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Updated: Mar 7, 2026
Biofunctionalization of Magnetic Nanomaterials
Published on: July 16, 2020
Polyvalent Folate-Dendrimer-Coated Iron Oxide Theranostic Nanoparticles for Simultaneous Magnetic Resonance Imaging
Duy Luong1, Samaresh Sau1, Prashant Kesharwani1
1Use-inspired Biomaterials & Integrated Nano Delivery (U-BiND) Systems Laboratory Department of Pharmaceutical Sciences, Eugene Applebaum College of Pharmacy and Health Sciences, Wayne State University , 259 Mack Avenue, Detroit, Michigan 48201, United States.
Abstract:
The low therapeutic index of conventional chemotherapy and poor prognosis of patients diagnosed with metastatic cancers are prompting clinicians to adopt newer strategies to simultaneously detect cancer lesions at an early stage and to precisely deliver anticancer drugs to tumor sites. In this study, we employed a novel strategy to engineer a polyvalent theranostic nanocarrier consisting of superparamagnetic iron oxide nanoparticle core (SPIONs) decorated with folic acid-polyamidoamine dendrimers surface (FA-PAMAM). In addition, a highly potent hydrophobic anticancer agent 3,4-difluorobenzylidene-curcumin (CDF) was coloaded in the FA-PAMAM dendrimer to increase its solubility and assess its therapeutic potentials. The resulting targeted nanoparticles (SPIONs@FA-PAMAM-CDF) exhibited high MR contrast. When tested on folate receptor overexpressing ovarian (SKOV3) and cervical (HeLa) cancer cells, the CDF loaded targeted nanoformulations showed higher accumulation with a better anticancer activity as compared to the nontargeted counterparts, possibly due to multivalent folate receptor binding interaction with cells overexpressing the target. The results were corroborated by observation of a larger population of cells undergoing apoptosis due to upregulation of tumor suppressor phosphatase and tensis homologue (PTEN), caspase 3, and inhibition of NF-κB in groups treated with the targeted formulations, which further confirmed the ability of the multivalent theranostic nanoparticles for simultaneous imaging and therapy of cancers.
Insights
This study introduces novel theranostic nanoparticles for early cancer detection and targeted drug delivery. These nanoparticles show enhanced anticancer activity and apoptosis induction in cancer cells.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Oncology
Background:
- Conventional chemotherapy has a low therapeutic index and poor prognosis for metastatic cancers.
- There is a need for strategies that enable early cancer detection and precise drug delivery to tumor sites.
Purpose of the Study:
- To engineer a novel polyvalent theranostic nanocarrier for simultaneous cancer imaging and therapy.
- To evaluate the efficacy of a hydrophobic anticancer agent loaded within the nanocarrier.
Main Methods:
- Fabrication of superparamagnetic iron oxide nanoparticle core (SPIONs) decorated with folic acid-polyamidoamine dendrimers (FA-PAMAM).
- Coloading of 3,4-difluorobenzylidene-curcumin (CDF) into the FA-PAMAM dendrimer.
- Testing of targeted nanoparticles (SPIONs@FA-PAMAM-CDF) on folate receptor-overexpressing ovarian (SKOV3) and cervical (HeLa) cancer cells.
- Assessment of MR contrast, cellular accumulation, anticancer activity, and apoptosis induction.
Main Results:
- The SPIONs@FA-PAMAM-CDF nanoparticles exhibited high MR contrast.
- Targeted nanoformulations showed higher accumulation and enhanced anticancer activity in cancer cells compared to non-targeted ones.
- Increased apoptosis was observed, linked to PTEN upregulation, caspase 3 activation, and NF-κB inhibition.
Conclusions:
- Multivalent theranostic nanoparticles demonstrate potential for simultaneous cancer imaging and therapy.
- The developed nanocarrier effectively delivers anticancer agents and enhances therapeutic outcomes.
- Targeted delivery via folate receptor interaction is a promising strategy for overcoming limitations of conventional cancer treatments.
