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Purpose <p>The advancement of drug delivery systems has garnered significant interest in cancer therapy, emphasizing the need for targeted and efficient treatment strategies. Among various nanocarriers, zeolitic imidazolate framework-8 (ZIF-8) has emerged as a promising candidate due to its tunable porosity, pH sensitivity, and biocompatibility. This study investigates the development of pH-responsive Imatinib (IM)-loaded ZIF-8 (IM@ZIF-8) nanoparticles for enhanced antileukemic efficacy.</p> Methods <p>A comprehensive preformulation analysis, including Fourier-transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), and differential scanning calorimetry (DSC), confirmed the purity and crystalline nature of IM. IM@ZIF-8 nanoparticles were synthesized via a facile one-pot method and evaluated for drug loading capacity and entrapment efficiency. Structural and morphological characterization was conducted using FTIR, XRD, dynamic light scattering for particle size and zeta potential, and field emission scanning electron microscopy (FESEM).</p> Results <p>The synthesized IM@ZIF-8 nanoparticles exhibited an average particle size of 127&#xa0;nm with high entrapment efficiency (92.7%) and drug loading capacity (84.48%). The in-vitro drug release profile demonstrated significantly higher drug release under acidic conditions (52.88% at pH 5.5) compared to physiological pH (16.19% at pH 7.4), confirming pH-responsive behaviour. Cytotoxicity assessment using the MTT assay on THP-1 leukemia cells showed enhanced anticancer activity of IM@ZIF-8 with a lower IC₅₀ value (3.97&#xa0;µg/mL) compared to free IM (15.43&#xa0;µg/mL), indicating improved therapeutic efficacy and potential for targeted leukemia therapy.</p> Conclusion <p>These findings underscore the potential of ZIF-8 as an effective nanocarrier for pH-responsive drug delivery, offering a promising approach to improving leukemia treatment and reducing the adverse effects associated with conventional chemotherapy.</p> Graphical Abstract <p></p>

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pH-Responsive Zeolitic Imidazolate Framework-8 (ZIF-8) for Targeted Delivery of Imatinib: Enhancing Antileukemic Efficacy

  • 期刊论文

  • 发表日期：

    2026年4月25日

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  • Rasika R. Patil,
  • Durgacharan A. Bhagwat,
  • Namdeo R. Jadhav,
  • Sameer J. Nadaf

摘要

Purpose

The advancement of drug delivery systems has garnered significant interest in cancer therapy, emphasizing the need for targeted and efficient treatment strategies. Among various nanocarriers, zeolitic imidazolate framework-8 (ZIF-8) has emerged as a promising candidate due to its tunable porosity, pH sensitivity, and biocompatibility. This study investigates the development of pH-responsive Imatinib (IM)-loaded ZIF-8 (IM@ZIF-8) nanoparticles for enhanced antileukemic efficacy.

Methods

A comprehensive preformulation analysis, including Fourier-transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), and differential scanning calorimetry (DSC), confirmed the purity and crystalline nature of IM. IM@ZIF-8 nanoparticles were synthesized via a facile one-pot method and evaluated for drug loading capacity and entrapment efficiency. Structural and morphological characterization was conducted using FTIR, XRD, dynamic light scattering for particle size and zeta potential, and field emission scanning electron microscopy (FESEM).

Results

The synthesized IM@ZIF-8 nanoparticles exhibited an average particle size of 127 nm with high entrapment efficiency (92.7%) and drug loading capacity (84.48%). The in-vitro drug release profile demonstrated significantly higher drug release under acidic conditions (52.88% at pH 5.5) compared to physiological pH (16.19% at pH 7.4), confirming pH-responsive behaviour. Cytotoxicity assessment using the MTT assay on THP-1 leukemia cells showed enhanced anticancer activity of IM@ZIF-8 with a lower IC₅₀ value (3.97 µg/mL) compared to free IM (15.43 µg/mL), indicating improved therapeutic efficacy and potential for targeted leukemia therapy.

Conclusion

These findings underscore the potential of ZIF-8 as an effective nanocarrier for pH-responsive drug delivery, offering a promising approach to improving leukemia treatment and reducing the adverse effects associated with conventional chemotherapy.

Graphical Abstract