JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS

Tc-99m-cefotaxime sodium (Tc-99m-CEF) was developed and standardized under varying conditions of reducing and antioxidant agent concentration, pH, radioactivity dose, and reducing agent type. Labeling studies were performed by changing the selected parameters one by one, and optimum labeling conditions were determined. After observing the conditions for maximum labeling efficiency and stability, lyophilized freeze dry kits were prepared accordingly. Simple method for radiolabeling of CEF with Tc-99m has been developed and standardized. Labeling efficiency of Tc-99m-CEF was assessed by both radio thin-layer chromatography and radio high-performance liquid chromatography and found higher than 90%. The labeled compound was found to be stable in saline and human serum up to 24h. Two different freeze dry kits were developed and evaluated. Based on the data obtained from this study, both products were stable for 6months with high labeling efficiency. The prepared cold kit was found sterile and pyrogen free. The bacterial infection and sterile inflammation imaging capacity of Tc-99m-CEF was evaluated. Based on the in vivo studies, Tc-99m-CEF has higher uptake in infected and inflamed thigh muscle than healthy thigh muscle

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS

Radiolabeled antibiotics are promising radiopharmaceuticals for the precise diagnosis and detection of infectious lesions. Doxycycline Hyclate (DOX) was chosen to investigate new Tc-99m-labeled antibacterial agent. Ready to use freeze dry kits were formulated with optimum labeling conditions. Human serum stability, sterility, and pyrogenicity of kits were estimated, and gamma scintigraphy, in vivo biodistribution, and histopathological studies with bacterial infected rats were performed. DOX were successfully labeled by Tc-99m with high radiochemical purity, and the labeled compound was stable in human serum. Kits were sterile, pyrogen-free, and stable up to 6months. Static images depicted rapid distribution throughout the body and high uptake in bacterial infected thigh muscle. The uptake ratios of radiopharmaceuticals in infected thigh muscle were found above 2 up to 5h. Five hours after injection, the rats were sacrificed, and biodistribution was determined. Samples of bacterial infected muscle, healthy muscle, blood, liver, spleen, lung, kidney, stomach, intestine, urine and heart were weighed, and the radioactivity was measured by using a gamma counter. The %ID/g of Tc-99m-DOX was found 0.230.06 for infected thigh muscle. According to the imaging, biodistribution, and histopathological studies, the promising characteristics of Tc-99m-DOX make the new radiopharmaceutical valuable to examine for future studies. Copyright (c) 2013 John Wiley & Sons, Ltd

Radioactive permeability studies of Doxycycline Hyclate from microemulsion and solution [Doksisiklin Hiklat’ın mikroemülsiyon ve çözelti dozaj şekillerinden radyoaktif permeabilite çalışmaları]

Doxycycline Hyclate (DOX) is an antibacterial drug which is member of the second tetracycline group and the absorption of DOX is reduced about 20% in the presence of skimmed milk. Therefore new drug delivery system can be advisable for DOX to reduce the food and drug interaction and improve the bioavailability. The aim of the present study is to prepare a microemulsion system of DOX which could result in reducing in food interaction and an improvement of oral bioavailability by increasing the drug’s permeability. For this purposes, DOX was radiolabeled with 99mTc. Radiochemical purity was determined with radioactive thin layer chromatography (RTLC) studies. Permeability of DOX from 99mTc-DOX solution (99mTc-DOX-S) and 99mTc-DOX loaded microemulsion (99mTc-DOX-M) was investigated with in vitro cell culture studies by using human colonic adenocarcinoma cell line (Caco-2). The radioactivity of99mTc-DOX-M for the apical to basolateral direction (Papp (A›B)) and basolateral to apical direction (Papp (B›A)) were found higher than 99mTc-DOX-S. Based on the in vitro cell culture studies, this dosage form is a promising formulation as an alternative for oral drug delivery of DOX. © 2016, Marmara University. All rights reserved

Radiolabeling and in vitro evaluation of 99mTc-methotrexate on breast cancer cell line

In the present study 99mTc-MTX was prepared with high labeling yield by a new simple and easy formulation method. According to cell culture studies, 99mTc-MTX incorporated with both MCF-7 and CRL8798 cells, with significant differences in the uptake percentages. Since 99mTc-MTX highly uptake in cancer cell line, the results demonstrated that radiolabeled MTX may be promising for breast cancer diagnosis of oncological patients. © 2015, Akadémiai Kiadó, Budapest, Hungary

