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Fluorinated PEG-PEI Coated Magnetic Nanoparticles for siRNA Delivery and CXCR4 Knockdown
Yixiang Cao1, Shiyin Zhang2, Ming Ma1
1State Key Laboratory of Bioelectronics, Jiangsu Key Laboratory for Biomaterials and Devices, School of Biological Sciences and Medical Engineering, Southeast University, Nanjing 210096, China.
Abstract:
CXC chemokine receptor 4 (CXCR4) is a promising therapeutic target. Previous studies have shown that intracellular delivery of siRNA to knockdown CXCR4 expression in cancer cells is an effective therapeutic strategy. To prepare efficient magnetic nucleic acid carriers, it is now necessary to improve the endocytosis efficiency of PEGylated magnetic nanoparticles. In our work, Heptafluorobutyryl-polyethylene glycol-polyethyleneimine (FPP) was first prepared and then used to coat magnetic nanoparticles (MNPs) to obtain magnetic nanocarriers FPP@MNPs. The materials were characterized by 19 F-Nuclear Magnetic Resonance (NMR), transmission electron microscope (TEM), energy dispersive spectroscopy (EDS), and dynamic light scattering (DLS). The biosecurity of FPP@MNPs was confirmed by cell viability and apoptosis experiments. Cellular uptake of FPP@MNPs and siRNA transfection enhanced by external magnetic fields were detected by fluorescence microscopy, confocal laser microscopy, and flow cytometry. The results show that the cellular uptake efficiency of FPP@MNPs was significantly improved, and transfection efficiency reached more than 90%. The knockdown of CXCR4 on the 4 T1 cell membrane was confirmed by real-time polymerase chain reaction (RT-PCR) and flow cytometry. In conclusion, the fluorinated cationic polymer-coated magnetic nanoparticles FPP@MNPs can be loaded with siRNA to reduce CXCR4 expression as well as be expected to be efficient universal siRNA carriers.
Insights
This study developed novel fluorinated polymer-coated magnetic nanoparticles (FPP@MNPs) for enhanced cellular uptake. These nanocarriers efficiently deliver siRNA to reduce CXCR4 expression in cancer cells, showing promise for targeted cancer therapy.
Area of Science:
- Biomaterials Science
- Nanotechnology
- Molecular Biology
Background:
- CXC chemokine receptor 4 (CXCR4) is a key therapeutic target in cancer.
- Intracellular siRNA delivery to silence CXCR4 is a promising strategy.
- Improving endocytosis of magnetic nanoparticles is crucial for efficient delivery.
Purpose of the Study:
- To develop novel magnetic nanocarriers (FPP@MNPs) with enhanced cellular uptake.
- To evaluate the efficiency of FPP@MNPs for siRNA delivery and CXCR4 knockdown.
- To assess the potential of FPP@MNPs as universal siRNA carriers.
Main Methods:
- Synthesis and characterization of Heptafluorobutyryl-polyethylene glycol-polyethyleneimine (FPP) coated magnetic nanoparticles (FPP@MNPs) using NMR, TEM, EDS, and DLS.
- Assessment of FPP@MNP biosecurity via cell viability and apoptosis assays.
- Evaluation of cellular uptake and siRNA transfection efficiency using fluorescence microscopy, confocal laser microscopy, and flow cytometry.
- Confirmation of CXCR4 knockdown using RT-PCR and flow cytometry.
Main Results:
- FPP@MNPs demonstrated significantly improved cellular uptake efficiency.
- siRNA transfection efficiency reached over 90% with FPP@MNPs.
- Effective knockdown of CXCR4 on 4 T1 cell membranes was confirmed.
- FPP@MNPs exhibited good biosecurity.
Conclusions:
- Fluorinated cationic polymer-coated magnetic nanoparticles (FPP@MNPs) are effective siRNA carriers.
- FPP@MNPs enhance cellular uptake and facilitate efficient siRNA delivery for gene silencing.
- These nanocarriers show potential for targeted cancer therapy by reducing CXCR4 expression.
