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<p>Apigenin, a naturally occurring flavonoid, has attracted increasing attention for its anticancer potential; however, its poor solubility, limited stability, and low cellular availability severely restrict its therapeutic efficacy. In this study, a steroid-based molecular carrier (SBM-1) was employed to construct an apigenin-loaded nanosystem (SBM-1@Api) with the aim of enhancing the physicochemical stability, controlled release behavior, and time-dependent anticancer activity of apigenin. The SBM-1@Api nanosystem exhibited well-defined nanoscale size, improved thermal stability, favorable rheological and interfacial properties, and excellent colloidal stability. Systematic release studies demonstrated that SBM-1@Api enabled temperature- and pH-responsive release of apigenin, governed predominantly by diffusion-controlled kinetics, while significantly prolonging its degradation half-life. In vitro studies using HepG2 and MHCC97-H hepatocellular carcinoma cells revealed that SBM-1@Api exerted markedly stronger and more sustained anti-proliferative effects than free apigenin in a time-dependent manner, without inducing carrier-related cytotoxicity. Collectively, these results demonstrate that SBM-1-based nano-encapsulation effectively overcomes key limitations of free apigenin and provides a robust platform for its sustained and controllable delivery in anticancer applications.</p> Graphical Abstract <p>The steroid-based small-molecule nanosystem (SBM-1@Api) showing environment-sensitive (pH- and temperature-dependent) release behavior and sustained apigenin availability, leading to time-dependent antiproliferative activity in vitro.</p> <p></p>

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A Multi-Stimuli-Responsive Steroid-Based Nanosystem for Apigenin Delivery and Time-Dependent Anti-HCC Activity In Vitro

  • 期刊论文

  • 发表日期：

    2026年1月24日

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  • Luwen Luo,
  • Yaoxiao Liang,
  • Luchang Chen,
  • Weipeng Yang,
  • Shenglin You,
  • Chunying Luo,
  • Cheng Lin

摘要

Apigenin, a naturally occurring flavonoid, has attracted increasing attention for its anticancer potential; however, its poor solubility, limited stability, and low cellular availability severely restrict its therapeutic efficacy. In this study, a steroid-based molecular carrier (SBM-1) was employed to construct an apigenin-loaded nanosystem (SBM-1@Api) with the aim of enhancing the physicochemical stability, controlled release behavior, and time-dependent anticancer activity of apigenin. The SBM-1@Api nanosystem exhibited well-defined nanoscale size, improved thermal stability, favorable rheological and interfacial properties, and excellent colloidal stability. Systematic release studies demonstrated that SBM-1@Api enabled temperature- and pH-responsive release of apigenin, governed predominantly by diffusion-controlled kinetics, while significantly prolonging its degradation half-life. In vitro studies using HepG2 and MHCC97-H hepatocellular carcinoma cells revealed that SBM-1@Api exerted markedly stronger and more sustained anti-proliferative effects than free apigenin in a time-dependent manner, without inducing carrier-related cytotoxicity. Collectively, these results demonstrate that SBM-1-based nano-encapsulation effectively overcomes key limitations of free apigenin and provides a robust platform for its sustained and controllable delivery in anticancer applications.

Graphical Abstract

The steroid-based small-molecule nanosystem (SBM-1@Api) showing environment-sensitive (pH- and temperature-dependent) release behavior and sustained apigenin availability, leading to time-dependent antiproliferative activity in vitro.