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image of Formulation and in vitro Evaluation of Targeted Chemotherapy of Crizotinib-loaded polymeric Nanoparticles on Cancer Cell Lines

Abstract

Introduction

Crizotinib, an inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, holds significant potential for the treatment of lung cancer. However, its toxicities present a major challenge to its clinical use. To enhance the targeted delivery of Crizotinib to lung tumors, polymeric-based nanoparticles were developed.

Methods

Crizotinib-loaded polymeric nanoparticles were prepared using a nano-precipitation method, incorporating stearic acid as the lipid, polyethylene glycol as the polymer, and Tween 80 as the surfactant. Key formulation parameters were optimized to achieve high-quality nanoparticles.

Results

The optimized formulation exhibited a mean particle size of 142 nm, a zeta potential of -31.9 mV, an entrapment efficiency of 82.35%, and an drug release of 60.69%. These nanoparticles were then tested on lung cancer cell lines to assess their cytotoxicity, apoptosis induction, and anti-proliferative effects on the cell cycle. studies confirmed that the Crizotinib-loaded nanoparticles exerted targeted effects on non-small cell lung carcinoma (NSCLC) cell lines, showing maximum inhibitory effects. One year of storage at 4°C, stability testing demonstrated that the lyophilized nanoparticles maintained their effectiveness.

Discussion

crizotinib nano-formulations were assessed for a variety of physicochemical and characterization. Five different formulations were designed and optimized on the basis of Particle size, Zeta potential, %EE, and drug release. Optimum formulation also showed maximum inhibitory effect on the cancer cell line.

Conclusion

This nanotechnology approach offers a promising targeted drug delivery system for Crizotinib, characterized by small particle size, high encapsulation efficiency (EE), and optimal drug release.

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2025-08-12
2025-12-13

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Formulation and in vitro Evaluation of Targeted Chemotherapy of Crizotinib-loaded polymeric Nanoparticles on Cancer Cell Lines
Bentham Science Publishers ; https://doi.org/10.2174/0113816128412622250730015435
/content/journals/cpd/10.2174/0113816128412622250730015435
/content/journals/cpd/10.2174/0113816128412622250730015435
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  • Article Type:     Research Article
Keywords: in vitro drug release ; Crizotinib ; lung cancer ; small cell lung carcinoma (NSCLC) ; targeted drug delivery ; polymeric nanoparticles

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