Preparation and biodistribution of [<sup>125</sup>I]Melphalan: a potential radioligand for diagnostic and therapeutic applications

Amin, A. M.; Soliman, S. E.; El-Aziz, H. A.

doi:10.1002/jlcr.1698

Cited by 16 publications

(3 citation statements)

References 14 publications

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“…Finally, all of the reactions were terminated by the addition of 50 μL of aqueous solution of sodium metabisulfite (20 mg/mL) to ensure that all the unreacted iodine is in a reduced form (I − ) before chromatographic analysis …”

Section: Methodsmentioning

confidence: 99%

Facile radiolabeling optimization process via design of experiments and an intelligent optimization algorithm: Application for omeprazole radioiodination

Farrag

Abdel-Halim

Moamen

2019

Labelled Comp Radiopharmac

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The major uses of radiopharmaceuticals (RP) in clinical areas are diagnosis and/or therapy. The present study aimed to utilize the application of fractional factorial design analysis (FFDA) coupled with particle swarm optimization algorithm (PSO) to assess the optimization of RP production process. In this regard, omeprazole (OMP), which is gastric parietal cell proton pump inhibitor (PPI), was radiolabeled with iodine‐125 (125I) isotope in order to be used as a radiotracer for stomach imaging. Different factors that affect radiolabeling process were studied. According to the proposed design, just 16 experimental runs of radiolabeling process were performed using the extremes of each factor. In addition, one run was executed at the mean point of each factor. Undesirable maximum radiolabeling yield (RY) of radioiodinated omeprazole (125I‐OMP) was deduced from application of FFDA (88.4%). Furthermore, after applying PSO with changing limits of one factor, the maximum RY of 125I‐OMP was found to be 93.78%. Moreover, the practically verification from optimum conditions, which obtained from PSO, was found to give an RY of 93.99%. Overall, the findings of this study confirmed the potential use of that hybrid design for optimization of radiolabeling processes.

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Section: Methodsmentioning

confidence: 99%

Facile radiolabeling optimization process via design of experiments and an intelligent optimization algorithm: Application for omeprazole radioiodination

Farrag

Abdel-Halim

Moamen

2019

Labelled Comp Radiopharmac

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“…Melphalan (Mel) is a bifunctional alkylating agent widely used at the clinical level in the treatment of multiple types of cancer and other diseases [ 1 , 2 , 3 , 4 ]. The effectiveness of killing cancer cells of this drug is based on the ability to react extensively with DNA, RNA, and proteins to form interstrand DNA crosslinks, inducing multiple kinds of molecular lesions [ 5 , 6 , 7 ]. Nevertheless, Mel presents serious therapeutic disadvantages related to its non-specificity, the resistance of tumor cells, and the need for increasingly higher doses during treatment, generating adverse effects that include leukopenia, mucositis, and diarrhea [ 8 , 9 ].…”

Section: Introductionmentioning

confidence: 99%

Solid-State Formation of a Potential Melphalan Delivery Nanosystem Based on β-Cyclodextrin and Silver Nanoparticles

Sierpe

Donoso-González

Lang

et al. 2023

IJMS

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Melphalan (Mel) is an antineoplastic widely used in cancer and other diseases. Its low solubility, rapid hydrolysis, and non-specificity limit its therapeutic performance. To overcome these disadvantages, Mel was included in β-cyclodextrin (βCD), which is a macromolecule that increases its aqueous solubility and stability, among other properties. Additionally, the βCD–Mel complex has been used as a substrate to deposit silver nanoparticles (AgNPs) through magnetron sputtering, forming the βCD–Mel–AgNPs crystalline system. Different techniques showed that the complex (stoichiometric ratio 1:1) has a loading capacity of 27%, an association constant of 625 M−1, and a degree of solubilization of 0.034. Added to this, Mel is partially included, exposing the NH2 and COOH groups that stabilize AgNPs in the solid state, with an average size of 15 ± 3 nm. Its dissolution results in a colloidal solution of AgNPs covered by multiple layers of the βCD–Mel complex, with a hydrodynamic diameter of 116 nm, a PDI of 0.4, and a surface charge of 19 mV. The in vitro permeability assays show that the effective permeability of Mel increased using βCD and AgNPs. This novel nanosystem based on βCD and AgNPs is a promising candidate as a Mel nanocarrier for cancer therapy.

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“…7 Melphalan has been labeled with 125 I directly to get [ 125 I]Melphalan, which has a high affinity to be localized in the tumor site and meets most of the requirements necessary to be used as a successful diagnostic and therapeutic agent. 8 We have synthesized a novel MFL derivative by conjugation of HYNIC to MFL, which is labeled by 99m Tc in high yield to get 99m Tc(HYNIC-MFL)(tricine)(TPPTS). The good accumulation in tumor tissue, high tumor/muscle ratios, and satisfactory scintigraphic images highlight the potential of 99m Tc(HYNIC-MFL)(tricine)(TPPTS) for tumor imaging.…”

Section: Introductionmentioning

confidence: 99%

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

Wang

Yang

Xue

et al. 2017

Labelled Comp Radiopharmac

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Melphalan (MFL) is a typical nitrogen mustard for the treatment of many types of cancer. For the purpose to develop novel Tc-labeled tumor imaging agents with SPECT, MFL was directly labeled by Tc using diethylene triamine pentacetate acid (DTPA) as bifunctional chelating agent. The novel ligands were successfully synthesized by conjugation of DTPA to MFL to get monosubstituted DTPA-MFL and bis-substituted DTPA-2MFL. Radiolabeling was performed in high yield to get Tc-DTPA-MFL and Tc-DTPA-2MFL, respectively, which were hydrophilic and stable at room temperature. The high initial tumor uptake with retention, good tumor/muscle ratios, and satisfactory scintigraphic images suggested the potential of Tc-DTPA-MFL and Tc-DTPA-2MFL for tumor imaging. However, the slow normal tissue clearance would be a great obstacle. Further modification on the linker and/or Tc-chelate to improve the tumor targeting efficacy and in vivo kinetic profiles is currently in progress.

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Preparation and biodistribution of [¹²⁵I]Melphalan: a potential radioligand for diagnostic and therapeutic applications

Cited by 16 publications

References 14 publications

Facile radiolabeling optimization process via design of experiments and an intelligent optimization algorithm: Application for omeprazole radioiodination

Facile radiolabeling optimization process via design of experiments and an intelligent optimization algorithm: Application for omeprazole radioiodination

Solid-State Formation of a Potential Melphalan Delivery Nanosystem Based on β-Cyclodextrin and Silver Nanoparticles

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

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Preparation and biodistribution of [125I]Melphalan: a potential radioligand for diagnostic and therapeutic applications

Cited by 16 publications

References 14 publications

Facile radiolabeling optimization process via design of experiments and an intelligent optimization algorithm: Application for omeprazole radioiodination

Facile radiolabeling optimization process via design of experiments and an intelligent optimization algorithm: Application for omeprazole radioiodination

Solid-State Formation of a Potential Melphalan Delivery Nanosystem Based on β-Cyclodextrin and Silver Nanoparticles

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

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Preparation and biodistribution of [¹²⁵I]Melphalan: a potential radioligand for diagnostic and therapeutic applications

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