Functionalized selenium nanoparticles for targeted delivery of doxorubicin to improve non-small-cell lung cancer therapy

Abstract

Yu Xia, Yi Chen, Liang Hua, Mingqi Zhao, Tiantian Xu, Changbing Wang, Yinghua Li, Bing Zhu Virus Laboratory, Guangzhou Institute of Pediatrics, Guangzhou Women and Children’s Medical Center, Guangzhou Medical University, Guangzhou, People’s Republic of China Background: Selenium nanoparticles (SeNPs) loaded with chemotherapeutic drugs provided a novel perspective for cancer therapy.Materials and methods: Here, SeNPs were modified with cyclic peptide (Arg–Gly–Asp–D-Phe–Cys [RGDfC]) to fabricate tumor-targeting delivery carrier RGDfC-SeNPs and, then, doxorubicin (DOX) was loaded to the surface of RGDfC-SeNPs for improving the antitumor efficacy of DOX in non-small-cell lung carcinoma therapy.Results: The chemical structure characterization of RGDfC-Se@DOX showed that DOX was successfully loaded to the surface of RGDfC-SeNPs to prepare functionalized antitumor drug delivery system RGDfC-Se@DOX. RGDfC-Se@DOX exhibited effective cellular uptake in A549 cells and entered A549 cells mainly by clathrin-mediated endocytosis pathway. Compared to free DOX or Se@DOX at the equivalent dose of DOX, RGDfC-Se@DOX showed greater activity to inhibit A549 cells’ proliferation and migration/invasion and induce A549 cells’ apoptosis. More importantly, compared with passive targeting delivery system Se@DOX, active targeting delivery system RGDfC-Se@DOX exhibited more significant antitumor efficacy in vivo.Conclusion: Taken together, RGDfC-Se@DOX may be a novel promising drug candidate for the lung carcinoma therapy. Keywords: nanoscale drug carrier, antitumor, chemotherapy, RGDfC peptide, apoptosis 

Keywords

• lung carcinoma
• tumor targeting
• RGDfC peptide
• doxorubicin
• nanoparticles