Radiolabeling efficiency and cell incorporation of chitosan nanoparticles

Cationic nanoparticles of CS were developed according to ionotropic gelation process as potential cancer cell targeting agent. CS nanoparticles (CSNP) (F1 and F2) diameters varied between ranges of 100 e800 nm. Particle size, polydispersity index and zeta potential values of formulations were measured by photon correlation spectroscopy. The morphological analysis for CSNPs was provided with scanning electron microscopy. For cell incorporation study, F1 and F2 were directly labeled by Technetium-99m (99mTc), radiochemical purity and stability of the complex were analyzed by radioactive thin layer chromatography and radioactive high performance liquid chromatography studies. After that, incorporation of 99mTc labeled F1 and F2 were evaluated in U2OS and NCIeH209 cell lines. The six well plates were used for all experiments and the integrity of each cell monolayer was checked by measuring its TEER values with an epithelial voltammeter. Results confirmed that F1 and F2 formulations were successfully radiolabeled with 99mTc. The incorporation percentages of 99mTc labeled F1 and F2 in NCIeH209 and U2OS cell lines were found different when they compared to 99mTc solution. Since 99mTc labeled F1 and F2 highly uptake in cancer cell line. The results demonstrated that radiolabeled CSNPs may be a promising agent for cancer diagnosis. © 2015 Elsevier B.V. All rights reserved

Gamma scintigraphy and biodistribution of 99mTc-cefotaxime sodium in preclinical models of bacterial infection and sterile inflammation

PubMed ID: 2688070599mTc-cefotaxime sodium (99mTc-CEF) was developed and standardized under varying conditions of reducing and antioxidant agent concentration, pH, radioactivity dose, and reducing agent type. Labeling studies were performed by changing the selected parameters one by one, and optimum labeling conditions were determined. After observing the conditions for maximum labeling efficiency and stability, lyophilized freeze dry kits were prepared accordingly. Simple method for radiolabeling of CEF with 99mTc has been developed and standardized. Labeling efficiency of 99mTc-CEF was assessed by both radio thin-layer chromatography and radio high-performance liquid chromatography and found higher than 90%. The labeled compound was found to be stable in saline and human serum up to 24 h. Two different freeze dry kits were developed and evaluated. Based on the data obtained from this study, both products were stable for 6 months with high labeling efficiency. The prepared cold kit was found sterile and pyrogen free. The bacterial infection and sterile inflammation imaging capacity of 99mTc-CEF was evaluated. Based on the in vivo studies, 99mTc-CEF has higher uptake in infected and inflamed thigh muscle than healthy thigh muscle. Cefotaxime sodium (CEF) was successfully labeled with 99mTc from newly developed instant kit. Radiochemical purity was found greater than 90% and the labeled compound was stable in human serum during incubation period up to 24 h. The improved kit was found to be sterile, pyrogen free and stable up to 6 months. According to gamma scintigraphy studies, 99mTc-CEF showed a higher uptake in bacterial infected and sterile inflamed muscle than healthy thigh muscle. © Copyright 2016 John Wiley & Sons, Ltd

Radiolabeling and in vitro evaluation of a new 5-fluorouracil derivative with cell culture studies

PubMed ID: 31495966The clinical impact and accessibility of 99mTc tracers for cancer diagnosis would be greatly enhanced by the availability of a new, simple, and easy labeling process and radiopharmaceuticals. 5-Fluorouracil is an antitumor drug, which has played an important role for the treatment of breast carcinoma. In the present study, a new derivative of 5-Fluorouracil was synthesized as (1-[{1?-(1??-deoxy-2??,3??:4??,5??-di-O-isopropylidene-?-D-fructopyranose-1??-yl)-1?H-1?,2?, 3?-triazol-4?-yl}methyl]-5-fluorouracil) (E) and radiolabeled with 99mTc. It was analyzed by radio thin layer chromatography for quality control and stability. The radiolabeled complex was subjected to in vitro cell-binding studies to determine healthy and cancer cell affinity using HaCaT and MCF-7 cells, respectively. In addition, in vitro cytotoxicity studies of compound E were performed with HaCaT and MCF-5 cells. The radiochemical purity of the [99mTc]TcE was found to be higher than 90% at room temperature up to 6 hours. The radiolabeled complex showed higher specific binding to MCF-7 cells than HaCaT cells. IC50 values of E were found 31.5 ± 3.4 ?M and 20.7 ± 2.77 ?M for MCF-7 and HaCaT cells, respectively. The results demonstrated the potential of a new radiolabeled E with 99mTc has selective for breast cancer cells. © 2019 John Wiley & Sons, Ltd.09/DPT/001 Türkiye Bilimsel ve Teknolojik Araştirma Kurumu, TÃœBITAK: TUBITAK?115/S/935This study was supported by The Scientific and Technological Research Council of Turkey (TUBITAK?115/S/935). The authors also would like to thank the T.R. Prime Ministry State Planning Organization Foundation (Project Number: 09/DPT/001). The authors would like to acknowledge the support of Ege University Nuclear Medicine Department to obtain the 99m Tc radionuclide