Writing in the journal Nutrition and Dietary Supplements, researchers from the United States (Texas Tech University and Increnovo, LLC), India (Radiant Research Services and Medstar Specialty Hospital) and Turkey (Atatürk University) indicated they now have clues into maximizing berberine’s metabolic potential.
“These findings support liposomal formulation as a promising strategy for improving berberine’s bioavailability and potential clinical utility,” the researchers wrote. “Given the small sample size and the inclusion of males only, these findings should be interpreted as exploratory and may not be generalizable to females or broader populations.”
Sebastian Balcombe, founder and CEO of Specnova, the company that sponsored the research, noted that the vastly superior bioavailability results from Specnova’s liposomal berberine versus non liposomal berberine were not surprising.
“I would say it was important to substantiate these results in high quality randomized, double-blind, cross over design study so brands and consumers can understand they can get much more from liposomal berberine versus non liposomal,” he said.
Liposomal efficacy
The alkaloid berberine is a naturally occurring substance found in the stems, roots and rhizomes of some medicinal plants and has been used in traditional Chinese and Ayurvedic medicine.
It has therapeutic benefits for metabolic health, helping to control conditions like hyperglycemia and blood pressure. Despite potential benefits, clinical studies show that berberine is absorbed poorly in the intestine and possesses low in vivo bioavailability.
“Since the late 1990s, liposomal delivery systems have gained commercial and scientific traction, demonstrating improved bioavailability for both hydrophilic and hydrophobic compounds compared with conventional powdered forms,” the researchers explained. “This enhanced performance is attributed to protection from gastrointestinal degradation and improved transmucosal uptake and absorption.”
They added that liposomal delivery systems can improve the oral bioavailability of alkaloids by assisting incorporation into mixed micelles, which aid in digestion and absorption of fats and vitamins. According to the researchers, liposomal delivery also promotes “uptake via intestinal lymphatic pathways, thereby reducing exposure to pre-systemic intestinal metabolism and hepatic first-pass clearance.”
The liposome’s phospholipid bilayer may protect possible degradation in the gastrointestinal environment, though there is limited data to demonstrate this for berberine.
Study details
The study included six healthy male participants who consumed a 400 mg dose of berberine (Specnova LLC, Tysons Corner, VA, USA) either unformulated or liposomal. The researchers collected participant blood samples at hourly increments up to 24 hours post-ingestion to assess plasma berberine.
Participants remained at the research site and followed a low-polyphenol diet, refraining from additional food consumption outside of the scheduled meals.
“Liposomal berberine produced significantly higher pharmacokinetic responses compared with unformulated berberine, including a 70.1% increase in Cmax (p = 0.03) and a 42.8% increase in AUC0–24 (p = 0.03),” the researchers noted. “The results have meaningful implications for improving berberine supplementation in various populations, including athletes, individuals with metabolic or cardiovascular disorders and those with impaired absorption.”
The results indicate liposomal berberine may benefit people suffering from gastrointestinal diseases, pancreatic insufficiency or bile acid deficiency, where lipid digestion is not adequate.
Source: Nutrition and Dietary Supplements. doi: 10.2147/NDS.S582434. “Liposomal Delivery as a Strategy to Improve Berberine Bioavailability: A Double-Blind, Crossover, Randomized Pilot Study in Healthy Males”. Authors: Martin Purpura et al.
