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<p>Oxy-Berberine (OBBR) is a metabolite of berberine (BBR) an isoquinoline alkaloid with promising hepatoprotective activity. But due to its lower aqueous solubility, and less retention time at site of action its clinical translation is limited. The present study aimed to develop and characterize a novel OBBR and ascorbic acid co-crystal (OBACC) incorporated in collagen microspheres (OBACC-CMPs) to enhance the solubility, release and hepatoprotective activity of OBBR. In-vitro solubility study showed that ~ 1.70-fold higher solubility of OBACC as compared to the plain drug in aqueous media. Further, FT-IR, DSC, and XRD are carried out to investigate the drug, polymer, and excipients interactions. The morphology study by scanning electron microscope showed porous and spherical shape of microsphere at a size range of 5&#xa0;μm. In-vitro drug release study revealed the controlled release manner of OBBR for 6&#xa0;h at the site of action and release kinetics followed Korsemeyar-Peppas model. The in-vitro cell internalization study ensures the higher cellular uptake for 6&#xa0;h as compared to the control and good cytocompatibility was observed at higher dose of microspheres in HepG2 cell line. In-vivo study emphasized the effectiveness of OBACC-CMPs on liver marker enzymes, proteins, lipid profile, cytokines and oxidative markers as compared to the PCM induced toxicity in rat model. Also, a prolonged accumulation of OBBR for 16&#xa0;h was observed in bio-distribution study of OBACC-CMPs. Furthermore, the study highlights the OBACC-CMPs promising, safe and effective application for hepatoprotective and liver targeted applications. </p> Graphical Abstract <p></p>

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Development and characterization of oxy-berberine co-crystal incorporated in collagen microspheres with enhanced hepatoprotective activity

  • 期刊论文

  • 发表日期：

    2026年7月11日

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  • Anindya Bagchi,
  • Anusree Raha,
  • Ajit Mishra,
  • Jitu Halder,
  • Rakesh Kumar Sahoo,
  • Vineet Kumar Rai,
  • Tushar Kanti Rajwar,
  • Debajyoti Das,
  • Bibhanwita Satpathy,
  • Priyanka Dash,
  • Chandan Das,
  • Saroj Kumar Rout,
  • Biswakanth Kar,
  • Goutam Ghosh,
  • Goutam Rath

摘要

Oxy-Berberine (OBBR) is a metabolite of berberine (BBR) an isoquinoline alkaloid with promising hepatoprotective activity. But due to its lower aqueous solubility, and less retention time at site of action its clinical translation is limited. The present study aimed to develop and characterize a novel OBBR and ascorbic acid co-crystal (OBACC) incorporated in collagen microspheres (OBACC-CMPs) to enhance the solubility, release and hepatoprotective activity of OBBR. In-vitro solubility study showed that ~ 1.70-fold higher solubility of OBACC as compared to the plain drug in aqueous media. Further, FT-IR, DSC, and XRD are carried out to investigate the drug, polymer, and excipients interactions. The morphology study by scanning electron microscope showed porous and spherical shape of microsphere at a size range of 5 μm. In-vitro drug release study revealed the controlled release manner of OBBR for 6 h at the site of action and release kinetics followed Korsemeyar-Peppas model. The in-vitro cell internalization study ensures the higher cellular uptake for 6 h as compared to the control and good cytocompatibility was observed at higher dose of microspheres in HepG2 cell line. In-vivo study emphasized the effectiveness of OBACC-CMPs on liver marker enzymes, proteins, lipid profile, cytokines and oxidative markers as compared to the PCM induced toxicity in rat model. Also, a prolonged accumulation of OBBR for 16 h was observed in bio-distribution study of OBACC-CMPs. Furthermore, the study highlights the OBACC-CMPs promising, safe and effective application for hepatoprotective and liver targeted applications.

Graphical Abstract