Article Summary:
- Berberine’s rapid metabolism in the body and its subsequent elimination from the body leads to poor absorption.
- Advanced berberine formulations that utilize nanodelivery and nutrient encapsulation techniques optimize berberine’s solubility and bioavailability.
Berberine is a naturally occurring bioactive ingredient widely known for helping to maintain healthy blood glucose levels, promoting weight management, supporting cardiovascular functions, and exerting neuroprotective effects.* When taken orally as a nutritional supplement, berberine can help address metabolic conditions by beneficially modulating key metabolic pathways and cellular targets involved in both glucose and lipid metabolism.
Unfortunately, berberine exhibits poor natural absorption and bioavailability. This post explains the factors that affect berberine’s absorption rate and why you should consider taking an advanced berberine supplement formulation to better promote your health and wellness.
Berberine Absorption Rates
Berberine’s superior health-promoting effects are undermined by its poor natural absorption and low bioavailability in the body.
| Only 0.5 percent of orally ingested berberine is actually absorbed in the small intestine, and only 0.36 percent enters the body’s circulation.1 Berberine’s absorption rate in the gut is about 9 percent, resulting in systemic bioavailability of less than 1 percent of an orally administered dose in both animal and human models.2 |
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| Typical Berberine Absorption Rates | |
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| Studies in healthy subjects show that after oral administration of standard berberine formulations, less than 1% of the ingested dose is absorbed into systemic circulation3. | |
| For example, a pharmacokinetic study found that the absorption rate of berberine powder was less than 1%, with plasma concentrations remaining very low after an 800 mg oral dose4. |
Factors that Influence Berberine’s Absorption Rate
The following table highlights several factors that influence berberine’s absorption rate:3
| Factors That Influence Berberine Absorption Rate | |
|---|---|
| Low Solubility | Berberine’s low solubility in water hinders its ability to move across intestinal plasma membranes and be absorbed by epithelial cells. Salt forms of berberine display relatively better bioavailability than free berberine. Berberine molecules tend to self-aggregate in a low pH/acidic environment, which results in poor absorption in the stomach and small intestine. |
| Rapid Metabolism | Berberine is rapidly distributed to the liver, kidneys, muscles, lungs, brain, heart, pancreas, and fat tissues. Most berberine is initially metabolized in the liver and then undergoes extensive intestinal first-pass elimination. Berberine is filtered out of circulation by the liver, resulting in a low level of systemic circulation. Due to its low bioavailability, berberine can easily reach the intestine and interact with the gut microbiota, transforming into metabolites. |
Various innovative approaches have been explored to overcome berberine’s poor natural absorption, including chemical structure modification, conversion of berberine into salt compounds, packaging it with other nutrients, and encapsulation through nanotechnology.
Include an Advanced Berberine Supplement in Your Health Routine/Regimen
Most commercially available berberine supplement formulations contain berberine hydrochloride due to its stability and ease of manufacture. However, berberine hydrochloride is characterized by low water solubility and low intestinal permeability, which together contribute to its poor oral bioavailability4. It is also challenging to mask the bitter taste of the salt. As a result, most berberine supplements have either poor palatability or a limited absorption rate.
On the other hand, a nano-formulated berberine supplement is better absorbed even in a lesser amount than is required with other nutrient delivery methods. A nano-formulated berberine supplement also masks the bitter taste of berberine to better achieve user compliance5.
BerberActiv® is a hypoallergenic berberine supplement developed by Tesseract Medical Research. BerberActiv contains a berberine extract derived from the root of the Berberis aristata plant and its regular use promotes both healthy endocrine function and healthy immune function.*
How is Tesseract’s BerberActiv® different from other commercially available berberine supplements?
- Nanodelivery nutrient technology: Tesseract’s innovative and proprietary CyLoc® – DexKey® nutrient delivery nanotechnology enables the unprecedented absorption of berberine molecules at the desired point in the intestinal tract.
- Enhanced palatability: BerberActive’s berberine is encapsulated in a cyclodextrin matrix that masks its bitter taste, thus enhancing the formula’s palatability.
- Micro-dosing: Enhanced absorption of berberine means micro-dosing is possible—the ingestion of a lesser amount of berberine is needed than previously required to achieve the desired health and wellness outcome.
The advantages of BerberActiv® make berberine a safe and effective reality for promoting optimal gut and endocrine functions.
The power of Tesseract supplements lies in enhancing palatability, maximizing solubility, absorption, and bioavailability, and micro-dosing nutrients in a single, highly effective capsule. Shop products on our website and learn more about how they support healthy endocrine function.*
References:
1https://clinicaltrials.gov/study/NCT03438292?term=AREA%5BBasicSearch%5D(berberine)&rank=2&tab=table
2Moon JM, et al. Nutrients vol. 14,1 124. 28 Dec. 2021, doi:10.3390/nu14010124
3Liu CS, Zheng YR, Zhang YF, Long XY. Research progress on berberine with a special focus on its oral bioavailability. Fitoterapia. 2016;109:274-282. doi:10.1016/j.fitote.2016.02.001
4Khoshandam A, Imenshahidi M, Hosseinzadeh H. Pharmacokinetic of berberine, the main constituent of Berberis vulgaris L.: A comprehensive review. Phytother Res. 2022;36(11):4063-4079. doi:10.1002/ptr.7589
4Sai Durga Surampudi AV, Prasad SR, Ramanujam P, et al. Improving the oral bioavailability of berberine: A crystal engineering approach. Int J Pharm. Published online September 17, 2025. doi:10.1016/j.ijpharm.2025.126177
5Xiong W, Sang W, Linghu KG, et al. Dual-functional Brij-S20-modified nanocrystal formulation enhances the intestinal transport and oral bioavailability of berberine. Int J Nanomedicine. 2018;13:3781-3793. Published 2018 Jun 28. doi:10.2147/IJN.S163763
