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Published on: September 20, 2011
Bioinformatics-Driven Engineering of ROS-Responsive Dextran-block-Poly(propylene sulfide) Nanoparticles
Yixun Zhang1, Zhenguo Liang2, Zeheng Tan3
1Department of Burn and Plastic Surgery, the Second Affiliated Hospital, School of Medicine, South China University of Technology, Guangzhou, Guangdong 510180, China.
Abstract:
Prostate cancer (PCa) remains a significant challenge in oncology due to its complex pathogenesis and resistance to conventional therapies. By leveraging bioinformatics-guided insights, we identified folate hydrolase 1 (FOLH1) as a crucial biomarker with overexpression in various cancers, particularly PCa. Therefore, we prepared folate receptor-targeted reactive oxygen species (ROS)-responsive dextran-block-poly-(propylene sulfide) nanoparticles to enhance targeted therapeutic efficacy against PCa. The block copolymer was achieved using Cu-(I)-catalyzed "click" chemistry, followed by the successful conjugation of folic acid (FA). Characterization confirmed the nanoparticles' ability to encapsulate doxorubicin (Dox) and respond to ROS, releasing the drug under oxidative conditions. In vitro studies demonstrated enhanced cellular uptake, increased ROS production, and superior cytotoxicity of FA-Dex-b-PPS-Dox in PC3 cells compared to free Dox and nontargeted Dex-b-PPS-Dox nanoparticles. Furthermore, FA-Dex-b-PPS-Dox significantly inhibited tumor cell migration and invasion, emphasizing its potential for comprehensive cancer therapy. In vivo efficacy was assessed using a PC3 tumor model, where FA-Dex-b-PPS-Dox notably reduced tumor volume and weight, with histological analyses confirming enhanced apoptosis and reduced cell proliferation. These findings underscore the promising potential of FA-Dex-b-PPS-Dox in providing a targeted, ROS-responsive therapeutic strategy for prostate cancer.
Insights
Novel nanoparticles targeting folate receptors show promise for prostate cancer treatment. These drug-carrying nanoparticles release medication in response to reactive oxygen species, enhancing cancer cell death and reducing tumor growth.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Oncology
Background:
- Prostate cancer (PCa) presents significant therapeutic challenges due to complex mechanisms and treatment resistance.
- Folate hydrolase 1 (FOLH1) is identified as a key biomarker overexpressed in PCa, indicating its potential as a therapeutic target.
Purpose of the Study:
- To develop novel folate receptor-targeted, reactive oxygen species (ROS)-responsive nanoparticles for enhanced prostate cancer therapy.
- To evaluate the efficacy of these nanoparticles in delivering doxorubicin (Dox) to PCa cells and inhibiting tumor progression.
Main Methods:
- Synthesis of dextran-block-poly-(propylene sulfide) (Dex-b-PPS) nanoparticles via "click" chemistry.
- Conjugation of folic acid (FA) for targeted delivery and characterization of Dox encapsulation and ROS-responsive release.
- In vitro assessment of cellular uptake, ROS generation, cytotoxicity, migration, and invasion in PC3 cells.
- In vivo evaluation of therapeutic efficacy in a PC3 xenograft mouse model.
Main Results:
- FA-targeted nanoparticles successfully encapsulated doxorubicin and demonstrated ROS-triggered drug release.
- Enhanced cellular uptake, increased ROS production, and superior cytotoxicity of FA-Dex-b-PPS-Dox in PC3 cells compared to controls.
- Significant inhibition of tumor cell migration and invasion observed with FA-Dex-b-PPS-Dox treatment.
- In vivo studies showed notable reduction in tumor volume and weight, with increased apoptosis and decreased proliferation.
Conclusions:
- FA-Dex-b-PPS-Dox nanoparticles represent a promising targeted and responsive drug delivery system for prostate cancer.
- This approach offers a potential strategy to overcome therapeutic resistance and improve treatment outcomes for PCa.
