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Background <p>Polyphenols have garnered significant interest because of their potential health benefits, but their bioavailability is limited. According to recent studies, in vivo metabolites of phenol compounds may mediate their biological activity, potentially countering systemic oxidation and inflammation and therefore reducing multi-organ dysfunction associated with gut microbiota alterations. This pre-clinical study aims to characterize a novel formulation, enhancing metabolite bioavailability, ensuring long-term stability, and employing sustainable production methods. Our research provides the first evidence of the presence of these metabolites in the blood plasma of animals receiving different Bergamot polyphenols fraction (BPF) formulations.</p> Methods <p>Male Sprague-Dawley were used throughout the study. The animals were subdivided into three groups of six animals each receiving 50&#xa0;mg/kg of BPF standard (BPF), 50&#xa0;mg/kg of Bergamot polyphenols fraction micronized (BPFmicro), and 50&#xa0;mg/kgof Bergamot polyphenols fraction encapsulation (BPFencap), respectively, by oral gavage. Blood samples were collected, and plasma was prepared with a specific protocol and analysed for the presence of primary and secondary metabolites through ultra-high performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS).</p> Results <p>UHPLC-MS/MS analysis showed significantly higher plasma concentrations of naringin and its metabolites in the BPFencap group compared to the BPF standard and BPFmicro groups at all time points. In comparison to BPF, plasma Area Under Curve (AUC) analysis of metabolites revealed substantially elevated values for the BPFencap group and substantially reduced values for the BPFmicro group.</p> Conclusion <p>While BPFmicro greatly increased bioavailability, the improvement was only temporary, highlighting a stability problem. The bioavailability and stability of metabolites are significantly improved over time by the new BPFencap formulation (micronized BPF in hybrid phospholipid systems with citrus albedo fibers).</p> Graphical abstract <p></p>

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The second life of Citrus bergamia: bioavailability analysis of a new formulation using waste-based microencapsulation as a valuable source of bioactive compounds

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2025年7月25日

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  • Maria Serra,
  • Roberta Macrì,
  • Sonia Bonacci,
  • Giovanna Ritorto,
  • Sara Ussia,
  • Saverio Nucera,
  • Rosamaria Caminiti,
  • Stefano Ruga,
  • Carmen Altomare,
  • Luigi Tucci,
  • Giuseppe Trunfio,
  • Donato Cosco,
  • Antonio Procopio,
  • Carolina Muscoli,
  • Rocco Mollace,
  • Vincenzo Mollace

摘要

Background

Polyphenols have garnered significant interest because of their potential health benefits, but their bioavailability is limited. According to recent studies, in vivo metabolites of phenol compounds may mediate their biological activity, potentially countering systemic oxidation and inflammation and therefore reducing multi-organ dysfunction associated with gut microbiota alterations. This pre-clinical study aims to characterize a novel formulation, enhancing metabolite bioavailability, ensuring long-term stability, and employing sustainable production methods. Our research provides the first evidence of the presence of these metabolites in the blood plasma of animals receiving different Bergamot polyphenols fraction (BPF) formulations.

Methods

Male Sprague-Dawley were used throughout the study. The animals were subdivided into three groups of six animals each receiving 50 mg/kg of BPF standard (BPF), 50 mg/kg of Bergamot polyphenols fraction micronized (BPFmicro), and 50 mg/kgof Bergamot polyphenols fraction encapsulation (BPFencap), respectively, by oral gavage. Blood samples were collected, and plasma was prepared with a specific protocol and analysed for the presence of primary and secondary metabolites through ultra-high performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS).

Results

UHPLC-MS/MS analysis showed significantly higher plasma concentrations of naringin and its metabolites in the BPFencap group compared to the BPF standard and BPFmicro groups at all time points. In comparison to BPF, plasma Area Under Curve (AUC) analysis of metabolites revealed substantially elevated values for the BPFencap group and substantially reduced values for the BPFmicro group.

Conclusion

While BPFmicro greatly increased bioavailability, the improvement was only temporary, highlighting a stability problem. The bioavailability and stability of metabolites are significantly improved over time by the new BPFencap formulation (micronized BPF in hybrid phospholipid systems with citrus albedo fibers).

Graphical abstract