Are you wondering about selecting the right berberine supplement from a variety of commercially available product formulations? Get the answers to common queries about the best berberine supplement based on ingredients, delivery technology, bioavailability enhancement, and absorption. Use the links below to jump ahead to different topics on the page.
The Need for A Berberine Supplement
Although berberine is naturally found in the roots, rhizomes, and stem bark of barberry trees, it is not usually found in our daily diets. The therapeutic benefits of berberine support a wide range of health functions, making regular intake important.
| Why Do You Need A Berberine Supplement? | ||
| For enhanced bioavailability: Raw berberine displays poor bioavailability, whereas supplements can be formulated to enhance berberine’s absorption. | ||
| For enhanced palatability: Berberine has a distinctive bitter taste that inhibits patient compliance. Newer supplement formulations enhance the palatability of berberine for oral intake. | ||
| For better absorption: Raw berberine displays poor membrane permeability. Berberine supplements address the shortcomings of unformulated berberine to optimize its solubility and absorption. |
Key Therapeutic Uses of Berberine Supplements
Berberine displays antioxidant properties and helps maintain a balanced inflammatory response in the body.* Berberine is known to regulate several signaling pathways, including AMP-activated protein kinase (AMPK) and nuclear factor κB (NF-κB), which exerts therapeutic benefits. Research studies have established the beneficial impact of berberine supplements on blood glucose levels, lipid levels, and inflammatory markers.* The following are some of the key therapeutic uses of berberine supplements to support health functions.
| System | Therapeutic Uses |
| Endocrine Health* | Berberine supplements promote normal glucose metabolism, including promoting insulin secretion and moderating intestinal absorption of glucose.* Various studies1 have established the potential benefits of berberine for nutritional support in diabetes.* |
| Cardiovascular Health* | Berberine supplements support normal lipid metabolism, which can reduce low-density lipoprotein (LDL) levels and promote cardiovascular health.* |
| Immune Health* | Berberine supplements help maintain immune health by promoting cell-mediated immune responses.* |
| Hepatic Health* | Berberine supplements promote optimal liver detoxification — by decreasing glucose generation from non-carbohydrate precursors and enhancing ammonia detoxification in the liver.* |
| Neuro-Hormonal System* | Berberine supplements optimizethe benefits of exercise and support healthy weight management by limiting exercise-induced exhaustion and muscle damage incurred during exercise.* |
| Gastrointestinal Health* | Berberine supplements promote a balanced and healthy gut microbiota, particularly enhancing growth of short-chain fatty acid (FCSA)-producing bacteria.* |
Berberine Supplement Forms
Berberine’s low bioavailability has led the research community to explore ways to increase its concentration in the blood to therapeutic levels. Injecting berberine offers a direct approach to enhancing its bioavailability by bypassing its breakdown in the gastrointestinal tract. However, injecting berberine can lead to adverse side effects. This makes the oral intake of berberine a more popular and safer approach. As a commercially available nutritional supplement, berberine supplements are available in different forms, including —
- Tablets
- Capsules
- Topical Gels
- Fluid extracts
Berberine Supplement Ingredients
Berberine hydrochloride salt is the key ingredient in a majority of oral berberine supplements, with a single supplement capsule typically containing 400-500 mg of berberine.
Converting berberine molecules into salt compounds is one approach to enhancing bioavailability. Berberine organic acid salts, such as berberine fumarate, berberine citrate, berberine phosphate, and berberine succinate, are used in certain formulations to enhance absorption in the body.
Further, the addition of sodium caprate to a supplement formulation has been found to enhance berberine absorption in the small intestine.
Palatability of Berberine Supplements
Berberine tastes intensely bitter, which impedes patient compliance. Here are several reasons why most berberine supplements have poor palatability.
- Properties of Berberine Chloride: As a primary ingredient in supplements, berberine chloride displays high aqueous solubility and makes it challenging to mask its bitter taste.
- Conventional Delivery Methods: Berberine supplements formulated with conventional delivery methods use higher amounts of berberine chloride salt to counter the poor bioavailability of berberine.
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 best berberine supplement should slow down the release rate of berberine molecules and reduce the concentration of free molecules in the saliva to mask berberine’s taste.
Delivery Technologies Used in Berberine Supplement Formulations
Although berberine has immense pharmacological potential, developing a successful delivery system has remained a challenge. The naturally low bioavailability of berberine and its poor absorption have led to the investigation of alternative modes and methods of nutrient delivery. The following are some of the common delivery technologies used in berberine supplement formulations.
- Conventional Delivery: Traditional delivery is more targeted toward masking the bitterness of a relatively higher amount of berberine present in the formulation. However, the tablet coating process of berberine is not easy to control with accuracy, with coating thickness, uniformity, and tablet adhesion being major challenges. Also, for sugar coating, the amount of coating materials is generally larger.
