Related Experiment Video
Updated: Jun 3, 2026

Synthesis of Aptamer-PEI-g-PEG Modified Gold Nanoparticles Loaded with Doxorubicin for Targeted Drug Delivery
Published on: June 23, 2020
Cyclic RGD functionalized gold nanoparticles for tumor targeting
Daniela Arosio1, Leonardo Manzoni, Elena M V Araldi
1CNR-Istituto di Scienze e Tecnologie Molecolari ( ISTM ), Via Fantoli 16/15, I-20138, Milan, Italy. daniela.arosio@istm.cnr.it
Abstract:
Integrin α(v)β(3) is an adhesion molecule involved in physiological and pathological angiogenesis as well as tumor invasion and metastasis. Therefore, it is considered an important target for molecular imaging and delivery of therapeutics for cancer, and there is a strong interest in developing novel agents interacting with this protein. Nevertheless, the interaction of individual ligands is often still weak for efficient tumor targeting, and many research groups have synthesized multivalent displays in order to overcome this problem. Gold nanoparticles can be considered a smart platform for polyvalent presentation on account of their globular shape, tunable size, facile surface chemistry, and biocompatibility. Moreover, their unique physical properties render gold nanoparticles ideal candidates for tumor diagnosis and therapy. Here, we report the synthesis and characterization of gold nanoparticles functionalized with cRGD integrin ligand and their employment for targeting human cancer cells expressing α(v)β(3) integrin.
Insights
Researchers developed gold nanoparticles functionalized with cRGD ligands to target cancer cells. This approach enhances targeting of integrin α(v)β(3), crucial for tumor growth and spread.
Area of Science:
- Nanomedicine
- Bioconjugation
- Oncology
Background:
- Integrin α(v)β(3) is a key adhesion molecule in angiogenesis, tumor invasion, and metastasis.
- Targeting integrin α(v)β(3) is crucial for cancer molecular imaging and therapeutics.
- Weak ligand interactions limit efficient tumor targeting, necessitating multivalent strategies.
Purpose of the Study:
- To synthesize and characterize gold nanoparticles functionalized with cRGD ligands.
- To evaluate the efficacy of these functionalized nanoparticles in targeting human cancer cells expressing integrin α(v)β(3).
Main Methods:
- Synthesis of gold nanoparticles.
- Surface functionalization with cRGD ligands.
- Characterization of the nanoparticles.
- In vitro targeting assays with human cancer cells expressing α(v)β(3) integrin.
Main Results:
- Successfully synthesized and characterized gold nanoparticles functionalized with cRGD.
- Demonstrated targeted binding of the functionalized nanoparticles to human cancer cells expressing α(v)β(3) integrin.
- The multivalent presentation on gold nanoparticles potentially enhances targeting efficiency.
Conclusions:
- Gold nanoparticles serve as effective platforms for polyvalent ligand display.
- cRGD-functionalized gold nanoparticles show promise for targeting integrin α(v)β(3) on cancer cells.
- This strategy holds potential for advancing cancer diagnostics and therapeutics.

