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Evaluation of radiogallium-labeled, folate-embedded superparamagnetic nanoparticles in fibrosarcoma-bearing mice
Seyyedeh Leila Hosseini-Salekdeh1, Amir Reza Jalilian, Hassan Yousefnia
1Department of Engineering and Technical, Science and Research Branch, Islamic Azad University, Tehran, 14778-93855, Iran.
Context:
Elevated expression of the folate receptor (FR) occurs in many human malignancies. Thus, folate targeting is widely utilized in drug delivery purposes specially using nano-radioactive agents.
Aims:
In this work, we report production and biological evaluation of gallium-67 labeled superparamagnetic iron oxide nanoparticles, embedded by folic acid ( 67 Ga-SPION-folate) complex especially in tumor-bearing mice for tumor imaging studies.
Settings And Design:
The structure of SPION-folate was confirmed by X-ray diffraction (XRD), transmission electron microscopy (TEM) and foureir transform infrared spectroscopy (FT-IR) analyses. The radiolabeled SPION-folate formation was confirmed by instant thin layer chromatography (ITLC). Tumor induction was performed by the use of poly-aromatic hydrocarbon injection in rodents as reported previously.
Materials And Methods:
[ 67 Ga]-SPION-folate was shown to possess a particle size of ≈ 5-10 nm using instrumental methods followed by ITLC test. Biocompatibility of the compound was investigated using an 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay followed by stability tests and tumor accumulation studies in fibrosarcoma-bearing mice after subcutaneous (s.c.) application.
Statistical Analysis Used:
All values were expressed as mean ± standard deviation (mean ± SD) and the data were compared using Student t-test. Statistical significance was defined as P<0.05.
Results:
[ 67 Ga]-SPION-folate was prepared by a modified co-precipitation method possessing a particle size of ≈ 5-10 nm using instrumental methods (>95% radiochemical purity). Biodistribution studies demonstrated tumor:blood, tumor:bone and tumor:muscle ratios of 4.23, 4.98 and 11.54 respectively after 24 h.
Conclusions:
Due to the nano-scale size and high-penetrative property of the developed folate-containing nano-complex, this system can be an interesting drug delivery modality with therapeutic applications and folate receptor-targeting behavior, while possessing paramagnetic properties for thermotherapy.
Insights
This study developed gallium-67 labeled superparamagnetic iron oxide nanoparticles (67Ga-SPION-folate) for targeted cancer imaging. The nanoparticles showed promising tumor accumulation in mice, indicating potential for advanced diagnostics and therapeutics.
Area of Science:
- Nanotechnology
- Radiopharmaceuticals
- Oncology
Background:
- Folate receptors (FR) are overexpressed in many human cancers.
- Folate targeting is a key strategy for cancer drug delivery, particularly with nano-radioactive agents.
Purpose of the Study:
- To produce and biologically evaluate gallium-67 labeled superparamagnetic iron oxide nanoparticles embedded with folic acid (67Ga-SPION-folate).
- To assess the potential of 67Ga-SPION-folate for tumor imaging in tumor-bearing mice.
Main Methods:
- SPION-folate structure confirmed by XRD, TEM, and FT-IR.
- Radiolabeling efficiency assessed by ITLC.
- Particle size determined to be approximately 5-10 nm.
- Biocompatibility evaluated using MTT assay.
- In vivo studies conducted in fibrosarcoma-bearing mice.
Main Results:
- The 67Ga-SPION-folate nanoparticles were successfully prepared with >95% radiochemical purity.
- Particle size was confirmed to be in the 5-10 nm range.
- Biodistribution studies showed significant tumor accumulation with high tumor-to-background ratios (e.g., tumor:muscle ratio of 11.54 at 24 h).
Conclusions:
- The developed 67Ga-SPION-folate nano-complex exhibits nano-scale size and high tumor-targeting capabilities.
- This system holds potential as a drug delivery modality for cancer therapy.
- The paramagnetic properties also suggest applications in thermotherapy.
