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Bioavailability Pharmacology: Exploring New Technology

Updated on December 22, 2022

  • Bioavailability is key to the therapeutic efficacy of nutritional supplements, but ensuring bioavailability can be challenging due to the nature of both the ingredients in nutritional supplements and the digestive tracts of patients.
  • A variety of innovative mechanisms and formulations have been developed to help optimize the bioavailability of nutritional supplements, including lipospheres and colloidal drug delivery systems, as well as nanodelivery technologies.
  • New encapsulation and release methods developed by Tesseract Medical Research help patients benefit from ingredients that have historically presented significant barriers to bioavailability, including butyrate.

Researchers face a unique challenge when studying bioavailability pharmacology: as a result of the process of digestion, the many contours of the intestinal system each have unique chemical microenvironments. Bioavailability pharmacology is the degree to which an active ingredient in a nutritional supplement can be absorbed into the bloodstream intact after the body has processed the supplement. This area of research is especially critical for nutritional supplements taken orally because it is difficult to precisely measure—and even more difficult to guarantee—uniform absorption throughout the gastrointestinal (GI) tract.

In particular, emerging nutritional supplement delivery systems are exciting news for the field of butyrate supplements. These supplements are especially sensitive to geographical bioavailability during absorption in the GI tract because butyric acid has varying physiological effects depending on which area absorbs the highest concentration from the supplement. For patients suffering from gastrointestinal issues to achieve systemic benefits from butyric acid supplements, the supplements must be absorbed in the distal colon rather than near the hepatic portal vein after metabolism by the liver.

To overcome this biological dilemma, researchers are currently developing more advanced delivery systems. In other words, they are working on creating supplements that are more effectively absorbed, allowing them to achieve passage through the blood-brain barrier. Based on preliminary research, the results appear promising.

Currently, advanced delivery systems available on the market include colloidal delivery, nanomaterial delivery, and superior refinements of traditional encapsulation techniques that finely tune bioavailability and absorption. Gastrointestinal doctors and patients alike must understand the differences between each of these delivery systems to adjust dosing and ultimately achieve the best possible medical outcome.How Lipospheres and Colloidal Drug 

Delivery Systems Increase Bioavailability

Although many pharmaceutical drugs already leverage the power of lipospheres, they have only recently been introduced into the arena of nutritional supplements. Lipospheres encapsulate ingredients in fatty acids to make them fat soluble, allowing for efficient delivery of the macromolecule. Macromolecules have traditionally suffered from steep first-pass digestive degradation that reduces the number of intact and still biologically active macromolecules that make it to the liver and beyond; partially degraded macromolecules don’t have the same physiological effects as intact ones. Ingredients enclosed in a liposphere bubble experience minimal digestive degradation and thus maintain a higher concentration of the macromolecule until its arrival at the intended delivery site.

Liposphere-based approaches to ingredient delivery are essentially based on colloid-forming technologies. Colloids help ingredients survive the stomach’s highly acidic microenvironment. Lipospheres behave as an emulsifying agent, allowing the ingredient to be suspended in a protective barrier.

Liposphere and colloidal delivery systems have already been proven effective in pharmaceutical environments and are now being introduced into the realm of bioavailability pharmacology. While they still require first-pass metabolism after digestion, patients with GI issues will experience far better absorption rates when using nutritional supplements with liposphere or colloidal delivery systems than with traditional options, which lack delivery systems of any kind.

Nanodelivery Technologies Improve Bioavailability Pharmacology

Nanoparticle-based delivery systems provide a molecularly-targeted means of bypassing undesirable metabolic or gastric gateways detrimental to the absorption rate of a nutritional supplement—and thus its bioavailability. In fact, attaching a nutritional supplement’s ingredients to nanoparticles can allow for bypassing first-pass metabolism entirely.

Nanodelivery systems include nanoencapsulants and nanoattachments. Both protect the ingredient from certain metabolic and gastric elements, which leaves more of the ingredient intact for absorption. The difference: nanoencapsulants act as a carriage for the supplement to ride in; whereas, nanoattachments are tabs attached to the supplement that are degraded during digestion and metabolism, protecting the supplement itself from being degraded and thus increasing its bioavailability.

