Targeted Chimera Delivery to Ovarian Cancer Cells by Multifunctional Ruthenium Polypyridine Nanoparticles

Abstract Background: In vivo efficient delivery of small interfering RNAs (siRNAs) to the targeted tumor cells has remained a significant challenge in clinical applications. Ruthenium (II) polypyridyl complexes have emerged both as anticancer agents and imaging theranostic agents because of unique photophysical and cytotoxic properties. However, a major limitation in their clinical implementation is effective cancer cell selectivity. In the present study, we present a novel targeted siRNA delivery platform obtained by ruthenium polypyridine complex nanoparticles (RPN).Results: The chimera molecules constructed by EGFR RNA aptamer and Notch3 siRNA, the chimera loaded RPN exhibited much higher silencing efficiency against Notch3 gene compared with chimera alone and lipofectamine-siRNA complex, and improved the antitumor effects of chimera in vitro and in vivo against ovarian cancer, indicating its potential capability for future targeted cancer therapy via RPN mediated chimera delivery. Conclusions: Overall, this work describes, to the best of our knowledge, the first in vivo study demonstrating the targeted chimera delivery into tumor cells by multifunctional ruthenium polypyridine nanoparticles.