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<p>Berberine, an isoquinoline alkaloid, is a compound of interest due to its structural diversity and wide range of biological activities; however, its pharmacological effects are significantly limited by poor intestinal absorption. In this study, a novel formulation approach was employed to improve the bioavailability of berberine by formulating lipid-polymer hybrid nanoparticles (BER-LPHN) using a modified nanoprecipitation method. The formulation was optimized using a 3<sup>2</sup> full factorial design, incorporating Phospholipon 90 H as the lipid and Gantrez as the hydrophilic polymer. The optimized BER-LPHN exhibited a nanosize of 250–350&#xa0;nm and a zeta potential of -25.00 ± 2.2&#xa0;mV, with notably high drug loading (~ 87%). TEM analysis revealed the spherical morphology of the BER-LPHN, with the lipid coat surrounding the polymeric matrix, which facilitated controlled drug release from the polymeric core <i>in vitro</i>, resulting in an 18-fold increase in the oral bioavailability of berberine. <i>In-vivo</i> studies using fluorescently labeled nanoparticles demonstrated a significant concentration of BER-LPHN near the villi boundary and significant uptake by Peyer’s patches. Confocal microscopy further confirmed the lymphatic uptake of BER-LPHN through M cells of Peyer’s patches, suggesting that the formulated nanoparticles have the potential to enhance berberine's bioavailability by boosting permeability in the intestine via lymph transport.</p> Graphical Abstract <p></p>

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Overcoming Bioavailability Barriers: Optimized Hybrid Nanocarrier System to Amplify Berberine Absorption via Peyer’s Patches

  • 期刊论文

  • 发表日期：

    2025年11月11日

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  • Shubhangi A. Thool,
  • Varsha B. Pokharkar

摘要

Berberine, an isoquinoline alkaloid, is a compound of interest due to its structural diversity and wide range of biological activities; however, its pharmacological effects are significantly limited by poor intestinal absorption. In this study, a novel formulation approach was employed to improve the bioavailability of berberine by formulating lipid-polymer hybrid nanoparticles (BER-LPHN) using a modified nanoprecipitation method. The formulation was optimized using a 32 full factorial design, incorporating Phospholipon 90 H as the lipid and Gantrez as the hydrophilic polymer. The optimized BER-LPHN exhibited a nanosize of 250–350 nm and a zeta potential of -25.00 ± 2.2 mV, with notably high drug loading (~ 87%). TEM analysis revealed the spherical morphology of the BER-LPHN, with the lipid coat surrounding the polymeric matrix, which facilitated controlled drug release from the polymeric core in vitro, resulting in an 18-fold increase in the oral bioavailability of berberine. In-vivo studies using fluorescently labeled nanoparticles demonstrated a significant concentration of BER-LPHN near the villi boundary and significant uptake by Peyer’s patches. Confocal microscopy further confirmed the lymphatic uptake of BER-LPHN through M cells of Peyer’s patches, suggesting that the formulated nanoparticles have the potential to enhance berberine's bioavailability by boosting permeability in the intestine via lymph transport.

Graphical Abstract