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Purpose <p>&gt;Luteolin, a naturally occurring flavonoid, exhibits potent anticancer activity but is limited by poor aqueous solubility and low oral bioavailability. This study aimed to develop and optimize a niosomal drug delivery system to enhance the solubility, stability, and therapeutic efficacy of luteolin against breast cancer.</p> Methods <p>Luteolin-loaded niosomes were prepared using the ethanol injection method and lyophilized with 2.5% mannitol as a cryoprotectant. A Central Composite Design (CCD) was used to optimize formulation variables, including the Span 60: cholesterol molar ratio, lipid concentration, and sonication time. The optimized formulation was evaluated for particle size, polydispersity index (PDI), zeta potential, entrapment efficiency, surface morphology (via TEM), drug release behavior, and in vitro cytotoxicity against MCF-7 breast cancer cells.</p> Results <p>The optimized niosomal formulation demonstrated a mean particle size of 162.67 ± 2.87&#xa0;nm, PDI of 0.173 ± 0.01, zeta potential of -34.63 ± 1.07 mV, and entrapment efficiency of 87.07 ± 1.69%. TEM confirmed spherical, nanosized particles. XRD analysis revealed reduced crystallinity of luteolin in the formulation, suggesting improved solubility. The in vitro release study showed sustained drug release over 24&#xa0;h in both simulated gastric (78.26 ± 3.87%) and intestinal (81.13 ± 2.85%) fluids. Cytotoxicity study showed significantly enhanced cytotoxicity across all tested concentrations for luteolin-loaded niosomes compared to pure luteolin (LUT), indicating improved anti-cancer potential.</p> Conclusion <p>The developed luteolin-loaded niosomal formulation significantly improved the physicochemical properties and anticancer efficacy of luteolin. These findings suggest that niosomal encapsulation is a promising strategy for enhancing the oral bioavailability and therapeutic potential of luteolin in breast cancer treatment.</p>

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Enhanced Cytotoxicity of Luteolin Via Optimized Niosomal Delivery System Against MCF-7 Breast Cancer Cells

  • 期刊论文

  • 发表日期：

    2026年1月12日

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  • Nikhil Girase,
  • Rakesh Daude,
  • Kailas Moravkar,
  • Shailesh Chalikwar,
  • Ganesh Shevalkar,
  • Bhushan Bhairav

摘要

Purpose

>Luteolin, a naturally occurring flavonoid, exhibits potent anticancer activity but is limited by poor aqueous solubility and low oral bioavailability. This study aimed to develop and optimize a niosomal drug delivery system to enhance the solubility, stability, and therapeutic efficacy of luteolin against breast cancer.

Methods

Luteolin-loaded niosomes were prepared using the ethanol injection method and lyophilized with 2.5% mannitol as a cryoprotectant. A Central Composite Design (CCD) was used to optimize formulation variables, including the Span 60: cholesterol molar ratio, lipid concentration, and sonication time. The optimized formulation was evaluated for particle size, polydispersity index (PDI), zeta potential, entrapment efficiency, surface morphology (via TEM), drug release behavior, and in vitro cytotoxicity against MCF-7 breast cancer cells.

Results

The optimized niosomal formulation demonstrated a mean particle size of 162.67 ± 2.87 nm, PDI of 0.173 ± 0.01, zeta potential of -34.63 ± 1.07 mV, and entrapment efficiency of 87.07 ± 1.69%. TEM confirmed spherical, nanosized particles. XRD analysis revealed reduced crystallinity of luteolin in the formulation, suggesting improved solubility. The in vitro release study showed sustained drug release over 24 h in both simulated gastric (78.26 ± 3.87%) and intestinal (81.13 ± 2.85%) fluids. Cytotoxicity study showed significantly enhanced cytotoxicity across all tested concentrations for luteolin-loaded niosomes compared to pure luteolin (LUT), indicating improved anti-cancer potential.

Conclusion

The developed luteolin-loaded niosomal formulation significantly improved the physicochemical properties and anticancer efficacy of luteolin. These findings suggest that niosomal encapsulation is a promising strategy for enhancing the oral bioavailability and therapeutic potential of luteolin in breast cancer treatment.