Bioavailability of berberine: challenges and solutions

#1

Berberine is a quaternary benzylisoquinoline alkaloid with multiple pharmacological effects used for the treatment of hyper- tension, tumors, bacterial infections, inflammation, HIV, and cardiac diseases.

In phase I clinical trials, berberine is safe at ex- cessive doses but manifests poor bioavailability. Major challenges like poor absorption, rapid metabolism, and rapid systemic elimination are responsible for low plasma and tissue levels of berberine.

Various strategies have been undertaken by several researchers to overcome this issue and enhance the bioavailability of berberine. This includes the design of new formulation strategies; novel drug delivery systems (NDDS) like liposomes, nanosized dosage forms, phospholipid complexes, muco- adhesive microparticles, and micoemulsions; the use of adjuvants; and the design of structural analogous of berberine.

This review focuses on the occurrence of berberine in numerous plants and its pharmacological activities as evidenced through numerous preclinical and clinical studies. The later part of this review highlights the bioavailability issue of berberine which arises due to its poor absorption, elevated rate and extent of metabolism, and quick elimination and clearance from the body. A systematic effort has beenmade to analyze the various formulation strategies, including the design of newer berberine analogues and derivatives. These strategies can be further explored to increase the bioavailability, medicinal value, and ap- plication of this promising molecule.

PDF copy of the paper.

Bioavailability of berberine_ challenges and solutions.pdf (258.6 KB)

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#2

Anyone here taking Berberine? Are you tracking your blood glucose levels - and how does the berberine help you exactly?

#3

Yes, I have taken berberine on and off for a few years. I start it when I read some new pro berberine paper and stop after a few months when it has no noticeable effect on my blood glucose. Even large doses daily before meals had no noticeable effect that I could see.

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#4

Berberine has a notoriously low bioavailability, less than 5% of supplementation gets in your system. You can mix it with fat if you open up a capsule. I tried a few times with olive oil, but it is so bad tasting that I stopped doing it and went over to Metformin. I will try NOW Foods supplement capsule where they add MCT oil for better absorption, that idea makes sense.

#5

I switched to adding empagliflozin which I get from India and is as cheap or cheaper than berberine and actually helps reduce my blood sugar levels.

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#6

I added berberine (slow release dihydroberberine…more bioavailable), some literature on ameliorating lipids (my keto diet), but I found NO discernible impact, including hbA1c. Has some AMPK signalling potential like metformin. Don’t have high conviction, considering dropping from my stack.

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#7

You might try liposomal berberine. I know that Alive By Nature offers such but I can’t speak to its bioavailability.

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