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<p>The IL-6 signalling pathway plays a significant role in the progression and development of squamous cell carcinoma (SCC). Bazedoxifene is a potent inhibitor of IL-6R; however, its efficacy is limited by its low solubility in water (0.54&#xa0;mg/mL). In contrast, BAZE-X1, a formulation of bazedoxifene using sulfobutylether-β-cyclodextrin (SBECD), exhibits enhanced solubility (38&#xa0;mg/mL). The preparation of this formulation was confirmed through X-ray diffraction and differential scanning calorimetry, while the structure of the bazedoxifene complex with SBECD was elucidated using 1D and 2D NMR spectroscopy. Although BAZE-X1 (10.0 µmol/L; 5.3&#xa0;µg/mL) demonstrated no toxicity toward SCC cell lines (SCC13, LLSCC1, and FaDu), its effect on IL-6-dependent proliferation was significantly better than that of tocilizumab. The reduction in nuclear accumulation of pSTAT3 (Ser727) by BAZE-X1 was confirmed using In-Cell Western analysis. In the scratch assay, BAZE-X1, like tocilizumab, exhibited antimigratory effects against LLSCC1 but not against SCC13. However, in the context of 3D models (SCC13, LSCLC1, and FaDu), BAZE-X1 (1.0 and especially 5.0 µmol/L; 2.65 and 0.53&#xa0;µg/mL) displayed a potent antimigration effect.</p>

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Novel soluble bazedoxifene formulation gains antiproliferative and migrastatic effect in squamous cell carcinoma cells

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2026年3月17日

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  • Lukáš Lacina,
  • Zdeněk Kejík,
  • Tomáš Pacák,
  • Martina Koziar Vašáková,
  • Lucie Hoznauerová,
  • Jiří Škopek,
  • Roman Ziegler,
  • Jan Brábek,
  • Jan Hajduch,
  • Kateřina Veselá,
  • Robert Kaplánek,
  • Pavel Martásek,
  • Karel Pacák,
  • Karel Smetana Jr.,
  • Milan Jakubek

摘要

The IL-6 signalling pathway plays a significant role in the progression and development of squamous cell carcinoma (SCC). Bazedoxifene is a potent inhibitor of IL-6R; however, its efficacy is limited by its low solubility in water (0.54 mg/mL). In contrast, BAZE-X1, a formulation of bazedoxifene using sulfobutylether-β-cyclodextrin (SBECD), exhibits enhanced solubility (38 mg/mL). The preparation of this formulation was confirmed through X-ray diffraction and differential scanning calorimetry, while the structure of the bazedoxifene complex with SBECD was elucidated using 1D and 2D NMR spectroscopy. Although BAZE-X1 (10.0 µmol/L; 5.3 µg/mL) demonstrated no toxicity toward SCC cell lines (SCC13, LLSCC1, and FaDu), its effect on IL-6-dependent proliferation was significantly better than that of tocilizumab. The reduction in nuclear accumulation of pSTAT3 (Ser727) by BAZE-X1 was confirmed using In-Cell Western analysis. In the scratch assay, BAZE-X1, like tocilizumab, exhibited antimigratory effects against LLSCC1 but not against SCC13. However, in the context of 3D models (SCC13, LSCLC1, and FaDu), BAZE-X1 (1.0 and especially 5.0 µmol/L; 2.65 and 0.53 µg/mL) displayed a potent antimigration effect.