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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.
Cellular association studies were performed by flow cytometry. Gene silencing was evaluated with
-overexpressing cells, by flow cytometry and real-time reverse-transcription PCR. Safety and immunogenicity was assessed in CD1 mice.
A strong improvement on siRNA internalization by the target cells was achieved, which was correlated with effective downregulation of
. In addition, the F3-targeted liposomes were nonimmunogenic, even in a multiadministration schedule.
Overall, the developed F3-targeted nanocarrier constitutes a valuable tool for the specific and safe systemic delivery of siRNA to solid tumors.
Original submitted 19 April 2012; Revised submitted 12 September 2012; Published online 8 February 2013