Investigation of Specific Targeting of Triptorelin-Conjugated Dextran-Coated Magnetite Nanoparticles as a Targeted Probe in GnRH+ Cancer Cells in MRI

Abstract

In recent years, the conjugation of superparamagnetic iron oxide nanoparticles (SPIONs), as tumor-imaging probes for magnetic resonance imaging (MRI), with tumor targeting peptides possesses promising advantages for specific delivery of MRI agents. The objective of the current study was to design a targeted contrast agent for MRI based on Fe3O4 nanoparticles conjugated triptorelin (SPION@triptorelin), which has a great affinity to the GnRH receptors. The SPIONs-coated carboxymethyl dextran (SPION@CMD) conjugated triptorelin (SPION@CMD@triptorelin) were synthesized using coprecipitation method and characterized by DLS, TEM, XRD, FTIR, Zeta, and VSM techniques. The relaxivities of synthetized formulations were then calculated using a 1.5 Tesla clinical magnetic field. MRI, quantitative cellular uptake, and cytotoxicity level of them were estimated. The characterization results confirmed that the formation of SPION@CMD@triptorelin has been conjugated with a suitable size. Our results demonstrated the lack of cellular cytotoxicity of SPION@CMD@triptorelin, and it could increase the cellular uptake of SPIONs to MDA-MB-231 cancer cells 6.50-fold greater than to SPION@CMD at the concentration of 75 μM. The relaxivity calculations for SPION@CMD@triptorelin showed a suitable r2 and r2/r1 with values of 31.75 mM−1·s−1 and 10.26, respectively. Our findings confirm that triptorelin-targeted SPIONs could provide a T2-weighted probe contrast agent that has the great potential for the diagnosis of GnRH-positive cancer in MRI.

Molecular MR Imaging of Prostate Cancer by Specified Iron Oxide Nanoparticles With PSMA‐11 Peptides: A Preclinical Study

“…MRI offers excellent contrast resolution and also has the possibility of using contrast agents to assist in the diagnosis of various types of diseases 2 . In this regard, targeted nanoparticles as contrast agents are very beneficial 3,4 . Nanoparticles that have been modified with cancer ligands, such as peptides, provide a specific and sensitive imaging probe 3–5 …”

“…In this regard, targeted nanoparticles as contrast agents are very beneficial 3,4 . Nanoparticles that have been modified with cancer ligands, such as peptides, provide a specific and sensitive imaging probe 3–5 …”

“…Super‐paramagnetic iron oxide nanoparticles (IONPs), are known as negative contrast agents in MRI, and have been used in a targeted manner to assist in the diagnosis and treatment of various tumors 3,5–8 . Signal intensity (SI) decreases with the selective accumulation of these nanoparticles at the target area 2,9–11 .…”

“…used in a targeted manner to assist in the diagnosis and treatment of various tumors. 3,[5][6][7][8] Signal intensity (SI) decreases with the selective accumulation of these nanoparticles at the target area. 2,[9][10][11] The magnetic cores are usually coated with biological materials because the naked nanoparticles are highly chemically reactive, and can be easily oxidized, which decreases their stability and magnetic properties.…”

Gold-iron oxide (Au/Fe3O4) magnetic nanoparticles as the nanoplatform for binding of bioactive molecules through self-assembly

“…For inorganic nanoparticles, silanization using functional silanes such as 3-aminopropyltriethoxysilane (APTES) is commonly used to functionalize Fe 3 O 4 and SiO 2 nanoparticles with amine (-NH 2 ) groups ( Yiu et al, 2013 ; Kumar and Paik, 2021 ). Another method is to graft organic groups onto the protective coating (e.g., dextran) ( Yousefvand et al, 2021 ; Xiong et al, 2022 ). However, these strategies may lead to several issues in both the synthesis and the final product characteristics/properties themselves.…”