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

Abstract

The 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‐β‐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 μM and 20.7 ± 2.77 μM 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.

Radiolabeled Trastuzumab Solid Lipid Nanoparticles for Breast Cancer Cell: in Vitro and in Vivo Studies

“…Twenty microliters of AO/EB solution (3.5 μM AO and 2 μM EB in PBS) was added to the formulations, and they were covered with a coverslip. 26 Morphological changes were also evaluated and imaged by fluorescence microscopy with a 350–400 nm filter (200× magnification).…”

“…Briefly, developed SLNs (SLN-1, SLN-2, TRZ-SLN-1, and TRZ-SLN-2) were administered to cells to show some changes in MCF-7 cells for 24 h. After that, cells were resuspended in pH 7 phosphate buffer and then transferred to glass slides. Twenty microliters of AO/EB solution (3.5 μM AO and 2 μM EB in PBS) was added to the formulations, and they were covered with a coverslip . Morphological changes were also evaluated and imaged by fluorescence microscopy with a 350–400 nm filter (200× magnification).…”

A preliminary study on radiolabeling and quality control of [99mTc]Tc-6-mercaptopurine to develop tumor scintigraphic agent

“…The radioactivity on plates was assessed using a TLC scanner (Bioscan AR 2000) after chromatographic separation, and the RP (%) of [ 99m Tc]Tc was estimated using the following equation (Eq. 1) [18,19]:…”

99mTc-exendin-4: Radiolabeling and quality control studies of glucagon-like peptide analog

“…Instant thin layer chromatography-silica gel coated plates (ITLC-SG) were used to determine R/H 99m Tc in a solvent system of Acetonitrile/Water/Trifluoroacetic acid (ACN/W/TFA; 50/25/1.5). The radioactivity of the stationary phases was assessed using a TLC scanner, and the RP of 99m Tc was estimated using following equation [30,31]: RP (percent) = 100 -[Free 99m Tc (percent) + R/H 99m Tc (percent)] In vitro stability: To test the stability of newly developed radiopharmaceutical, 0.1 mL of 99m Tc-exendin-4 and 0.4 mL of 0.9 percent sodium chloride solution was mixed [32]. After that, the mixture was allowed to leave at room temperature for 6 h. Every hour, RTLC experiments were used to assess the complex's labeling stability.…”