How to Choose a Supplement: Why Bioavailability is Essential to Ensure Efficacy

How to Choose a Supplement: Why Bioavailability is Essential to Ensure Efficacy

Sep 1st 2021

Article Summary:

  • While supplements can significantly enhance health, many people struggle with choosing a supplement that is safe and effective
  • Bioavailability is one of the most important attributes of a high-quality supplement
  • Choosing a product that is designed to safely optimize bioavailability is the first step toward realizing the benefits of nutritional supplementation

With the help of the right nutritional supplement, many people can experience greater levels of health and fewer symptoms of illnesses than would otherwise be possible. Indeed, nutritional supplements can often successfully make up for dietary shortcomings or address symptoms that are not resolved using conventional therapies. However, consumers are often confused about how to choose a supplement that will deliver meaningful benefits. Unfortunately, nutritional supplements are often of dubious quality, and some products don’t contain any of the ingredients that they advertise.1 When the advertised ingredients are present, many supplements aren’t formulated in a way that allows the body to use those ingredients effectively, which means the majority of each dose will go to waste and the patient is unlikely to experience beneficial effects.

In light of such widespread industry practices, knowing how to choose a supplement that will deliver on its promises can be complicated. But it doesn’t have to be if you know what to look for. In this two-part series, we will explore the fundamentals of effective supplements and how they work in the body as well as how the quality of ingredients can make or break a product. As you begin your search for the right product, it is critical to understand one of the most essential attributes of nutritional supplements: bioavailability.

The Basics of Bioavailability

Bioavailability refers to the proportion of a drug or supplement product that ultimately enters the bloodstream and produces the therapeutic effects after consumption. This is of paramount concern for consumers because supplements formulated for high bioavailability will provide more substantial benefits than those with poor bioavailability.

The bioavailability of a given supplement varies depending on its route of administration as well as the chemical properties of the supplement itself. While intravenously injected medicines are 100% bioavailable, an oral supplement typically results in bioavailability of less than 50% as a result of the digestive process and the metabolic activity of the liver. Depending on the supplement’s formulation, the bioavailability may be even lower, greatly compromising the ability to produce therapeutic effects, and some ingredients aren’t bioavailable at all unless they’re formulated using an appropriate delivery system.

For example, curcumin supplements universally suffer from low bioavailability unless they are specifically designed to survive the gastrointestinal tract and first-pass metabolism in the liver. 2 As a nutritional supplement, curcumin is prized for its anti-inflammatory and antioxidant effects and used for a diverse range of health conditions, including gastrointestinal disorders and neurological diseases. However, curcumin is notorious for its very poor oral bioavailability on account of its low molecular stability, which means that patients taking standard supplements often experience no meaningful benefits. If, on the other hand, patients take a highly bioavailable curcumin supplement, they could derive substantial therapeutic effects with a comparatively smaller dose.

So why don’t supplement manufacturers stick to only creating supplements which are highly bioavailable? The answer is: improving bioavailability is expensive. There is a high cost associated with the chemical and pharmaceutical techniques required to package supplements in a way that allows them to survive digestion and metabolism. In fact, bioavailability is so expensive that many manufacturers end up cutting corners while formulating their supplements to be bioavailable.

Avoiding Harmful or Ineffective Bioavailability Enhancements

Supplement manufacturers can improve bioavailability in a variety of ways depending on the ingredients of a particular product. However, not all methods are created equal; while certain formulation strategies do indeed enhance bioavailability, they do so while sacrificing the tolerability and safety of the product. For example, curcumin supplements that are formulated using compounds like piperine may cause damage to the gastrointestinal tract.3

Piperine is an inexpensive chemical derived from the black peppercorn and is responsible for the sharp flavor and aroma of pepper. Piperine can improve bioavailability because it inhibits the metabolic processes of the liver that break down molecules like curcumin, leaving those molecules intact for the body to use. Inhibiting the liver in this fashion can be dangerous, but patients are far more likely to experience harm from piperine’s negative impact on the gastrointestinal tract, where it activates the pain and heat sensors of nerve cells. Once the nerve cells are activated, the patient can experience inflammation, pain, leaky gut syndrome, and loose stools as a result.

