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Background <p>Capecitabine (CPB) is a widely used chemotherapeutic agent; however, its clinical effectiveness is limited by poor site-specific delivery and rapid degradation in the gastrointestinal tract. This study aimed to enhance the therapeutic efficacy of CPB by formulating solid lipid nanoparticles (SLNs) using a modified spontaneous nanoprecipitation method.</p> Methods <p>CPB-loaded SLNs were prepared and characterized for particle size, polydispersity index (PDI), zeta potential (ZP), drug loading, entrapment efficiency, and morphology, zeta analysis, and transmission electron microscopy (TEM). Fourier transform infrared spectroscopy (FTIR) was conducted to assess drug–excipient compatibility. In vitro drug release studies were performed in simulated gastric (pH 1.2) and intestinal (pH 6.8) fluids. Cytotoxicity was evaluated on HT-29 colon cancer cells using the MTT assay, with 5-fluorouracil as the standard control.</p> Results <p>The optimized formulation (F-3) exhibited a mean particle size of 22.93 ± 0.17&#xa0;nm, drug loading (31.27 ± 0.53%) and entrapment efficiency (45.49 ± 0.26%), and a zeta potential of − 20.30 ± 0.26 mV, indicating colloidal stability. FTIR analysis confraphical abstractd continued slow release over 12&#xa0;h at pH 6.8. MTT assay results demonstrated significant cytotoxicity of CPB-SLNs against HT-29 cells after 48&#xa0;h, comparable to or exceeding the effect of the standard drug.</p> Conclusion <p>The developed CPB-loaded SLNs exhibit promising physicochemical and biological characteristics, including controlled drug release and enhanced cytotoxicity. These findings suggest their potential as a novel oral delivery system for improving the therapeutic efficacy of CPB in colon cancer treatment.</p> Graphical Abstract <p></p>

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Innovations in Drug Formulation: A Focus on Capecitabine-Loaded Solid Lipid Nanoparticles

  • 期刊论文

  • 发表日期：

    2025年10月17日

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  • Mayukh Jana,
  • Chandra Sekhar Patro,
  • Suraj Sharma,
  • Sweet Naskar,
  • Ujjwal Kumar Biswas,
  • Biplab Debnath

摘要

Background

Capecitabine (CPB) is a widely used chemotherapeutic agent; however, its clinical effectiveness is limited by poor site-specific delivery and rapid degradation in the gastrointestinal tract. This study aimed to enhance the therapeutic efficacy of CPB by formulating solid lipid nanoparticles (SLNs) using a modified spontaneous nanoprecipitation method.

Methods

CPB-loaded SLNs were prepared and characterized for particle size, polydispersity index (PDI), zeta potential (ZP), drug loading, entrapment efficiency, and morphology, zeta analysis, and transmission electron microscopy (TEM). Fourier transform infrared spectroscopy (FTIR) was conducted to assess drug–excipient compatibility. In vitro drug release studies were performed in simulated gastric (pH 1.2) and intestinal (pH 6.8) fluids. Cytotoxicity was evaluated on HT-29 colon cancer cells using the MTT assay, with 5-fluorouracil as the standard control.

Results

The optimized formulation (F-3) exhibited a mean particle size of 22.93 ± 0.17 nm, drug loading (31.27 ± 0.53%) and entrapment efficiency (45.49 ± 0.26%), and a zeta potential of − 20.30 ± 0.26 mV, indicating colloidal stability. FTIR analysis confraphical abstractd continued slow release over 12 h at pH 6.8. MTT assay results demonstrated significant cytotoxicity of CPB-SLNs against HT-29 cells after 48 h, comparable to or exceeding the effect of the standard drug.

Conclusion

The developed CPB-loaded SLNs exhibit promising physicochemical and biological characteristics, including controlled drug release and enhanced cytotoxicity. These findings suggest their potential as a novel oral delivery system for improving the therapeutic efficacy of CPB in colon cancer treatment.

Graphical Abstract