Gastrointestinal

Bioavailability Pharmacology: The New Technology Giving Nutraceuticals a Stronger Punch

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 nutraceutical can be absorbed into the bloodstream intact after the body has processed a supplement. This area of research is especially critical for nutraceuticals that are taken orally since it is difficult to precisely measure—and even more difficult to guarantee—uniform absorption throughout the gastrointestinal (GI) tract.

In particular, emerging nutraceutical 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, leading researchers in the field are currently developing more advanced bioavailable nutraceutical delivery systems. In other words, they’re 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 nutraceutical delivery systems available on the market include colloidal delivery, nanomaterial delivery, and extreme 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 in order to titrate—or adjust—dosing and ultimately achieve the best possible medical outcome.

How Lipospheres and Colloidal Drug Delivery Systems Increase Bioavailability

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

Liposphere-based approaches to nutraceutical delivery are essentially based on colloid-forming technologies. Colloids help the nutraceutical to endure the stomach’s highly acidic microenvironment. The lipospheres behave as an emulsifying agent for the nutraceutical, allowing it to become suspended within 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 suffering from GI issues will experience far better absorption rates when using nutraceuticals with liposphere or colloidal delivery systems than with traditional options, which lack delivery systems of any kind.

The Nanodelivery Technologies Improving Bioavailability Pharmacology

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

Nanodelivery systems include nanoencapsulants and nanoattachments. Both protect the nutraceutical from certain metabolic and gastric elements, which leaves more intact for absorption. The difference: nanoencapsulants act as a carriage for the nutraceutical to ride in; nanoattachments are tabs attached to the nutraceutical which are degraded during digestion and metabolism, protecting the nutraceutical 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 nutraceuticals like butyric acid supplements as well. However, a key hurdle that nanotechnology-based delivery systems face in the context of nutraceuticals and pharmacology is their cost efficiency. Nanotechnology is expensive to test and finicky to implement, so it may take time for these solutions to hit the broader nutraceutical market.

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

Improved Bioavailability Pharmacology Via Modern Encapsulation Methods

The newest encapsulation technology being introduced by pharmaceutical companies can increase the bioavailability of supplements as well. 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 which occurs based on specific chemical environments.

Historically, erodibles stumble at delivering nutraceuticals 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 may be ways around this obstacle by simply increasing the amount of time that it takes for the pill to erode. This may cause other dilemmas, however, such as nutraceutical concentrations that are too high in one portion of the GI tract and too low in another. However, when fully refined, erodible nutraceuticals can provide many of the same benefits that the 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 in particular is securing the intellectual property necessary for their manufacture. Many of the most effective erodible formats are patented by the major pharmaceutical companies, which makes 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 nutraceutical companies are able to license the intellectual property.

Nutraceutical bioavailability pharmacology is having its day in the sun and the benefits of these new technologies will be passed directly to patients with gastrointestinal pathologies. Leaning on the pharmaceutical industry’s previous research and insights means that there’s a good chance the breakthroughs being made today can be deployed tomorrow. For example, Tesseract’s patent-pending delivery system is designed specifically to optimize the bioavailability of nutraceuticals 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 nutraceutical therapies. This is vital for patient health; when patients are prescribed or consume supplements with superior bioavailability pharmacology, they experience more effective outcomes and benefits.

The great news is that the development of nutraceutical delivery technology is just getting started—and is expected to quickly make an impact on the bioavailability and effectiveness of butyrate supplements. Whether by improving traditional nutraceutical 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.

Foundational Medicine Review is dedicated to exploring topics around bioavailability pharmacology and modern insights on foundational medicine impacting patients with gastrointestinal and neurological disorders and syndromes. Join our mailing list to receive our monthly newsletter.

Works Cited

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Arora D, Jaglan S. 2016. Nanocarriers based delivery of nutraceuticals for cancer prevention and treatment: a review of recent research developments. Trends in Food Science & Technology. 54:114-126. http://www.sciencedirect.com/science/article/pii/S0924224416301406

Glesson JP, Ryan SM, Brayden DJ. 2016. Oral delivery strategies for nutraceuticals: delivery vehicles and absorption enhancers. Trends in Food Science & Technology. 53:90-101. http://www.sciencedirect.com/science/article/pii/S0924224415301096

Lungare S, Hallam K, Badhana RKS. 2016. Phytochemical-loaded mesoporous silica nanoparticles for nose-to-brain olfactory drug delivery. International Journal of Pharmaceutics. 513(1-2):280-293. http://www.sciencedirect.com/science/article/pii/S0378517316308729

Maroni A, Zema L, Cerea M, Foppoli A, Pagula L, et al. 2016. Erodible drug delivery systems for time-controlled release into the gastrointestinal tract. 32(B):229-235. http://www.sciencedirect.com/science/article/pii/S1773224715300344

McClements DJ. 2017. Recent progress in hydrogel delivery systems for improving nutraceutical bioavailability. Food Hydrocolloids. 68:238-245.
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Moquet PCA, Salami SA, Onrust L, Hendriks WH, Kwakkel RP. 2017. Butyrate presence in distinct gastrointestinal tract segments modifies differentially digestive processes and amino acid bioavailability in young broiler chickens. Poultry Science. 97(1):167-176. https://academic.oup.com/ps/advance-article-abstract/doi/10.3382/ps/pex279/4565720?redirectedFrom=fulltext

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