Hypoglycemic and Hypolipemic Effects of a New Lecithin Formulation of Bergamot Polyphenolic Fraction: A Double Blind, Randomized, Placebo- Controlled Study

Abstract

Objective: Hyperlipemia represents an independent risk factor in the development of atherosclerosis in patients undergoing type 2 diabetes mellitus (DM). Moreover, the pharmacological treatment of dyslipemia in patients undergoing type 2 DM (e.g. by means of statins), is accompanied by relevant side effects and oral supplementation with natural antioxidants, such as Citrus polyphenols, has recently been suggested to improve cardioprotection in such patients. However, due to the poor gastrointestinal absorption of polyphenols, novel formulations have recently been developed for getting a better bioavailability of polyphenolic rich fractions of citrus species extract rich in polyphenols. Methods: Here, we investigated the effect of standard bergamot polyphenolic fraction (BPF®) as well as of its phytosomal formulation (BPF Phyto), in patients with type 2 DM and hyperlipemia. A randomized, double blind, placebo-controlled study was carried out in 60 patients suffering from type 2 DM and mixed hyperlipemia. </P><P> Patients were divided into three groups: one receiving placebo, the second receiving standard BPF and the third BPF Phyto. Results: In the groups receiving BPF and BPF Phyto, a significant reduction of fasting plasma glucose, serum LDL cholesterol and triglycerides accompanied by increased HDL cholesterol was observed. This effect was associated with significant reduction of small dense atherogenic LDL particles, as detected by means of proton NMR Spectroscopy, thus confirming the hypolipemic and hypoglycemic effect of bergamot extract both when using standard formulation as well as BPF Phyto. No differences were seen in the therapeutic response among groups receiving BPF and BPF Phyto, thus suggesting a substantial bioequivalence in their hypoglycemic and hypolipemic profile. However, when comparing the pharmacokinetic profile of naringin (the major component of BPF) and its metabolites, in patients treated with BPF Phyto, an at least 2,5 fold increase in its absorption was found, confirming in human studies the better profile of BPF Phyto compared to standard BPF. Conclusion: These data suggest that better absorption and tissue distribution of BPF Phyto formulation represents an innovative approach in supplementation treatments of cardiometabolic disorders.

Prevention and Treatment of Atherosclerosis: The Use of Nutraceuticals and Functional Foods

“…In randomized, double-blind studies carried out in hyperlipemic and type 2 diabetes subjects, a remarkable effect of BPF was found in terms of reducing fasting blood glucose, LDL cholesterol, and triglycerides and increasing HDL cholesterol (Cai et al 2017;Toth et al 2015). In another study, a lecithin formulation (to increase bioavailability) of BPF, already successfully tested at the preclinical level, was used at a daily dose of 1,000 mg (corresponding to 400 mg of BPF) (Mollace et al 2019). Lipid-lowering and hypoglycemic effects similar to those of BPF at a dose of 1,300 mg were recorded (Mollace et al 2019).…”

“…In another study, a lecithin formulation (to increase bioavailability) of BPF, already successfully tested at the preclinical level, was used at a daily dose of 1,000 mg (corresponding to 400 mg of BPF) (Mollace et al 2019). Lipid-lowering and hypoglycemic effects similar to those of BPF at a dose of 1,300 mg were recorded (Mollace et al 2019). All these data must be, obviously, confirmed in other randomized clinical trials before the BPF can become part of the therapeutic armamentarium (Nauman and Johnson 2019).…”

Healthy Protection Of Bergamot Is Linked To The Modulation Of Microbiota

“…A recent paper reported a decrease in both triglycerides and LDL-C after 8-week treatments of a nutraceutical mixture containing BPF in dislypidemic overweight patients [19]. A signi cant reduction of serum low density lipoprotein cholesterol (LDL-C) and triglyceride was also demonstrated by a new bergamot phytosome formulation [9]: in that clinical study, the delivery by phytosome allowed increased oral absorption of the naringin, the major component of bergamot, in respect to standard unformulated bergamot. Actually, phytosome techniques have recently demonstrated the successful delivering of other low-soluble natural compounds, like quercetin [20] and Coenzyme Q10 [21].…”

“…A lecithin food-grade delivery system (Phytosome®) containing the Bergamot Polyphenolic Fraction (BPF) from Citrus Bergamia Risso et Poiteau from Calabria was developed by Indena SpA to ameliorate the oral absorption of avonoids. The structural phytochemical composition of bergamot was deeply analysed by HPLC-DAD-MS and LC-NMR [8], and a recent clinical trial in individuals with type 2 diabetes mellitus and hyperlipaemia showed a reduction of cardiovascular risk by modulating total cholesterol (tChol), low-density Lipoproteins (LDL), triglycerides (TG), high-density Lipoproteins (HDL) and blood glucose after just 30-day supplementation [9].…”

Non-pharmaceutical treatment of dyslipidemia: review of current methods of diet and nutraceuticals

“…И наконец, некоторые исследования продемонстрировали у бергамота достоверный гипогликемический и противовоспалительный эффекты [49]. В связи с описанным профилем действия применение данного агента может оказаться весьма успешным у лиц с метаболическим синдромом.…”