What is a delivery system and what is the purpose of having one? Is an innovative delivery system worth the extra money? What is the added value or benefit from a consumer perspective? There are many, many questions surrounding this topic but I’ll go through a few of the main ones here.
In short, an innovative delivery system is about ensuring that end-users get value for money, and the product they consume helps to deliver the benefits where it is needed in a quantity that is beneficial to their health. Without some of these delivery systems, the product we consume could be of very little benefit at all. I shall not consider the quality or production method here but merely the actual delivery methods for products themselves.
The efficacy of the ingredient is directly proportional to its bioavailability: the better the bioavailability, the better the efficacy. Hence, in order to achieve the highest possible efficacy, one must have a higher bioavailability. Another advantage with higher bioavailability is that with an increase there can be a corresponding reduction in the dosage. In other words, the higher the bioavailability, the lower the dosage requirement.
A Coating Process refers to atomising the air coating polymer into droplets, which hits the substrate particle and spreads on the surface where the active ingredient is and forms a uniform coating. When it comes to effective delivery systems, this technology offers many protection benefits for the bioactive: it reduces the overages of nutrients by reducing losses and cost savings, protection from moisture, acidic pH, ingredient interactions, heat, and exposure to oxygen, release parameters can be altered as desired (for instance, at a specified temperature or in the stomach for digestion), flavour and odour masking, ease of handling, effectiveness in products like medical foods, nutraceuticals, and meal replacement products where characteristics such as stability, bioavailability, delivery, and effectiveness are closely regulated.
Encapsulation can be an excellent approach to deliver biological functionality to a target site for action (e.g. absorption of a nutrient). Most often its complexity is heavily underestimated. To create a successful product, the total life cycle of the product has to be considered: the creation of the ingredient, processing of the product, shelf life, and for the utilization phase, storage, kitchen processing, passage through the mouth and stomach, release at the right location in the intestine. Through this life cycle, a wide range of aspects should be considered, for example, heat resistance; oxygen resistance; mechanical resistance; dehydration/rehydration; acid, bile, enzyme resistance; osmotic effects. Also including the duration of these individual conditions (or in combination) and the total duration to go through the life cycle.
One very popular delivery system is micro-encapsulation, and this is highly useful for many ingredients that need to be released or active later in the “acid” form in the body otherwise they will simply be eaten up by this natural bodily function. One such nutrient could be iron. Some companies have perfected this delivery method and are able to also prove and demonstrate the benefit of micro-encapsulated iron. Micro-encapsulation technology also has an additional benefit of reducing the undesirable organoleptic attributes of some nutrients like iron that have a metallic taste. Applications for micro-encapsulation also greatly improve as some foods may otherwise inactivate the beneficial attributes of an active.
Ingredients such as dairy products can be difficult to add active ingredients to as can probiotics. With micro-encapsulation, this issue can be overcome as the active protects itself from being attacked by other living organisms. Natural protective delivery systems can also be achieved with a controlled manufacturing method using a fibre that is naturally present around the actives, ensuring it is stable and protected against the acid in the body and therefore can reach its “end” destination where the active is then released.
Another example is liposomes, another delivery vehicle used in dietary supplement and functional foods and beverages. Originally developed for drugs but in recent years several dietary supplement companies have also released many supplements using this technology. They are hollow spherical vesicles composed of a lipid bilayer made from the same few component materials of the cell membrane that can be filled with drugs and/or dietary supplements and used to deliver drugs for various diseases. They are simple or double emulsions in sub-micron size, generally, 20 – 250 um in diameter and are prepared using different methods: mechanical dispersion, solvent dispersion or detergent removal. The advantages of liposomal composition are to increase the bioavailability and targeting property of the active ingredient, to increase the dissolution rate of the oil/water-soluble drug and to enhance the stability of the product. With the delivery of a drug/supplement with a typically slow or regulated pattern of absorption, such as vitamin C or Curcumin, may be accelerated when encapsulated within a liposome.
