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Introduction <p>Sorafenib (SOR) is a low-dose multikinase inhibitor that suppresses angiogenesis by blocking vascular endothelial growth factor (VEGF) and platelet-derived growth factor (PDGF) receptors. The aim of the present study was to develop Sorafenib-loaded chitosan (CS) and hyaluronic acid (HA) polyelectrolyte complex nanoparticles (SCH-NP) for triple negative breast cancer (TNBC).</p> Methods <p>For TNBC therapy, SCH-NP were formulated and optimized using Central Composite Design (CCD). The prepared SCH-NP were characterized by particle size, zeta potential, Polydispersity index, Fourier Transform Infrared Spectroscopy (FTIR), entrapment efficiency, invitro drug release study, <i>in-vitro</i>&#xa0;and <i>in vivo</i> studies.</p> Results <p>SCH-NP were formulated and optimized using CCD. The developed SCH-NP showed particle size of 125&#xa0;nm, zeta potential of -13.7&#xa0;mV, PDI value 0.21 and entrapment efficiency of 82.07%. FTIR study confirmed no interaction between drug and polysaccharide. The cumulative release percentage of SOR from SCH-NP was 81.73%. SOR's IC50 value was much larger than, SCH-NP's in both MDA-MB 231 &amp; 4T1 cell lines. After treatment for 18&#xa0;days, the tumor volumes in mice increased to 447.4 mm<sup>3</sup> (Phosphate buffer solution), 263.6 mm<sup>3</sup> (pure SOR), treatment with SCH-NP results in a noteworthy decrease in the tumor volumes in mice by 66.1% (151.3 mm<sup>3</sup>).</p> Conclusions <p>The present study suggests that SCH-NP might be effective for the tumor-targeted delivery of Sorafenib and it might be a suitable nanocarrier for enhancing SOR cytotoxicity <i>in vitro</i> and may be useful for the tumor-targeted delivery&#xa0;of SOR.</p>

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Development and optimisation of Polyelectrolyte Complex Nanoparticles Loaded with Sorafenib by Central Composite Design (CCD): In Vitro and In Vivo Studies for the Treatment of Triple Negative Breast Cancer

  • 期刊论文

  • 发表日期：

    2025年12月10日

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  • Sangita A. Kale,
  • Savita S. Deokar,
  • Karimunnisa S. Shaikh

摘要

Introduction

Sorafenib (SOR) is a low-dose multikinase inhibitor that suppresses angiogenesis by blocking vascular endothelial growth factor (VEGF) and platelet-derived growth factor (PDGF) receptors. The aim of the present study was to develop Sorafenib-loaded chitosan (CS) and hyaluronic acid (HA) polyelectrolyte complex nanoparticles (SCH-NP) for triple negative breast cancer (TNBC).

Methods

For TNBC therapy, SCH-NP were formulated and optimized using Central Composite Design (CCD). The prepared SCH-NP were characterized by particle size, zeta potential, Polydispersity index, Fourier Transform Infrared Spectroscopy (FTIR), entrapment efficiency, invitro drug release study, in-vitro and in vivo studies.

Results

SCH-NP were formulated and optimized using CCD. The developed SCH-NP showed particle size of 125 nm, zeta potential of -13.7 mV, PDI value 0.21 and entrapment efficiency of 82.07%. FTIR study confirmed no interaction between drug and polysaccharide. The cumulative release percentage of SOR from SCH-NP was 81.73%. SOR's IC50 value was much larger than, SCH-NP's in both MDA-MB 231 & 4T1 cell lines. After treatment for 18 days, the tumor volumes in mice increased to 447.4 mm3 (Phosphate buffer solution), 263.6 mm3 (pure SOR), treatment with SCH-NP results in a noteworthy decrease in the tumor volumes in mice by 66.1% (151.3 mm3).

Conclusions

The present study suggests that SCH-NP might be effective for the tumor-targeted delivery of Sorafenib and it might be a suitable nanocarrier for enhancing SOR cytotoxicity in vitro and may be useful for the tumor-targeted delivery of SOR.