Synthesis, 99mTc‐labeling, and preliminary biological evaluation of <scp>DTPA</scp>‐melphalan conjugates

Wang, Jianjun; Yang, Wenjiang; Xue, Jian; Zhang, Yanhua; Liu, Yü

doi:10.1002/jlcr.3575

Cited by 5 publications

(4 citation statements)

References 14 publications

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“…This data aligns with those reported in the literature, where high radiolabeling efficiency can be achieved at room temperature. [52][53][54][55] Hence, all radiolabeling processes were conducted at room temperature in this study. The radiolabeling process was optimized by taking four factors into account: concentrations of TPGS-DTPA and SnCl 2 ⋅H 2 O, pH of the solution during radiolabeling, and incubation time.…”

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confidence: 99%

Characterization, optimization, and in vitro evaluation of Technetium-99m-labeled niosomes

Silva

Htar

et al. 2019

IJN

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Background and purpose Niosomes are nonionic surfactant-based vesicles that exhibit certain unique features which make them favorable nanocarriers for sustained drug delivery in cancer therapy. Biodistribution studies are critical in assessing if a nanocarrier system has preferential accumulation in a tumor by enhanced permeability and retention effect. Radiolabeling of nanocarriers with radioisotopes such as Technetium-99m ( 99m Tc) will allow for the tracking of the nanocarrier noninvasively via nuclear imaging. The purpose of this study was to formulate, characterize, and optimize 99m Tc-labeled niosomes. Methods Niosomes were prepared from a mixture of sorbitan monostearate 60, cholesterol, and synthesized D-α-tocopherol polyethylene glycol 1000 succinate-diethylenetriaminepentaacetic acid (synthesis confirmed by 1 H and 13 C nuclear magnetic resonance spectroscopy). Niosomes were radiolabeled by surface chelation with reduced 99m Tc. Parameters affecting the radiolabeling efficiency such as concentration of stannous chloride (SnCl 2 ·H 2 O), pH, and incubation time were evaluated. In vitro stability of radiolabeled niosomes was studied in 0.9% saline and human serum at 37°C for up to 8 hours. Results Niosomes had an average particle size of 110.2±0.7 nm, polydispersity index of 0.229±0.008, and zeta potential of −64.8±1.2 mV. Experimental data revealed that 30 µg/mL of SnCl 2 ·H 2 O was the optimal concentration of reducing agent required for the radiolabeling process. The pH and incubation time required to obtain high radiolabeling efficiency was pH 5 and 15 minutes, respectively. 99m Tc-labeled niosomes exhibited high radiolabeling efficiency (>90%) and showed good in vitro stability for up to 8 hours. Conclusion To our knowledge, this is the first study published on the surface chelation of niosomes with 99m Tc. The formulated 99m Tc-labeled niosomes possessed high radiolabeling efficacy, good stability in vitro, and show good promise for potential use in nuclear imaging in the future.

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confidence: 99%

Characterization, optimization, and in vitro evaluation of Technetium-99m-labeled niosomes

Silva

Htar

et al. 2019

IJN

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“…The stability of [ 99m Tc]Tc-labeled niosomes was assessed in SF at 25 °C, serum (FBS:PBS (pH 7.4); 50:50%, v/v) at 37 °C, and cell medium at 37 °C (Figure ). These conditions were chosen to shed light on the application of [ 99m Tc]Tc-niosome formulations in an in vivo internal environment at pH 7.4 (physiological pH) and in vitro storage . As [ 99m Tc]NaTcO 4 is eluted from [ 99 Mo]Mo/[ 99m Tc]Tc generator using SF, it is crucial for [ 99m Tc]Tc-niosomes to remain stable in SF.…”

Section: Resultsmentioning

confidence: 99%

“…These conditions were chosen to shed light on the application of [ 99m Tc]Tc-niosome formulations in an in vivo internal environment at pH 7.4 (physiological pH) and in vitro storage. 42 As [ 99m Tc]NaTcO 4 is eluted from [ 99 Mo]Mo/[ 99m Tc]Tc generator using SF, it is crucial for [ 99m Tc]Tc-niosomes to remain stable in SF. The [ 99m Tc]Tc-niosome formulations were found to be extremely stable in SF, with a high labeling efficiency (>90%) and only a 4.63% decrease in RP after 6 h ( Figure 5 ).…”

Section: Resultsmentioning

confidence: 99%

[^99mTc]Technetium-Labeled Niosomes: Radiolabeling, Quality Control, and In Vitro Evaluation

et al. 2023

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The aim of this research was to develop technetium-99m ([99mTc]Tc)-radiolabeled niosomes and evaluate the cancer cell incorporation capacity of radiolabeled niosomes. For this purpose, niosome formulations were developed by film hydration method, and prepared niosomes were characterized to particle size, polydispersity index (PdI), ζ-potential value, and image profile. Then, niosomes were radiolabeled with [99mTc]Tc using stannous salts (chloride) as a reducing agent. The radiochemical purity (RP) and stability in different mediums of the niosomes were assessed by ascending radioactive thin-layer chromatography (RTLC) and radioactive ultrahigh-performance liquid chromatography (R-UPLC) methods. Also, the partition coefficient value of radiolabeled niosomes was determined. The cell incorporation of [99mTc]Tc-labeled niosome formulations, as well as reduced/hydrolyzed (R/H)-[99mTc]NaTcO4 in the HT-29 (human colorectal adenocarcinoma) cells, was then assessed. According to the obtained results, the spherical niosomes had a particle size of 130.5 ± 1.364 nm, a PdI value of 0.250 ± 0.023, and a negative charge of −35.4 ± 1.06 mV. The niosome formulations were effectively radiolabeled with [99mTc]Tc using 500 μg mL–1 stannous chloride for 15 min, and RP was found to be over 95%. [99mTc]Tc-niosomes showed good in vitro stability in every system for up to 6 h. The log P value of radiolabeled niosomes was found as −0.66 ± 0.02. Compared to R/H-[99mTc]NaTcO4 (34.18 ± 1.56%), the incorporation percentages of [99mTc]Tc-niosomes (88.45 ± 2.54%) were shown to be higher in cancer cells. In conclusion, the newly developed [99mTc]Tc-niosomes showed good prototype for potential use in nuclear medicine imaging in the near future. However, further investigations, such as drug encapsulation and biodistribution studies, should be performed, and our studies are continuing.

