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Controlled and Sustained Release of Bioactive Ingredients

Controlled and Sustained Release of Bioactive Ingredients

Winston A. Samuels, Ph.D., Maxx Performance Inc.

Customers are constantly demanding the highest quality and integrity in the nutritional supplements they consume. They want products that taste good and provide health benefits based on superior performance ingredients. They want to know that a supplement works and that it contains the level of ingredients shown on the label. For manufacturers, the wellness product industry is fraught with processing challenges caused by the inherently sensitive nature of bioactive substances. Whether it is the premature reaction or release of ingredients when combined or the damaging effects of environmental conditions such as heat, oxygen, moisture, light or pH, the result is products that can taste or smell bad, release too quickly and/or do not deliver on their therapeutic promise because of reduced bioavailability.

Nutrient Protection and Delivery

The Maxx System of nutrient protection and delivery enables protection of nutrients from processing and storage losses. Maxx microencapsulation has an excellent capacity to protect bioactive molecules against temperature, humidity, and acidic conditions and allow a controlled release of these compounds during passage through the gastrointestinal tract. Maxx microencapsulation protects vitamin C (ascorbic acid) from traditional losses during processing and storage and delivers this essential nutrient in a highly bioavailable form for use in different fortification applications. The technology allows one to regulate

  • The specific time, temperature and release of nutrients up and down the gastrointestinal tract. The release is triggered by factors such as pH and enzyme activity
  • The release of active nutrients for precise delivery
  • The release of active nutrients or biologics at precise absorption sites

Shield nutrients from

  • Temperature and pH changes
  • Microbial degradation
  • Degradation and undesirable interactions
  • Air, light and metal to maintain potency
  • Nuisance, dust control of ingredients


  • Stabilized free-flowing nutrients with longer shelf life
  • Nutrients to replenish the antioxidant status associated with stress
  • Biologics for inclusion in different food and dietary supplements preparations that involves higher temperature
  • Nutrients cost effectively
  • Taste masking of undesirable flavors and odors while delivering desirable attributes
  • Consistent nutrient quality

Ingredient Limitations

Supplement manufacturers have tried to overcome ingredient limitations in a variety of ways. It is a common practice to add extra excipients to minimize ingredient interactions, however this takes up valuable space in oral dosage forms and only partly solves the problem. Often, overdosing is used to achieve a label claim by compensating for expected stability losses, but that can be expensive, arguably harmful and can negatively impact the flavor system. Some ingredients, such as Arginine Ethyl Ester, B-vitamins, certain minerals, alpha lipoic acid, choline, fish oils and many botanicals may be avoided entirely because of their taste, odor or stability, which greatly limits formulation creativity and effectiveness. Melatonin and other similar substances may lose their effectiveness because of their quick release. Coenzyme Q10 because of its morphology is tacky, does not flow freely and creates processing challenges. These issues and others are why Maxx Performance microencapsulation has emerged as an excellent processing tool to solve many challenges with problematic ingredients.


Microencapsulation is a technology with a long history in the pharmaceutical, nutritional and food science fields. The latest advances in drug delivery have their roots in basic microencapsulation. Simply put, microencapsulation is a process whereby small particles, such as bioactive substances, are protected from their environment by enveloping them with a protective barrier coating material.

The technology allows a compound to be encapsulated inside a tiny sphere that can be as small as 15 microns, about half the thickness of a human hair. Like the pharmaceutical industry, the food and supplement industries have adopted this technology and adapted it to meet their special needs. Microencapsulated ingredients can be designed to release core bioactives through a variety of mechanisms. Coating materials can be selected to dissolve slowly or quickly in stomach acid, or only when a certain pH is reached. Microencapsulation enables formulators to strike the proper balance between protection, which means improved bioavailability.

What exactly is bioavailability?

Bioavailability is frequently defined as the degree to which an ingredient becomes available at the site of physiological activity. It is the amount of a compound that is absorbed or available for therapeutic action, relative to the amount originally provided. In foods and supplements, very few compounds are directly ingested in their raw form. They are typically ingested as part of a complex matrix of nutrients and ingredients. The losses in bioavailability of a compound may start during formulation, continue through product manufacturing, including shelf life instability, and any enteric losses either through premature degradation or through incomplete digestion or release. Most importantly, bioavailability is a function of both ingredient stability and subsequent availability.

