top of mind for industry experts

26 Oct 2023 --- Active ingredient absorption, also referred to as bioavailability, is one of the most vital aspects of dietary supplements, as without it, their functionality diminishes greatly. Nutrition Insight discusses the issue with experts from Lubrizol Life Science, Gencor and Balchem. 

“Human nutrition is mainly based on digestibility. Digestion deals with the breakdown of complex food materials into simpler food materials, whereas absorption means the body accepts those simpler food materials,” says Alan Connolly, R&D manager of nutraceutical ingredients at Lubrizol Life Science, Health.

“Without the absorption of nutrients by the human body through blood, the body would not be able to use the food material; therefore, the nutrients must be well absorbed for the repair of body cells, generation of energy, and maintenance of osmoregulation, among others.”

Maggie McNamara, marketing director at Gencor, adds: “Without good absorption, the efficacy is strongly reduced. Many active ingredients or nutrients are lipophilic (fat-soluble) or insoluble in water, consequently offering poor bioavailability.”

“Together with our partner, Pharmako Biotechnologies, we specialize in developing and manufacturing scientifically proven delivery systems designed to increase bioavailability and uptake while improving the functionality of actives,” McNamara continues.

Maintaining functionality through digestion
The most important aspect is that the active ingredient is intact and maintains its functionality until it reaches the target area, underscores Connolly.

“Vitamins and botanicals are very sensitive to external factors and, once destroyed, lose their beneficial effect. Encapsulation of the sensitive ingredients is the most effective way to protect them. Encapsulation involves ‘packaging’ the sensitive ingredient in a secondary material resulting in improved stability and bioavailability.”

“For both consumers and product formulators, bioavailability is a major concern as it determines supplements’ efficacy,” agrees Eric Ciappo, Balchem’s strategic development manager for nutrition science.

He clarifies that the better a nutrient is absorbed, the higher the amount is available to our body for metabolic use. On the contrary, when a nutrient is poorly absorbed, it cannot support critical bodily functions, providing limited value to users.The bioavailability of supplements is vital because it determines their functionality.

Absorption factors
McNamara tells us that bioavailability is defined by the percentage of a nutrient that is absorbed into the circulating bloodstream after consumption. Only absorbed compounds can offer a functional benefit to the body.

She explains that numerous factors affect bioavailability, including an ingredient’s chemical form and physical properties, such as its hydrophobicity and solubility, the formulation or galenic form, or the supplement matrix in which it is consumed.

Whether the formulation is administered in a “fed or fasted gastric emptying rate”, as well as “age, gender, physiologic state and coexisting pathologic conditions” are also highlighted by McNamara as having the capacity to affect bioavailability.

Meanwhile, Balchem’s Ciappo outlines the interaction with other nutrients and dietary components as the most impactful determinant of bioavailability.

“The so-called anti-nutrients are a great example — compounds found in food that can interfere with the absorption of specific minerals such as calcium, iron, zinc and magnesium.”

He explains that phytates and oxalates are among the most common anti-nutrients, these are typically found in plant-based foods such as whole grains, nuts, seeds and legumes. “Their effect can be remarkable — just 10 mg of phytates can inhibit iron absorption by roughly 60%.”

“Stomach acidity can also have a negative impact on ingredient absorption. To favor the digestion process, meals stimulate the release of gastric acid that helps break down nutrients into absorbable forms. However, our gastric acidity can decrease as we age, leading to lower absorption of key nutrients.”

Ciappo points to several specific forms of calcium, such as calcium carbonate, as being particularly vulnerable to the reduction of gastric acidity, being less absorbed when taken without food.

Delivery technology
Connolly explains that Lubrizol Life Science combines multiple technologies to ensure a great taste and low gastric irritation, enabling the delivery of nutrient-enriched products with optimum performance.

“In several cases, we first micronize the active ingredients to reduce the mean particle size and increase the bioavailability of different nutrients. This allows for more excellent absorption within the body in a second step. The micronized nutrient particles are encapsulated in protective matrices to impart additional functionality.”

McNamara describes Gencor and Pharmako Biotechnologies’s delivery technologies as critical to unlocking the potential of dietary supplements.

“We offer four advanced delivery systems that provide efficacious, bioavailable doses, with the flexibility of various finished product formats.”

