Development of an Innovative Berberine Food-Grade Formulation with an Ameliorated Absorption: In Vitro Evidence Confirmed by Healthy Human Volunteers Pharmacokinetic Study

Abstract

Objective. To evaluate in vitro solubility, bioaccessibility, and cytotoxic profile, together with a pharmacokinetic profile by oral administration to healthy volunteers of a novel food-grade berberine formulation (BBR-PP, i.e., berberine Phytosome®). Results. An in vitro increase of solubility in simulated gastric and intestinal fluids and an improved bioaccessibility at intestinal level along with a lower cytotoxicity with respect to berberine were observed with BBR-PP. The pharmacokinetic profile of the oral administration to healthy volunteers confirmed that berberine Phytosome® significantly ameliorated berberine absorption, in comparison to unformulated berberine, without any observed side effects. The berberine plasma concentrations observed with both doses of BBR-PP were significantly higher than those seen after unformulated berberine administration, starting from 45 min (free berberine) and 30 min (total berberine). Furthermore, BBR-PP improved berberine bioavailability (AUC) was significantly higher, around 10 times on molar basis and with observed dose linearity, compared to the unformulated berberine. Conclusion. These findings open new perspectives on the use of this healthy berberine formulation in metabolic discomforts.

Effect of Berberine Phytosome on reproductive, dermatologic, and metabolic characteristics in women with polycystic ovary syndrome: a controlled, randomized, multi-centric, open-label clinical trial

“…Frontiers in Pharmacology frontiersin.org administration of pure berberine (Petrangolini et al, 2021), can produce clear positive effects. This was evident from the analysis of the parameters commonly used as references in the diagnosis of PCOS, such as insulin resistance, lipid profile, hyperandrogenism (both biochemical and clinical) and inflammatory balance.…”

“…The product is named Berberine Phytosome ® (BP). When administered to healthy volunteers, absorption is improved by up to ten-fold in comparison with pure berberine (Petrangolini et al, 2021). BP, in a small pilot study performed on 12 Caucasian, PCOS-diagnosed women, has demonstrated a significant decrease in Homeostasis Model Assessment (HOMA), C-Reactive Protein (CRP), TNF-α, triglycerides, testosterone, Body Mass Index (BMI), Visceral Adipose Tissue (VAT), fat mass, and acne severity, along with a significant increase in sex hormone-binding globulin (SHBG) (Rondanelli et al, 2021).…”

Gut Microbiota, Metabolic Disorders and Breast Cancer: Could Berberine Turn Out to Be a Transversal Nutraceutical Tool? A Narrative Analysis

“…Finally, it should be noted that, as often happens in the use of nutraceuticals and/or phytotherapics, despite the main problem of inclusion in clinical practice, caused by the poor bioavailability of the compounds and the low quantity of drugs that reach their destination, for BBR, this problem has now been overcome by associating it with silymarin (milk thistle extract) used as a herbal bioenhancer and inhibitor of the major glycoprotein P (gp-P) responsible for poor cellular absorption [ 54 ], or by producing it in phytosomal forms such as a recent commercially available formulation [ 55 , 56 , 57 ].…”

Berberine: A Perspective Compound in the Development of New Medicines

“…Trong một nghiên cứu đánh giá sản phẩm phytosome BBR, Giovanna Petrangolini đã công bố độ hoà tan BBR clorid từ viên phytosome BBR cao hơn 3-4 lần so với BBR tự do ở cả môi trường dịch dạ dày và dịch ruột nhân tạo. Đánh giá dược động học trên người tình nguyện, phytosome BBR với 1 và 2 liều tương ứng BBR 188 mg so với BBR tự do liều 452 mg cao hơn 4 và 6 lần [62].…”