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<p>The efficient pulmonary delivery of the third-generation EGFR-TKI osimertinib (OSI) is hindered by its low solubility and systemic toxicity. This study aimed to enhance OSI delivery by incorporating it into lactoferrin nanoparticles (LF-NPs) and comparing it with bovine serum albumin nanoparticles (BSA-NPs). The nanoparticles were synthesized using the desolvation method and characterized via dynamic light scattering (DLS), zeta potential, and field emission scanning electron microscopy (FE-SEM). LF-NPs exhibited superior drug loading (DL = 54.54%) and loading efficiency (LE = 49.03%) relative to BSA-NPs (DL = 43.38%, LE = 38.99%), with hydrodynamic sizes below 225 nm and a moderate negative surface charge. Molecular docking studies using the GOLD software indicated higher predicted binding propensity of OSI toward LF (GOLD fitness score = 63.6; unitless), mediated by a hydrogen bond with Glu664, suggesting receptor-specific interactions. Cytotoxicity assays on H1975 lung cancer cells and human dermal fibroblasts (HDF) demonstrated that OSI-LF-NPs significantly enhanced the selectivity index (SI = 7.06) compared to free OSI (SI = 2.95), while reducing toxicity toward normal cells. Despite a modest increase in IC50 for cancer cells relative to the free drug, the LF-based delivery system exhibited improved biocompatibility and targeted action. These findings support the potential of lactoferrin nanoparticles as a promising bio-carrier for OSI, warranting further in vivo evaluation for NSCLC-targeted therapy.</p>

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Osimertinib-Loaded Lactoferrin Nanoparticles for Lung Cancer Therapy

  • 期刊论文

  • 发表日期：

    2025年9月18日

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  • Zainab Sabri Abbas,
  • Zaizafoon N. Nasif,
  • Amer T. Tawfeeq

摘要

The efficient pulmonary delivery of the third-generation EGFR-TKI osimertinib (OSI) is hindered by its low solubility and systemic toxicity. This study aimed to enhance OSI delivery by incorporating it into lactoferrin nanoparticles (LF-NPs) and comparing it with bovine serum albumin nanoparticles (BSA-NPs). The nanoparticles were synthesized using the desolvation method and characterized via dynamic light scattering (DLS), zeta potential, and field emission scanning electron microscopy (FE-SEM). LF-NPs exhibited superior drug loading (DL = 54.54%) and loading efficiency (LE = 49.03%) relative to BSA-NPs (DL = 43.38%, LE = 38.99%), with hydrodynamic sizes below 225 nm and a moderate negative surface charge. Molecular docking studies using the GOLD software indicated higher predicted binding propensity of OSI toward LF (GOLD fitness score = 63.6; unitless), mediated by a hydrogen bond with Glu664, suggesting receptor-specific interactions. Cytotoxicity assays on H1975 lung cancer cells and human dermal fibroblasts (HDF) demonstrated that OSI-LF-NPs significantly enhanced the selectivity index (SI = 7.06) compared to free OSI (SI = 2.95), while reducing toxicity toward normal cells. Despite a modest increase in IC50 for cancer cells relative to the free drug, the LF-based delivery system exhibited improved biocompatibility and targeted action. These findings support the potential of lactoferrin nanoparticles as a promising bio-carrier for OSI, warranting further in vivo evaluation for NSCLC-targeted therapy.