Specifically, Gencor’s patent-pending, clinically validated self-micro-emulsifying drug delivery system, branded as AquaCelle, is designed to increase the bioavailability of lipophilic actives such as ubiquinol, omega-3s, lutein and resveratrol while maintaining product stability. Factors such as chemical form, physical properties, formulation and matrix can affect bioavailability.

“A second opinion for increased absorption is LipiSperse. This technology is an advanced cold water dispersion technology that allows solid or powder lipophilic active ingredients, such as curcumin, resveratrol, palmitoylethanolamide and quercetin — with otherwise relatively low bioavailability and poor solubility in water — to be easily dispersed in cold water, thereby increasing their bioavailability.”

Only 10% of LipiSperse is required with a 90% active load, which she asserts represents the most significant active to nutrient ratio in a water-dispersible formulation.

Gencor’s Compressible Powdered Oils (CPOs) use an oil-to-powder conversion technology designed to overcome the challenges of formulating with oily lipid-based ingredients and optimize an ingredient’s functionality. CPOs tackle formulation challenges by addressing the problem of product spoilage from oils.

“This material development allows oily active ingredients to be included in stable tablet and powder formulations without the oils leaching,” notes McNamara.

“Lastly, PlexoZome is a scientifically proven complex liposomal technology verified through Transmission Electron Microscopy (TEM) and cryo-TEM imaging, Zeta potential and dynamic light scattering testing. PlexoZome formulations offer targeted delivery, are fully customizable and are made on-site in Pharmako’s licensed facility.”

Multi-ingredient solutions
Considering the growing consumer interest in convenient supplements designed to tackle different health areas simultaneously, Ciappo highlights the need for brands to master the art of blended formulations without compromising on absorbability, bioavailability and effectiveness.

“Vitamin K2 is a good example of where we have worked to overcome this challenge. When it comes to multi-ingredient products that combine vitamin K2 with other ingredients, stability is a big issue as the vitamin quickly degrades in blended formulations. To ensure vitamin K2 solutions stay intact and deliver full health benefits, Kappa Bioscience (recently acquired by Balchem) developed K2vital Delta — the first double micro-encapsulated vitamin K2.”

Ciappo states that K2vital Delta can be used in tandem with Balchem’s bioavailable chelated minerals from the Albion Minerals range without compromising on results. “This is also something we’re currently investigating further, focusing on exploring the synergies between our expanded portfolio.”

“Besides being more easily absorbed into the human body, Albion Minerals’ organic mineral amino acid chelates are also digestive-friendly, due to the fact that they’re absorbed intact and will then break apart in the intestinal cell for transport.” Scientific research is essential to understanding and improving active ingredient absorption.

Clinical trials
Scientific research is essential to understanding and improving active ingredient absorption. Ciappo explains how these were utilized by Balchem to address bioavailability issues arising from ingredient interaction.

He argues that chelated minerals such as Balchem’s Ferrous Bisglycinate — the iron chelate found in Ferrochel — can limit the interaction with the environment and other ingredients, such as anti-nutrients.

“Clinical trials on humans estimated that in the presence of an anti-nutrient such as phytates, Ferrous Bisglycinate is up to five times better absorbed than ferrous sulfate. This is one of the reasons why the WHO selected Ferrous Bisglycinate iron chelate as a ‘fortificant of choice.’”

“With Albion Minerals, we’ve also been able to prevent the effects of decreased gastric acidity on nutrients. For example, our Calcium Citrate Malate (CCM) provides superior benefits in terms of absorption if compared to calcium carbonate. CCM is more soluble and is optimally assimilated even when taken without meals.”

The European Food Safety Authority recognizes CCM as up to 15% better absorbed than other calcium sources.

“This ingredient’s high bioavailability, combined with the neutral taste profile and enhanced solubility of CCM, make it an excellent option for manufacturers looking to maximize assimilation while also providing formulation benefits at the benchtop,” Ciappo adds.

“To enhance reliability and transparency within the industry, we’ve introduced TRAACS — The Real Amino Acid Chelate System — referring to the processes and proof of the quality we apply to our chelated minerals. We also provide the TRAACS seal to our co-branding customers.”

Ciappo concludes that details like this are essential for both purchasers looking for high-quality ingredients and consumers seeking digestive-friendly, highly efficient mineral supplements.

By Milana Nikolova

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