99mTc-labeled glimepiride as a tracer for targeting pancreatic β-cells mass: preparation and preclinical evaluation

El-Kawy, O. A.; Garcı́a-Horsman, J. Arturo

doi:10.1007/s10967-017-5615-1

Cited by 11 publications

(7 citation statements)

References 33 publications

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“…An ideal partition coefficient for a drug is typically intermediate in value (neither too lipophilic nor too hydrophilic) in cases where molecules reach their targets. The observed participation coefficient (P) value of the 99m Tc‐plazomicin complex was 0.8 ± 0.1, indicating a hydrophilic complex with low liver uptake (El‐Kawy & García‐Horsman, 2017a). This is promising as the complex may be used to detect liver abscesses.…”

Section: Resultsmentioning

confidence: 99%

“…The 99m Tc‐plazomicin structure was predicted by molecular mechanics calculations using ChemBio3D ultra 14 software (El‐Kawy & García‐Horsman, 2017a). The proposed structure was further confirmed by subjecting the complex rhenium analog following HPLC purification (3 mg plazomicin, 1.71 mg stannous chloride dihydrate, 730 µg potassium perrhenate, pH 7, and the reaction was kept at room temperature for 20 min) to 1 HNMR analysis in CDCl 3 using Bruker High‐Performance Digital FT‐NMR Spectrometer Avance III MHz (Bruker, UK) following its HPLC isolation.…”

Section: Methodsmentioning

confidence: 99%

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Radiolabeling, characterization, and preclinical evaluation of plazomicin: A potential tracer for bacterial infection

2022

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In this study, 99mTc–plazomicin, a new radio‐antibiotic complex, was prepared specifically for bacterial infection localization and monitoring. Factors affecting the labeling reaction were studied and optimized to obtain a high yield (98.8 ± 0.2%). In silico, radiochemical and physicochemical characterization and biodistribution were performed to assess the complex aptness as a radiopharmaceutical. The complex was biologically evaluated in vitro using bacteria and in vivo using different inflammation models (sterile, bacterial, and fungal). Uptake in the bacterial model was highest (7.8 ± 0.3%). Results indicated that the technetium label did not alter the antibiotic biological behavior and backed the usefulness of 99mTc‐plazomicin as a potential tracer.

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Section: Resultsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

Radiolabeling, characterization, and preclinical evaluation of plazomicin: A potential tracer for bacterial infection

2022

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“…The structure was predicted by synthesizing the complex cold rhenium analog. 21 Accurately weighed acetaminosalol (6 mg, 22.1 μmol) was added to a mixture of freshly prepared stannous chloride dihydrate solution (2 mg, 8.8 μmol) and perrhenate solution (3.2 mg, 11.1 μmol). Sodium hydroxide (0.2 M) was used to adjust the pH of the reaction mixture to 7.…”

Section: Structure Confirmation and Characterization Of The Labeled C...mentioning

confidence: 99%

Preparation and evaluation of radiolabeled acetaminosalol microspheres: A new potential selective radiotracer for ulcerative colitis early diagnosis

El‐Kawy,

Shweeta,

Abdelgawad

2023

Labelled Comp Radiopharmac

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Acetaminosalol labeling reaction with technetium‐99m was optimized, and the radiocomplex was obtained in a high radiochemical yield of 98.9 ± 0.6% and high stability (>30 h). The tracer was characterized, and its binding to the PPARγ receptor was assessed in silico. To reduce radiation exposure to non‐target organs and increase accumulation in the colon, the tracer was formulated as pH‐sensitive microspheres with a mean particle size of 201 ± 2.1 μm, a polydispersity index of 0.18, a 25.3 ± 3.6 zeta potential, and 98.6 ± 0.33% entrapment efficiency. The system suitability was assessed in vivo in normal and ulcerative rats, and the biodistribution profile in the colon showed 56.5 ± 1.4% localization within 4 h. Blocking study suggested the selectivity of the tracer to the target receptor. Overall, the reported data encouraged the potential use of the labeled microspheres to target ulcerative colitis.

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“…ChemBio3D ultra 2014 software was used to predict the structure and generate the optimized geometries of the 177 Lu-TDTMP complex by molecular mechanics' calculations using our previously reported method [20,21]; (a molecular geometry related physiochemical property) was computed and compared with the experimental value to confirm the proposed structure of the complex. Then, 1 H NMR analysis was performed using Bruker High Performance Digital FT-NMR Spectrometer Avance III 400 MHz and the software ACD/ 1 D NMR Processor V 12 was used to process the NMR data, assign correlation and further confirm the proposed structure [22] .…”

Section: Structure Prediction and Nmr Analysismentioning

confidence: 99%

Preparation and Evaluation of 177Lu-TDTMP: A Potential Theranostic Agent for Bone Metastases

Talaat¹

2019

Arab Journal of Nuclear Sciences and Applications

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Lu was produced in high-specific activity and excellent radionuclidic purity by thermal neutron bombardment of 176 Yb target. Tetramethylene diamine tetramethylenephosphonic acid (TDTMP) was radiolabeled with 177 Lu and the complexation parameters were studied and optimized: 8.4 µg TDTMP, ~243 µCi of 177 Lu activity, pH= 8 and the reaction mixture was kept at room temperature for 30 min. The complex was formed with high yield (>99%) and retained its stability for more than 14 days. The complex structure was predicted and its binding to target enzyme was assessed. A biodistribution study carried out in normal and tumorized Wister rats showed a significant skeletal uptake, the 177 Lu-TDTMP, the results clearly indicated that it has high affinity for bone mineral. Femur and tibia uptakes of the labelled complex were ~ 6.4 % and ~7.1 % at 3 hours post injection compared to ~ 4 % and ~ 4.3 % in case of 177 LuCl 3. Thereafter, the uptakes increased continuously to a maximum of ~ 7.9 % and ~ 8.3 % at 48 hours after injection were noticed.

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99mTc-labeled glimepiride as a tracer for targeting pancreatic β-cells mass: preparation and preclinical evaluation

Cited by 11 publications

References 33 publications

Radiolabeling, characterization, and preclinical evaluation of plazomicin: A potential tracer for bacterial infection

Radiolabeling, characterization, and preclinical evaluation of plazomicin: A potential tracer for bacterial infection

Preparation and evaluation of radiolabeled acetaminosalol microspheres: A new potential selective radiotracer for ulcerative colitis early diagnosis

Preparation and Evaluation of 177Lu-TDTMP: A Potential Theranostic Agent for Bone Metastases

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