Efficient intracellular delivery of siRNA with a safe multitargeted lipid-based nanoplatform

Gomes-da-Silva LC, Fernández Y, Abasolo I, Schwartz S Jr, Ramalho JS, Pedroso de Lima MC, Simões S, Moreira JN.

Nanomedicine (Lond). 2013 Sep;8(9):1397-413.

http://www.futuremedicine.com/doi/abs/10.2217/nnm.12.174

Abstract

AIM:

The design of novel F3-targeted liposomes with adequate features for systemic administration, to enable efficient intracellular delivery of siRNA toward both cancer and endothelial cells from angiogenic blood vessels.

MATERIALS & METHODS:

Cellular association studies were performed by flow cytometry. Gene silencing was evaluated with eGFP-overexpressing cells, by flow cytometry and real-time reverse-transcription PCR. Safety and immunogenicity was assessed in CD1 mice.

RESULTS:

A strong improvement on siRNA internalization by the target cells was achieved, which was correlated with effective downregulation of eGFP. In addition, the F3-targeted liposomes were nonimmunogenic, even in a multiadministration schedule.

CONCLUSION:

Overall, the developed F3-targeted nanocarrier constitutes a valuable tool for the specific and safe systemic delivery of siRNA to solid tumors.