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.
Highlights
Cancers are one of the most frequent mortality causes worldwide due to the challenges arising in the diagnosis and clinical management of the cancerous patients [1, 2]
Regarding the dynamic light scattering (DLS) results, only one peak was observed in both superparamagnetic iron oxide nanoparticles (SPIONs)@carboxymethylated dextran (CMD) and SPION@CMD@triptorelin (Figures 2(a) and 2(b)). e highest number of SPION@ CMD and SPION@CMD@triptorelin complexes had a diameter of 160 nm and 116 nm, respectively. is phenomenon indicates narrow particle size distribution and monomodal population of the particles due in part to the contribution of triptorelin with SPIONs
R2/r1 ratio of the targeted SPIONs was calculated as 10.26; this finding demonstrated the potential use of the synthesized SPION@CMD@triptorelin as appropriate targeted negative contrast agents at conventional magnetic resonance imaging (MRI) system at low applied concentration
Summary
Cancers are one of the most frequent mortality causes worldwide due to the challenges arising in the diagnosis and clinical management of the cancerous patients [1, 2]. Targeted nanomolecular imaging has been proposed as a suitable solution for early detection and improvement of contrast-to-noise ratio. Erefore, the developments of novel efficient approaches for early diagnosis of cancer are of paramount importance for decreasing of cancer mortality [3]. The detection of cancer based on specific biomarkers or receptors has resulted in substantial improvements in early and specific diagnosis of human cancers, as well as monitoring the outcome of the disease during and after the course of the treatment [4,5,6]. Several methods (including physical, laboratory, biopsy, and imaging tests) are used for the diagnosis of various human cancers. E most common imaging methods that are used in diagnosing cancer may include a computerized tomography (CT) scan, bone scan, ultrasound, X-ray, positron emission tomography (PET) Imaging tests as a noninvasive way allow examining bones and internal organs. e most common imaging methods that are used in diagnosing cancer may include a computerized tomography (CT) scan, bone scan, ultrasound, X-ray, positron emission tomography (PET)
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