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“…The stability of [ 99m Tc]Tc-labeled nanoparticles was evaluated in saline, serum, and cell media ( Figure 3 ). These parameters were selected to provide information about using [ 99m Tc]Tc-nanoparticles in an internal environment and in vitro storage [ 64 ]. As [ 99m Tc]NaTcO 4 was eluted from the [ 99 Mo]Mo/[ 99m Tc]Tc-generator using saline, [99mTc]Tc-nanoparticles must remain stable in saline.…”

Section: Resultsmentioning

confidence: 99%

Radiolabeled Human Serum Albumin Nanoparticles Co-Loaded with Methotrexate and Decorated with Trastuzumab for Breast Cancer Diagnosis

Ekinci,

Alencar,

Lopes

et al. 2023

JFB

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Breast cancer is a leading cause of cancer-related mortality among women worldwide, with millions of new cases diagnosed yearly. Addressing the burden of breast cancer mortality requires a comprehensive approach involving early detection, accurate diagnosis, effective treatment, and equitable access to healthcare services. In this direction, nano-radiopharmaceuticals have shown potential for enhancing breast cancer diagnosis by combining the benefits of nanoparticles and radiopharmaceutical agents. These nanoscale formulations can provide improved imaging capabilities, increased targeting specificity, and enhanced sensitivity for detecting breast cancer lesions. In this study, we developed and evaluated a novel nano-radio radiopharmaceutical, technetium-99m ([99mTc]Tc)-labeled trastuzumab (TRZ)-decorated methotrexate (MTX)-loaded human serum albumin (HSA) nanoparticles ([99mTc]-TRZ-MTX-HSA), for the diagnosis of breast cancer. In this context, HSA and MTX-HSA nanoparticles were prepared. Conjugation of MTX-HSA nanoparticles with TRZ was performed using adsorption and covalent bonding methods. The prepared formulations were evaluated for particle size, PDI value, zeta (ζ) potential, scanning electron microscopy analysis, encapsulation efficiency, and loading capacity and cytotoxicity on MCF-7, 4T1, and MCF-10A cells. Finally, the nanoparticles were radiolabeled with [99mTc]Tc using the direct radiolabeling method, and cellular uptake was performed with the nano-radiopharmaceutical. The results showed the formation of spherical nanoparticles, with a particle size of 224.1 ± 2.46 nm, a PDI value of 0.09 ± 0.07, and a ζ potential value of −16.4 ± 0.53 mV. The encapsulation efficiency of MTX was found to be 32.46 ± 1.12%, and the amount of TRZ was 80.26 ± 1.96%. The labeling with [99mTc]Tc showed a high labeling efficiency (>99%). The cytotoxicity studies showed no effect, and the cellular uptake studies showed 97.54 ± 2.16% uptake in MCF-7 cells at the 120th min and were found to have a 3-fold higher uptake in cancer cells than in healthy cells. In conclusion, [99mTc]Tc-TRZ-MTX-HSA nanoparticles are promising for diagnosing breast cancer and evaluating the response to treatment in breast cancer patients.

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Synthesis, ^99mTc‐labeling, and preliminary biological evaluation of DTPA‐melphalan conjugates

Cited by 5 publications

References 14 publications

<p>Characterization, optimization, and in vitro evaluation of Technetium-99m-labeled niosomes</p>

<p>Characterization, optimization, and in vitro evaluation of Technetium-99m-labeled niosomes</p>

[^99mTc]Technetium-Labeled Niosomes: Radiolabeling, Quality Control, and In Vitro Evaluation

Radiolabeled Human Serum Albumin Nanoparticles Co-Loaded with Methotrexate and Decorated with Trastuzumab for Breast Cancer Diagnosis

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Synthesis, 99mTc‐labeling, and preliminary biological evaluation of DTPA‐melphalan conjugates

Cited by 5 publications

References 14 publications

<p>Characterization, optimization, and in vitro evaluation of Technetium-99m-labeled niosomes</p>

<p>Characterization, optimization, and in vitro evaluation of Technetium-99m-labeled niosomes</p>

[99mTc]Technetium-Labeled Niosomes: Radiolabeling, Quality Control, and In Vitro Evaluation

Radiolabeled Human Serum Albumin Nanoparticles Co-Loaded with Methotrexate and Decorated with Trastuzumab for Breast Cancer Diagnosis

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Product

Resources

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Synthesis, ^99mTc‐labeling, and preliminary biological evaluation of DTPA‐melphalan conjugates

[^99mTc]Technetium-Labeled Niosomes: Radiolabeling, Quality Control, and In Vitro Evaluation