Article Summary:
- A majority of berberine supplements currently on the market fail to address its poor bioavailability and bitter taste.
- Nanoformulated berberine is a better alternative than unformulated berberine for superior absorption in the body.
- Tesseract’s BerberActiv® is a revolutionary formulation that enhances the palatability and bioavailability of berberine.
Berberine is a plant alkaloid — a class of nitrogenous organic compounds of plant origin found in many plants, such as Berberis vulgaris (barberry), Hydrastis canadensis (goldenseal), and Berberis aristata (tree turmeric). Berberine has a distinctive yellow color and fluorescence and is known for its various beneficial pharmacological properties. Berberine’s beneficial properties have led to its widespread use as a nutritional supplement supporting different endocrine and immune functions.*
Although berberine is presumed safe for oral ingestion, its poor bioavailability hinders its efficacy. While various formulations have been developed to enhance berberine’s effectiveness, it is challenging to determine which is the most effective berberine supplement for your health. Also, berberine has an intense bitter taste that makes it difficult for oral ingestion. Below, we discuss the factors impacting berberine absorption in the body, its oral intake, and frequently asked questions about how to choose a berberine supplement.
Factors Influencing Berberine Absorption and Oral Intake
The physiochemical properties of berberine impact its oral bioavailability to a large extent. Studies1 reveal that less than 5% of an oral dose of berberine is absorbed in the intestine within 2.5 hours of its ingestion. Let’s look at how the physiochemical properties of berberine, along with the physiological aspects of the gut environment, hinder berberine’s absorption in the body.
| Factors Affecting Berberine Absorption | ||
| Solubility: The water solubility of berberine is relatively low. | ||
| Permeability: Berberine’s lipophobicity hinders its crossing the plasma membrane of intestinal cells. | ||
| Stability in GI tract environment: Berberine molecules tend to self-aggregate in a low pH environment, which results in poor absorption in the stomach and small intestine. | ||
| Metabolism in the gut wall and liver: Berberine undergoes extensive intestinal first-pass elimination, with a majority of berberine being metabolized in the liver. |
The slow rate of dissolution of berberine molecules adversely impacts berberine’s absorption in the body. In addition to its poor bioavailability and absorption, the bitter taste of berberine severely affects patient compliance. The combination of bitter-tasting berberine molecules and the presence of bitter-taste receptors in the oral cavity results in the unpalatability of most berberine supplements.
The chloride salt of berberine, a principal constituent of commercially available berberine supplements, displays high aqueous solubility and makes it challenging to mask its bitter taste. Slowing down the release rate of a supplement formulation and reducing the concentration of free molecules in the saliva is an essential approach to masking berberine’s bitter taste.
FAQs: How to Choose A Berberine Supplement?
Here are some of the frequently asked questions on choosing a berberine supplement to include in your diet.
What is the most absorbable form of berberine?
Dihydroberberine (dhBBR) has a 5-fold greater intestinal absorption rate than berberine, making it the most absorbable form of berberine. Clinical trials2 on rats show that the gut microbiota — the collection of microorganisms that colonize the gastrointestinal tract, converts berberine (BBR) into dhBBR. However, dhBBR is a transient form of BBR in the intestinal lumen and is oxidized back to BBR after its absorption in intestine tissues and, finally, when it enters the blood.
What is the best form of berberine for oral ingestion?
Researchers have used several nanoparticulate approaches, such as solid-lipid nanoparticles, micelles, and liposomes to enhance the bioavailability and absorption of berberine. Nanoformulated berberine supplements developed through solid dispersion or cyclodextrin inclusion to mask the bitterness of berberine appear to be more effective and easier to ingest orally than unformulated berberine.
What should I look for in a berberine supplement?
When choosing a suitable berberine supplement, it is essential to consider palatability, bioavailability, and absorption. BerberActiv®, the proprietary berberine formulation developed by Tesseract Medical Research, utilizes the revolutionary CyLoc® – DexKey® technology to achieve unprecedented absorption of berberine. The CyLoc® matrix masks the unpleasant taste of berberine to vastly enhance its palatability. Available in both quick-release and sustained-release forms, BerberActiv® supports a wide range of critical biochemical pathways to help maintain endocrine and immune health.*
Visit Tesseract Medical Research to learn more about how to choose a berberine supplement and how you can incorporate a berberine supplement into your diet to support various health functions.*
Citations:
1Pan, G, et al. Yao xue xue bao = Acta pharmaceutica Sinica 2003;38(12):911-914.2Feng R, et al. Transforming berberine into its intestine-absorbable form by the gut microbiota. Scientific reports 2015;5:12155., doi:10.1038/srep12155
