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<p>This study developed PEGylated liposomal gefitinib (GTL) to overcome clinical limitations of gefitinib therapy in NSCLC, including poor tumor targeting and suboptimal therapeutic outcomes. GTL was formulated using DPPC:cholesterol:mPEG-2000-DSPE (8:7:1) and comprehensively evaluated for tumor treatment efficacy. GTL achieved optimal physicochemical properties (87.7 ± 4.81 nm, EE 60.15%) with polymer relaxation-controlled release kinetics (Super Case II transport, <i>n</i> = 1.0789) providing sustained therapeutic exposure. The GTL demonstrated superior tumor treatment outcomes with threefold enhanced cytotoxicity (IC₅₀: 4.93 <i>vs</i> 15.03 μg/mL) and remarkable <i>in vivo</i> efficacy including 57% tumor volume reduction versus control and 32% superiority over free gefitinib. Comprehensive tumor treatment evaluation revealed enhanced apoptotic activity (68.35% caspase 3/7 activation), near-complete restoration of normal lung architecture, and significant tumor clearance confirmed by histopathological analysis. The controlled release mechanism enabled sustained therapeutic levels while minimizing systemic toxicity. GTL maintained stability for 12 months under ICH conditions, supporting clinical development. This work represents the comprehensive tumor treatment evaluation of gefitinib nanoformulation, demonstrating clinically relevant therapeutic superiority for improved NSCLC patient outcomes.</p> Graphical Abstract <p></p>

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Enhanced Tumor Treatment Outcomes of PEGylated Liposomal Gefitinib in Non-Small Cell Lung Cancer: A Comprehensive Preclinical Evaluation with Superior Therapeutic Efficacy

  • 期刊论文

  • 发表日期：

    2025年10月8日

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  • Rajeshkumar S. Palva,
  • Jolly R. Parikh,
  • Rajnikant M. Suthar,
  • Musaratafrin Saiyed,
  • Mitali Patel,
  • Prajesh Prajapati,
  • Umang H. Shah

摘要

This study developed PEGylated liposomal gefitinib (GTL) to overcome clinical limitations of gefitinib therapy in NSCLC, including poor tumor targeting and suboptimal therapeutic outcomes. GTL was formulated using DPPC:cholesterol:mPEG-2000-DSPE (8:7:1) and comprehensively evaluated for tumor treatment efficacy. GTL achieved optimal physicochemical properties (87.7 ± 4.81 nm, EE 60.15%) with polymer relaxation-controlled release kinetics (Super Case II transport, n = 1.0789) providing sustained therapeutic exposure. The GTL demonstrated superior tumor treatment outcomes with threefold enhanced cytotoxicity (IC₅₀: 4.93 vs 15.03 μg/mL) and remarkable in vivo efficacy including 57% tumor volume reduction versus control and 32% superiority over free gefitinib. Comprehensive tumor treatment evaluation revealed enhanced apoptotic activity (68.35% caspase 3/7 activation), near-complete restoration of normal lung architecture, and significant tumor clearance confirmed by histopathological analysis. The controlled release mechanism enabled sustained therapeutic levels while minimizing systemic toxicity. GTL maintained stability for 12 months under ICH conditions, supporting clinical development. This work represents the comprehensive tumor treatment evaluation of gefitinib nanoformulation, demonstrating clinically relevant therapeutic superiority for improved NSCLC patient outcomes.

Graphical Abstract