Nanocarriers that encapsulate pharmaceutical drugs for oral administration have been proven effective for increasing bioavailability. This effectiveness translates to butyric acid supplements as well. However, a key hurdle that nanotechnology-based delivery systems face in the context of both nutritional supplements and pharmacology is their cost efficiency. Nanotechnology is expensive to test and finicky to implement, so it will likely take time for these solutions to hit the broader nutritional supplement market.

Nanodelivery systems have a short history of use in pharmaceutical delivery systems, and shorter still for the delivery of nutritional supplements. The cost of this technology also means it likely faces an uphill battle for implementation. However, the potential for extremely high bioavailability with nanotechnological delivery systems means that supplement developers are heavily incentivized to continue research.

Improved Bioavailability Pharmacology Via Modern Encapsulation Methods

The newest encapsulation technology being introduced by pharmaceutical companies can also increase the bioavailability of supplements. Cutting edge encapsulation drug delivery methods are effective at surviving entry into the GI tract. This is due to advances in multi-phasic capsule degradation that occurs based on specific chemical environments.

Historically, erodibles stumble at delivering nutritional supplements to exact structures of the GI tract if their chemical environments are too similar for the capsule’s dissolving mechanism to differentiate between. But there might be ways around this obstacle by simply increasing the amount of time that it takes for the capsule to erode. This might cause other dilemmas, however, such as ingredient concentrations that are too high in one portion of the GI tract and too low in another. However, when fully refined, erodible supplements can provide many of the same benefits that more complex technologies do in the quest to improve bioavailability.

The sensitivity of the delivery environment is the primary challenge of erodibles; however, a crucial challenge for pharmacology is securing the intellectual property necessary for their manufacture. Many of the most effective erodible formats are patented by major pharmaceutical companies, making them expensive to license. Continued refinements of encapsulation, erosion, and time-released technologies aren’t the most exciting advancements in drug delivery, but they’re the most likely to be deployed and extensively tested, provided that supplement companies are able to license the intellectual property.

Bioavailability pharmacology is having its day in the sun, and the benefits of these new technologies will be passed directly to patients with GI pathologies. Leaning on the pharmaceutical industry’s previous research and insights means there’s a good chance the breakthroughs being made today can be deployed tomorrow. For example, Tesseract Medical Research’s patent-pending delivery system is designed specifically to optimize the bioavailability of nutritional supplements via unique encapsulation and release mechanisms that allow for maximum therapeutic efficacy. This technology is ushering in the next wave of bioavailability pharmacology, changing the very foundation of what we can expect from supplement therapies. When patients are prescribed or consume supplements with superior bioavailability pharmacology, the technology enables them to experience more effective outcomes and benefits.

The great news is that the development of delivery technology for nutritional supplements is just getting started—and is expected to quickly make an impact on the bioavailability and effectiveness of butyrate supplements. Whether by improving traditional formulations, implementing more sophisticated nanotechnology schemes, or exploring colloidal and lipid-based solutions, bioavailability is an obstacle that’s being overcome, one research paper at a time.

Tesseract Medical Research is dedicated to exploring topics around bioavailability pharmacology and modern insights on foundational medicine impacting patients with gastrointestinal and neurological disorders.

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Al Czap, Founder | Tesseract

Al Czap has more than four decades of professional experience in preventative medicine. He founded Thorne Research in 1984 (sold in 2010) and he published Alternative Medicine Review for 17 years beginning in 1996. AMR was a highly acclaimed, peer-reviewed, and indexed medical journal. Al was the first to recognize the need for hypoallergenic ingredients and to devise methods of manufacture for and delivery of hypoallergenic products to underserved patient populations. His work has greatly impacted those with impaired immune and digestive systems and compromised health due to environmental exposures.

The advanced formulations based on our revolutionary, patented, and patent-pending technology are only available through Tesseract. No other medical, pharmaceutical, or supplement company is licensed to utilize our proprietary technology.
*These statements have not been evaluated by the Food and Drug Administration. These products are not intended to diagnose, treat, cure, or prevent any disease.
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