Nanomedicines for targeted delivery of etoposide to non-small cell lung cancer using transferrin functionalized nanoparticles

Abstract

Lung cancer is the most common cause of cancer death. Clinical applications of anticancer drugs are limited due to non-specificity and systemic toxicity. Transferrin (Tf) receptors have been recognized to be up-regulated in several malignant carcinomas including non-small cell lung cancer. Herein, we investigate the anticancer activity of Tf conjugated and etoposide (ETPS) loaded solid lipid nanoparticles (Tf-ESN) against Tf-receptors expressing A549 human non-small cell lung cancer cells. Pharmacokinetic and tissue-distribution profiles of nanoparticles were studied in Balb/c mice. Targeted nanoparticles showed significantly higher anticancer activity of etoposide manifested by anti-proliferation assay, morphological changes and induced apoptosis in A549 cells. In biodistribution studies, Tf-ESN had higher plasma concentration, longer blood circulation and decrease in clearance of encapsulated ETPS than Etosid®, a marketed formulation of etoposide. In conclusion, the promising results of this study suggest that targeting of nanomedicines to Tf-receptors, those that are over expressed in non-small cell lung cancer could increase the therapeutic efficacy of lung cancer therapy.