Piperine is a particularly damaging offender as far as supplement ingredients go, but most bioavailability-enhancing formulations and supplement delivery mechanisms do not share the same potential for negative side effects. Instead, some are merely ineffective or of limited use, like the Theracurmin formulation of curcumin. Theracurmin is designed specifically to enhance bioavailability by suspending curcumin molecules in colloidal nanoparticles that can subsequently survive oral administration.4 However, while Theracurmin exhibits significantly higher bioavailability than curcumin powder (which has virtually no bioavailability), its overall bioavailability remains relatively poor; one study found that doubling the supplement’s dose led to a plasma concentration that was only 25% higher than what was observed with the lower dose, indicating that the vast majority of the curcumin was not being utilized by the body.5 As such, picking the right supplement means avoiding pitfalls of seemingly sophisticated supplement delivery systems that fail to deliver real results.

How to Choose a Safe Supplement Engineered for Bioavailability

Considering the prevalence of dangerous or ineffective supplements, how can consumers ensure that the supplements they choose are safe and effective? While there is no perfect method for evaluating a supplement, there are a few rules of thumb that can help you select a high-quality product. Supplements that are highly bioavailable:

  • Use a proven supplement delivery system
  • Do not contain piperine or other problematic bioavailability-increasing chemicals
  • May be more expensive than other products with the same active ingredient
  • May use a lower dose than other products with the same active ingredient

Because many delivery systems and bioavailability practices are proprietary, sticking with a reputable manufacturer is of chief importance. Supplements by Tesseract Medical Research have long been upheld as among the supplement industry’s best on account of their sophisticated bioavailability technology. By developing safe, innovative ways of optimizing bioavailability, Tesseract has been able to unleash the therapeutic potential of ingredients that have historically been of limited use.

Tesseract’s strategy for bioavailability has multiple components. First, Tesseract uses raw materials of the highest quality, such as tetrahydrocurcumin. In contrast to unmetabolized curcumin, tetrahydrocurcumin is naturally bioavailable because it does not need to be metabolized by the liver before it is accessible to the body. Additionally, Tesseract encapsulates its supplements in a specialized delivery system that can weather exposure to stomach acids, preventing loss of bioavailability as the result of digestion. After digestion and passage through the liver, the delivery system degrades, safely dispensing the tetrahydrocurcumin into the bloodstream. Once the supplement is in the bloodstream, it can exert its physiological effects and help patients achieve their health goals. Because Tesseract’s delivery system is based on nanomaterials constructed out of sugars, it is hypoallergenic and extremely unlikely to cause any side effects for patients, which is especially critical for those who are usually sensitive to therapeutics.

Today, Tesseract supplements lead the market as a result of their verified ingredients, high bioavailability, and advanced delivery systems. Thanks to deep experience operationalizing historically challenging ingredients like curcumin, butyric acid, and glutathione, Tesseract is now uniquely positioned to provide consumers with supplements that work. For consumers seeking the right supplement, there’s no better place to start than with their products.

Works Cited

  1. Berry S. 2015. The supplements scandal: herbal pills do not always contain ingredients on label. The Sydney Morning Herald. https://www.smh.com.au/lifestyle/health-and-wellness/the-supplements-scandal-herbal-pills-do-not-always-contain-ingredients-on-label-20150205-1376ec.html
  2. Nelson KM, Dahlin JL, Bisson J, Graham J, Pauli GF, et al. 2017. Curcumin may (not) defy science. ACS Medicinal Chemistry Letters. 8(5):467-470. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5430405/
  3. Dudhatra GM, Mody SK, Awale MM, Patel HB, Modi CM, et al. 2012. A comprehensive review of pharmacotherapeutics of herbal bioenhancers. The Scientific World Journal. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3458266/
  4. Sasaki H, Sunagawa Y, Takahashi K, Imaizumi A, Fukuda H, et al. 2011. Innovative preparation of curcumin for improved oral bioavailability. Biological Pharmacy Bulletin. 34(5):660-665. https://www.ncbi.nlm.nih.gov/pubmed/21532153/
  5. Kanai M, Otsuka Y, Otsuka K, Sato M, Nishimura T, et al. 2013. A phase I study investigating the safety and pharmacokinetics of highly bioavailable curcumin (Theracurmin) in cancer patients. Cancer and Chemotherapy Pharmacology. 71(6):1521-1530. https://www.ncbi.nlm.nih.gov/pubmed/23543271.