- Polymer-Based Delivery: Encapsulating berberine in polymers, such as sodium alginate and calcium alginate, is a popular approach to enhance its absorption. Examples of polymer-based supplement formulations include micro-capsules, spheres, particles, and dendrimers (highly-branched polymers). However, polymer-based drug delivery has certain limitations, including low drug loading capacity and cellular toxicity.
- Lipid-Based Delivery: This involves encapsulating berberine in a lipid-based microscopic bubble to prevent its degradation in the gastrointestinal tract. Liposomes, micelles, and micro-emulsions are some of the common lipid-based delivery methods used in these formulations. However, lipid-based delivery is susceptible to enzymatic degradation of active nutrients, displays physical and chemical stability, and has poor oral bioavailability of the active nutrients.
- Nano-Based Delivery: Several formulations use nanotechnology, including cyclodextrins, nanogel, nanoparticles, and nano-suspension, for targeted delivery of berberine at the desired point in the intestinal tract. It is worth noting that a nano-formulated berberine supplement is relatively better absorbed even in lesser amounts than required with other delivery methods while masking the unpalatability of berberine to achieve patient compliance.
Bioavailability Challenges of Berberine Supplements
The absolute bioavailability of berberine is as low as 0.68 percent. Studies2 reveal that less than five percent of an oral dose of berberine is absorbed in the intestine within 2.5 hours of its ingestion. The poor bioavailability of berberine hinders its efficacy in supplement formulations. The following are some of the key factors affecting the absorption of berberine.
| Factors Affecting Berberine Absorption | ||
| Solubility and permeability: The low water-solubility of berberine and its lipophobicity hinder berberine molecules moving across the plasma membrane of intestinal cells. | ||
| Stability in the GI tract environment: The tendency of berberine molecules to self-aggregate in a low pH environment leads to their poor absorption in the stomach and small intestine. | ||
| Extensive Metabolism: Berberine undergoes extensive intestinal first-pass elimination, with a majority of berberine being metabolized in the liver. |
Side Effects of Berberine Supplements
The short-term safety profile of berberine is well-established, although there is limited data about the effects of berberine supplements in pregnant or breastfeeding women. Furthermore, berberine can cause mild or infrequent side effects or potential contraindications when taken with certain prescription medications. The following table highlights some of the common side effects of berberine supplements.
| Berberine Supplement Side Effects | |
| Gastrointestinal side effects include constipation, diarrhea, flatulence, and stomach pain. | |
| Potential risk of low glucose level with prolonged intake of a berberine supplement in high doses. | |
| Potential contraindications with drugs that are metabolized via CYP enzymes. |
Side effects of berberine supplements depend on the delivery route (type of formulation) and the duration of intake of berberine. Hence, it is always recommended to consult with your healthcare provider before including a berberine supplement in your diet or taking one with prescription medications.
Why BerberActiv® is One of the Best Berberine Supplements
When considering the best berberine supplement, you should look for enhanced bioavailability, enhanced palatability, and optimized absorption of the active ingredient molecules.
Tesseract Medical Research’s BerberActiv® is an innovative, palatable, and hypoallergenic berberine supplement that contains a berberine extract derived from the root of the Berberis aristata plant. The following factors make it one of the best berberine supplements on the market.
- Nanodelivery technology: Tesseract’s formulation utilizes the proprietary CyLoc® – DexKey® nutrient delivery nanotechnology for unprecedented absorption of berberine molecules at the desired point in the intestinal tract — one molecule at a time.
- Enhanced Palatability: Encasing individual berberine molecules in their own cyclodextrin fiber delivery cage masks the bitter taste of berberine and enhances the palatability of the formulation.
- Micro-dosing: Enhanced absorption of berberine means that micro-dosing—the ingestion of a lesser amount of berberine— can still achieve a powerful and rapid physiological response to support overall health.
BerberActiv® is manufactured following Good Manufacturing Practices (GMP), implementing scientifically advanced analytical techniques and quality control systems. This ensures the unparalleled efficacy of the supplement formulation in supporting overall health and wellness.
The power of Tesseract nutritional supplements lies in enhancing palatability, maximizing bioavailability and absorption, and micro-dosing multiple nutrients in a single, highly effective capsule. Visit our website for more information about how Tesseract’s products can support your health.*
Citations:
1Guo J, et al. Oxidative medicine and cellular longevity vol. 2021 2074610. 15 Dec. 2021, doi:10.1155/2021/2074610
2Moon JM, et al. Nutrients vol. 14,1 124. 28 Dec. 2021, doi:10.3390/nu14010124
