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Updated: Jan 4, 2026
Preparation of Neutrally-charged, pH-responsive Polymeric Nanoparticles for Cytosolic siRNA Delivery
Published on: May 2, 2019
The Codelivery of siRNA and QDs by pH-Responsive Micelle for Hepatoma Cancer Cells
Zhonglin Cao1,2, Huiyu Xiao1, Li Li3
1Key Laboratory of Optoelectronics Devices and Systems of Ministry of Education and Guangdong Province, College of Optoelectronic Engineering, Shenzhen University, Shenzhen, China.
Abstract:
Recently, RNA interfering (RNAi) has become a promising approach for cancer therapy. However, the application of RNAi for clinics is still hindered due to the lack of safe and efficient carriers. In this study, a pH-responsive micelle based on polycaprolactone-block-poly 2-(dimethylamino)ethyl methacrylate (PCL-PDEM) cationic copolymer was developed to carry short interfering RNA (siRNA) for silencing interleukin 8 (IL-8) gene in hepatoma cancer cells. The transfection efficiency of the PCL-PDEM-siRNA/quantum dots (QDs) nanoplex has reached about 70%, and the expression level of IL-8 decreased about 63%. Furthermore, the codelivery of QDs and siRNA has been realized, which is beneficial to visualize the process of siRNA delivery. No considerable cytotoxicity from the nanoparticles has been observed, indicating that our responsive cationic micelle is potential in clinical trial for hepatoma cancer therapy.
Insights
This study developed a pH-responsive micelle for delivering short interfering RNA (siRNA) to target cancer genes. The novel carrier efficiently silenced the interleukin 8 (IL-8) gene in hepatoma cells with minimal toxicity, showing promise for cancer therapy.
Area of Science:
- Biotechnology
- Nanomedicine
- Cancer Therapy
Background:
- RNA interfering (RNAi) shows potential for cancer treatment but requires effective delivery systems.
- Current RNAi delivery methods face challenges in safety and efficiency for clinical application.
Purpose of the Study:
- To develop a pH-responsive cationic micelle for efficient siRNA delivery in hepatoma cancer therapy.
- To investigate the silencing of the interleukin 8 (IL-8) gene using the developed nanocarrier.
Main Methods:
- A pH-responsive micelle was synthesized using polycaprolactone-block-poly 2-(dimethylamino)ethyl methacrylate (PCL-PDEM) cationic copolymer.
- Short interfering RNA (siRNA) targeting the IL-8 gene was encapsulated within the micelle.
- Quantum dots (QDs) were co-delivered with siRNA for visualization of the delivery process.
Main Results:
- The PCL-PDEM-siRNA/QDs nanoplex achieved approximately 70% transfection efficiency.
- IL-8 gene expression was reduced by about 63% in hepatoma cells.
- The nanoparticles demonstrated no considerable cytotoxicity, indicating good safety.
Conclusions:
- The developed pH-responsive cationic micelle is a safe and efficient carrier for siRNA delivery in hepatoma cancer therapy.
- Codelivery of siRNA and QDs allows for visualization of the delivery process, aiding therapeutic monitoring.
- This nanocarrier shows significant potential for clinical trials in hepatoma treatment.
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