Related Experiment Video
Updated: Jan 6, 2026
Author Spotlight: Innovative Cancer Therapies with Iron Oxide Nanoparticles for Glioblastoma Treatment
Published on: September 27, 2024
Surface decoration of solid lipid nanoparticles with cyclic RGD peptides for precision therapy in high-risk
Sara Lorenzoni1,2,3, Carlos Aydillo1,2, Carlos Rodríguez-Nogales4
1Department of Pharmaceutical Sciences, School of Pharmacy and Nutrition, Universidad de Navarra, Pamplona, Spain.
Abstract:
High-risk neuroblastoma poses significant therapeutic challenges due to tumor heterogeneity, drug resistance, and systemic toxicity associated with conventional chemotherapies. To overcome these limitations, we developed cyclic RGD-decorated solid lipid nanoparticles for integrin-targeted delivery of etoposide, aiming to enhance tumor selectivity and therapeutic efficacy. SLNs were prepared using hot homogenization and ultrasonication, with cyclic RGD peptides conjugated to the surface via non-covalent and covalent strategies. Among three conjugation approaches evaluated, maleimide-based functionalization was selected for its reproducibility, stability, and high coupling efficiency. RGD-functionalized SLNs were physicochemically characterized and assessed for integrin-mediated uptake, cytotoxicity, cell cycle effects, and apoptosis induction in SH-SY5Y (integrin-high) and SK-N-BE(2) (integrin-low) NB cell lines. RGD-SLNs demonstrated efficient peptide conjugation while maintaining colloidal stability and drug loading. Flow cytometry confirmed enhanced uptake in αvβ3 integrin-expressing SH-SY5Y cells, with moderate uptake in SK-N-BE(2) cells. ETP encapsulation within SLNs significantly improved its cytotoxic profile, with RGD functionalization further reducing IC50 values and promoting apoptosis. These findings establish RGD-functionalized SLNs as a promising integrin-targeted platform for ETP delivery in NB. To our knowledge, this is the first report of this approach using SLNs for NB, offering a novel strategy for translational nanomedicine.
Insights
Targeted delivery of etoposide using RGD-decorated solid lipid nanoparticles (SLNs) enhances neuroblastoma treatment. This novel approach improves drug efficacy and reduces toxicity for high-risk neuroblastoma patients.
Area of Science:
- Nanomedicine
- Oncology
- Drug Delivery
Background:
- High-risk neuroblastoma presents treatment challenges due to tumor heterogeneity and drug resistance.
- Conventional chemotherapy for neuroblastoma often leads to systemic toxicity.
- There is a need for targeted drug delivery systems to improve therapeutic outcomes.
Purpose of the Study:
- To develop cyclic RGD-decorated solid lipid nanoparticles (SLNs) for targeted delivery of etoposide (ETP) in neuroblastoma.
- To enhance tumor selectivity and therapeutic efficacy of etoposide by targeting integrins.
- To investigate the potential of RGD-functionalized SLNs as a novel nanomedicine strategy for neuroblastoma.
Main Methods:
- Solid lipid nanoparticles (SLNs) were prepared using hot homogenization and ultrasonication.
- Cyclic RGD peptides were conjugated to SLNs via maleimide-based functionalization.
- Physicochemical characterization, integrin-mediated uptake studies, cytotoxicity assays, cell cycle analysis, and apoptosis induction were performed on neuroblastoma cell lines.
Main Results:
- RGD-functionalized SLNs exhibited efficient peptide conjugation, colloidal stability, and drug loading.
- Enhanced cellular uptake of RGD-SLNs was observed in integrin-high SH-SY5Y cells compared to integrin-low SK-N-BE(2) cells.
- Etoposide-loaded RGD-SLNs demonstrated improved cytotoxicity, reduced IC50 values, and induced significant apoptosis in neuroblastoma cells.
Conclusions:
- RGD-functionalized SLNs represent a promising platform for targeted etoposide delivery in neuroblastoma.
- This approach offers enhanced therapeutic efficacy and reduced toxicity compared to conventional chemotherapy.
- This study presents a novel strategy for translational nanomedicine in neuroblastoma treatment.