Microencapsulation: Applications Benefits

Protect Labile Nutrients. Some raw ingredients are especially sensitive to environmental conditions; ascorbic acid is a good example. Vitamin C is very labile and many aspects of processing destroy its stability. Unprotected ascorbic acid is readily oxidized and loses its activity when exposed to air. Losses in potency are exacerbated under complex processing conditions such as tableting and extrusion. Not only does Maxx Performance microencapsulation improve time zero retention (comparing raw ascorbic versus microencapsulated ascorbic immediately after processing), it also significantly slows degradation in the finished product. In one study, nearly 50 percent of the ascorbic acid was lost just from tableting and only about 10 percent was still there after six months, whereas nearly 70 percent of the microencapsulated ascorbic acid was still available after six months under similar storage conditions. Microencapsulated Ascorbic Acid, through its increased stability in air and more gradual release over time of its antioxidant (Oxygen scavenging) properties is a convenient method to provide added nutritional value through product fortification.

Gut Health. Probiotics (beneficial bacteria and enzymes) are another category of very unstable ingredients. Live organisms are very difficult to work with because they are so susceptible to oxidative losses. Most probiotic products on the shelf today are not viable; the organisms are no longer there in the quantities to be useful—processing and storage have killed them. Fortunately, recent advances in microencapsulation technology have allowed for excellent shelf stability and viability of live beneficial bacteria, even through food processing (hot and cold systems) and prolonged shelf life. Moreover, microencapsulation from Maxx Performance can protect the organisms from low pH in gastric fluids, and can release the organisms lower in the intestinal tract where they provide the greatest health benefit. Probiotics from Maxx Performance are being used in nutrient bars, bakery products, malt type beverages and dry mixes.
Heart Health. Indeed, there are many oxidatively sensitive materials that are very important in human nutrition and health. Omega-3 fatty acids are another example. Additionally, Anthocyanins have been shown to protect against oxidative damage from superoxide radicals, hydrogen peroxide and other oxidants. Here, too, microencapsulation makes it possible to stabilize very unstable bioactive substances so they can do their job. Taking it yet another step, Maxx Performance has the technology that allows these oils to be used in many more delivery systems by converting the oil to a free-flowing powder, if required. Marketers are no longer limited in the product forms they can use to sell these ingredients. They can go beyond softgel capsules to tablets, two-piece capsules, nutrient bars and powdered beverages, to name a few.

Masks Taste and Off Odors. By using proprietary new microencapsulation technology individual particles are coated with a thin film which permits ingredients such as choline, caffeine, fish oil, flax seed, B-vitamins, minerals and other ingredients to be incorporated into different finished products without the taste and off odor. Product developers can now formulate without the chalky taste of calcium. Maxx microencapsulation prevents oxidation and rancidity of Omega-3 fatty acids and choline allowing them to be used in finished goods without the characteristic fishy rancid taste and off odor. The technology is also used to coat B vitamins and minerals to mask their typical bitter and metallic taste and prevent the oxidation of iron to overcome rancidity and off odor, mask objectionable colors and permit manufacturers to use them in end products.

Microencapsulation: The Value Proposition.

Improve Stability and Bioavailability. Maxx Microencapsulation is changing the way product developers create new food and supplement products. Many doors have been opened because microencapsulation technology can regulate, shield and deliver bioactive substances in precisely defined ways. The ultimate question for manufacturers and consumers remains, however, what is the value of using microencapsulated ingredients to improve stability and subsequent bioavailability? This value proposition can be tested in many ways, some more objective than others. Clearly, using 10 times the starting dose of raw ascorbic acid in order to have enough to meet label claims after six months is a cost that can be compared, especially with the current cost of raw ascorbic acid, against the price of Maxx Microencapsulated Ascorbic Acid (other issues aside, such as toxicity and regulatory compliance of using so much vitamin C). Iron can be highly reactive in foods, especially in its most bioavailable form Ferrous Sulfate. Nearly all commonly used minerals for fortification (zinc, copper, iron) present problems and are easily overused unless scaling is controlled. Avoiding the bad taste and odor of a raw ingredient such as caffeine, B-vitamins, metal compounds, amino acids for example by using a microencapsulated form adds cost to the finished product, but if the product never sells because of its bad taste, it becomes another product failure. Therefore, what is the cost of product failures and false promises? Microencapsulation should be considered when asking that question.

Increase Stability and Extend Shelf Life, Prevent Premature Reactions, Mask Odors and Flavors. Maxx Performance through its proprietary new microencapsulation technology has the capability to mask taste and off odor, mask objectionable colors, of many beneficial ingredients, extend shelf life, prevent ingredient interactions, prevent moisture pick up, remove tackiness, and make ingredients free-flowing without any change in processing. Microencapsulation is a vehicle to facilitate the controlled and sustained release of labile nutrients up and down the gastrointestinal tract.

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