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Updated: Aug 27, 2025

Preparation of Neutrally-charged, pH-responsive Polymeric Nanoparticles for Cytosolic siRNA Delivery
Published on: May 2, 2019
A bivalent aptamer and terminus-free siRNA junction nanostructure for targeted gene silencing in cancer cells
Fang Yang1, Shunmei Li1, Ruo Yuan1
1Key Laboratory of Luminescence Analysis and Molecular Sensing, Ministry of Education, School of Chemistry and Chemical Engineering, Southwest University, Chongqing 400715, P. R. China. yunatswu@swu.edu.cn.
Abstract:
Small interfering RNA (siRNA) has increasingly evolved as a potent therapeutic solution for several pathological conditions including cancers via post-transcriptional oncogene suppression in cellular pathways. And, the key for siRNA-based therapy highly relies on the successful siRNAs delivery into the target cells, which is significantly challenged by their instability, poor cellular uptake and targeting capability. To overcome these issues, herein, a new type of RNA nanostructure, the bivalent aptamer and terminus-free siRNA junction, is synthesized and employed for effective gene silencing in cancer cells. Such a siRNA junction can be readily prepared by the self-assembly of three RNA sequences and subsequent ligation of the nicks. The as-synthesized siRNA junction shows highly improved enzymatic stability and targeting capability and can be efficiently delivered into the target cells to induce cell apoptosis. With these integrated advantages, the siRNA junction can therefore offer new potentials for the design of different siRNA therapeutics for various diseases.
Insights
A novel RNA nanostructure, the bivalent aptamer and terminus-free small interfering RNA (siRNA) junction, enhances siRNA delivery and stability for effective cancer gene silencing and apoptosis induction.
Area of Science:
- Biotechnology
- Molecular Biology
- Nanomedicine
Background:
- Small interfering RNA (siRNA) offers therapeutic potential for cancers by suppressing oncogenes.
- Effective siRNA delivery is hindered by instability, poor cellular uptake, and limited targeting.
Purpose of the Study:
- To develop a novel RNA nanostructure for improved siRNA delivery and gene silencing in cancer cells.
Main Methods:
- Synthesized a bivalent aptamer and terminus-free siRNA junction through self-assembly and ligation of RNA sequences.
- Evaluated the nanostructure's enzymatic stability, cellular uptake, and targeting capability.
- Assessed the induction of apoptosis in cancer cells post-delivery.
Main Results:
- The novel siRNA junction demonstrated enhanced enzymatic stability and targeting efficacy.
- Efficient delivery into target cancer cells was achieved.
- Significant induction of cancer cell apoptosis was observed.
Conclusions:
- The bivalent aptamer-siRNA junction represents a promising platform for overcoming siRNA delivery challenges.
- This nanostructure holds potential for developing advanced siRNA therapeutics for various diseases.
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