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Folate-Mediated Targeted Delivery of siPLK1 by Leucine-Bearing Polyethylenimine
Lu Hou1,2, Zheyu Song3, Zhonghang Xu3
1College of Life Science, Jilin University, Changchun, Jilin 130012, People's Republic of China.
Background:
siRNA-mediated polo-like kinase 1 (PLK1) silencing has been proposed as a promising therapeutic method for multiple cancers. However, the clinic application of this method is still hindered by the low specific delivery of siPLK1 to desired tumor lesions. Herein, folate (FA)-modified and leucine-bearing polyethylenimine was successfully synthesized and showed excellent targeted silencing to folate receptor overexpressed cells.
Materials And Methods:
The condensation of siPLK1 by FA-N-Ac-L-Leu-PEI (NPF) was detected by the gel retardation assay. The targeted and silencing efficiency was evaluated by flow cytometry and confocal laser scanning microscope. The PLK1 expressions at gene or protein levels were detected by quantitative real-time PCR and Western blotting assay. Further impacts of the PLK1 silencing on cell viability, cell cycle, migration, and invasion were studied by MTT, colony formation, wound healing and transwell assays.
Results:
The NPF and siPLK1 could efficiently assemble to stable nanoparticles at a weight ratio of 3.0 and showed excellent condensation and protection effect. Owing to the FA-mediated targeted delivery, the uptake and silencing efficiency of NPF/siPLK1 to SGC-7901 cells was higher than that without FA modification. Moreover, NPF-mediated PLK1 silencing showed significant antitumor activity in vitro. The anti-proliferation effect of PLK1 silencing was induced via the mitochondrial-dependent apoptosis pathway with the cell cycle arrest of 45% at G2 phase and the apoptotic ratio of 28.3%.
Conclusion:
FA-N-Ac-L-Leu-PEI (NPF) could generate targeted delivery siPLK1 to FA receptor overexpressed cells and dramatically downregulate the expression of PLK1 expression.
Insights
Folate-modified nanoparticles deliver polo-like kinase 1 siRNA (siPLK1) effectively to cancer cells. This targeted delivery enhances PLK1 gene silencing and demonstrates significant antitumor activity by inducing apoptosis.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Cancer Therapeutics
Background:
- siRNA-mediated silencing of polo-like kinase 1 (PLK1) shows therapeutic potential for cancers.
- Clinical application is limited by inefficient and non-specific delivery of siPLK1 to tumors.
Purpose of the Study:
- To develop a targeted delivery system for siPLK1 using folate-modified nanoparticles.
- To evaluate the efficacy of targeted PLK1 silencing in cancer cells.
Main Methods:
- Synthesis of folate (FA)-modified and leucine-bearing polyethylenimine (NPF).
- Assembly of NPF with siPLK1 into stable nanoparticles.
- Assessment of cellular uptake, PLK1 gene/protein silencing, and anti-cancer effects in vitro.
Main Results:
- NPF efficiently condensed and protected siPLK1, forming stable nanoparticles.
- FA-mediated targeting significantly increased NPF/siPLK1 uptake and silencing in folate receptor-overexpressing cells.
- PLK1 silencing induced significant antitumor activity, G2 cell cycle arrest, and apoptosis via the mitochondrial pathway.
Conclusions:
- FA-N-Ac-L-Leu-PEI (NPF) nanoparticles enable targeted delivery of siPLK1.
- This approach effectively downregulates PLK1 expression and exhibits potent in vitro anti-cancer effects.
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