SLN Mediate Active Delivery of Gefitinib into A549 Cell Line: Optimization, Biosafety, and Cytotoxicity Studies



The present study aimed to prepare and optimize solid lipid nanoparticles (SLN) consisting of fatty acids (FAs; stearic acid), that are actively uptaken by cancer cells.



Enhance cytotoxic activity of chemotherapeutic agent required to increase drug safety profile.



The present study aimed to prepare and optimize solid lipid nanoparticles (SLN) consisting of fatty acids (FAs; stearic acid), that are actively uptaken by cancer cells.



Stability of the prepared SLN formulations was characterized for 90 days. The most stable formulations were loaded with GEF (GEF-SLN) and subjected to pharmaceutical characterization. In-vitro dissolution of GEF-SLN was studied using the dialysis method. Biosafety in the terms of hemocompatibility of the prepared SLN was investigated using fresh blood samples. Additionally, cytotoxicity of GEF-SLN was investigated using the A549 cell line as a surrogate model for lung cancer.



The present results revealed that the prepared SLN formulations were homogeneously distributed in the nanosize range from (114 to 411 nm) with a negative zeta potential value from (-17 to -27 mV). The drug loading increased the particle size of SLN compared to the plain-SLN. Furthermore, PXRD results showed that the degree of stearic acid crystallization was disrupted by the presence of GEF. GEF entrapment efficiency into SLN 88% with a sustained-release profile of about 75% GEF was liberated in 24 h. Hemocompatibility results revealed that all SLN formulations showed insignificant hemolysis (1- 4%) at all concentrations. Moreover, cytotoxicity studies showed that SLN improves GEF anticancer effect compared to free GEF.



These data concluded that, SLN promising approach to enhancing the selective deposition of GEF into cancer cells and reducing the lymphatic metastasis of lung cancer.



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