Time-released products have additional benefits especially if they are multi-ingredients or if an ingredient’s “half-life” is too short for some actives such as Vitamin C (Ascorbic Acid). With a time-released Vit C tablet which can release the active slowly during the day this will then help to ensure maximum benefit from the supplement when there is a need from a user perspective. An example of a time-released system is a 3-layer tablet where each layer releases the ingredients after a specific time such as 1h, 4h and 6h. This is a great way of getting the active ingredient(s) to be effective and used by the body at different stages.
In terms of processing and technology, note that being nano in particle size provides a higher and quicker absorption, sustained over a period of standard time ensuring maximum concentration of ingredients. When ingested, the pharmacokinetic properties of liposome intestinal absorption override the usual absorption pattern of the encapsulated drug. In other words, it provides the higher Cmax with shortest of Tmax, meaning that the time to reach the maximum ingredient concentration after absorption is much shorter. This is suggestive of rapid absorption, hence the rapid effects.
Delivery methods are most advanced on the system or matrix side rather than on the actual ingredient. Other innovation in delivery systems could be a strip or mouth spray which is especially beneficial if the ingredient used must be absorbed quickly and easily as this is not always the case. Liquids and syrups are a fantastic delivery method especially for the younger generation and the elderly where having to swallow a tablet or capsule can be difficult. Many tasty syrups are already on the market but it’s best to look out for those with no sugar. Effervescent tablets could also be discussed. This is said to be a very fast way of ensuring active absorption. In some regions, this is a very popular way to take paracetamol and sports nutrition/energy where you need to replace sugars, salts and so on in a fast way allowing you to hydrate while replacing vital ingredients for your muscles/energy.
Each application will require a customised bioactive solution for bespoke criteria for efficiency: taste masking & aroma retention, extended & targeted release, moisture, light, oxygen protection, effectiveness improvement, any chemical, preservative-free solution. It is not enough to concentrate on one of these conditions. For a successful application, it is required to have a clear picture of the full life cycle of the product (ingredient), to know the vulnerabilities of the critical ingredients, and the trigger for release at the target location. The product design should include “the total product performance”, covering all relevant aspects of the life cycle.
In-vitro digestion systems are very valuable in this context. The work can be best organized in a multi-partner and multi-disciplinary consortium, to cover all challenging aspects over the full life cycle. Depending on the application and the underlying challenges, the complex systems of approach can be of great help. To obtain insight into what the key parameters are, their hierarchical interrelation and inter-dependences such as in-silico simulations will allow the definition of efficient experimental work.
There are a few areas worth considering when product designers and technologists want to unlock and enhance nutritional, functional and health benefits of bioactives:
- With higher bioavailability, one gets the highest physiological activity of the ingredient.
- With rapid absorption, the onset of action of ingredient should be quick, in other words, ‘fast-acting’ molecules.
- Being natural and inert in nature (like a bilayer), the matrix should possess a minimum to zero interaction level with the drug substances or other food ingredients, ensuring the onsite delivery of the ingredients.
- Safe quick and effective mechanism of action. The ingredients used should be natural in origin, ensuring the safety of the coating.
- The delivery system should be specific where possible and facilitate intake, digestion and absorption – delivering the active to the exact “spot” where it is needed for maximum benefit.
As you can see there are many options for customers to take their daily intake of bioactive to find the delivery system that suits your target consumer. There is no right or wrong delivery system, but the ingredient could be wrong for the delivery system and this is where it could get challenging. Success relies on a balanced combination of formulation and technology. Nanocarrier systems consist of lipid vesicles. These systems based on an edible emulsifier derived from sunflower, which is commonly used in the food industry. Some of these systems are suitable for encapsulating water-soluble and poorly soluble active ingredients, others for lipophilic active ingredients and oils. These lipid vesicles are dispersible in water and have a particle size of 100- 500 nm. Therefore, all encapsulated active ingredients (especially oil-soluble active ingredients) can also be used in aqueous formulations to increase their absorption in the intestine and thus their bioavailability in the body.
Often, companies are not doing the due diligence activities to check whether the finished product can deliver on what the ingredient companies promote and ultimately the consumer is missing out on the promised value and the health benefits.
Would you like to discuss innovation or renovation projects on protection mechanisms for your range of bioactives or how to protect or unlock the health benefits of your product with iNewtrition? If so, please contact Raphaëlle at [email protected] to discuss how we can help you and your team to develop and launch successful consumer-centric products.