Synthesis and Biological Evaluation of Bisphosphonate Compound Labeled with Tc-99m(CO)(3)(+)

WOS: 000350112600015PubMed ID: 25092179In this study, radiolabeling of a bisphosphonate, alendronate (Alendronate sodium), was performed with the help of a bifunctional chelating agent. For that purpose, DTPA-NHS (Diethylenetriaminepentaacetic acid dianhydride-N-hydroxysuccinimide) was synthesized with an esterification between DTPA and NHS. Combining the DTPA-NHS ester with alendronate yields the DTPA-Alendronate compound. The structure of synthesized compound was analyzed by H-1/C-13/P-31-NMR and HPLC. After then, the labeling with [Tc-99m(CO)(3)](+) core of synthesized compound was provided. Performing quality controls of newly synthesized [Tc-99m(CO)(3)-DTPA-Alendronate] complex with thin layer radiochromatography (TLRC) and high-performance liquid radiochromatography (HPLRC), the labeling yield was found as 99%. It was observed that the compound conserves its stability for 24h in serum media. Biodistribution of the radiolabeled complex was performed on Wistar Albino rats to determine radiopharmaceutical potential of the [Tc-99m(CO)(3)-DTPA-Alendronate] complex. It is thought that the data gained from this study will contribute to the development of complexes with bisphosphonate.Ege University (Bornova Izmir, Turkey)Ege University [2009NBE010]This study was financially supported by the Ege University Scientific Research Project numbered 2009NBE010, (Bornova Izmir, Turkey)

Design of docetaxel-loaded polymeric nanoparticles: characterization, radiolabeling with Tc-99m and in vitro evaluation

WOS: 000584877900005This research aims to develop a polymeric drug delivery system for docetaxel (DTX) and to investigate its radiotracer potential by in vitro. DTX loaded Poly(lactic acid)/Poly(ethylene glycol) diblock copolymer (PLA-PEG) was synthesized and radiolabeled with technetium-99m tricarbonyl core. PLA-PEG-DTX nanoparticles had a particle size and zeta potential 120 +/- 7.3 nm and - 24.66 +/- 1.5 mV respectively, which was further supported by SEM image. the radiolabeling efficiency of Tc-99m(CO)(3)-PLA-PEG-DTX was found to be 90 +/- 3.51%,. in vitro study was carried out on cancer cell lines (MCF7, MDA-MB-231) to examine the biological behavior of docetaxel loaded PLA-PEG nanoparticles. [GRAPHICS]

Synthesis of a radioiodinated antiestrogen glucuronide compound (TAM-G)

WOS: 000287756900002Tamoxifen [TAM; ([Z]-2-[4-(1,2-diphenyl-1-di-butenyl)-phenoxy]-N,N-dimethylethanamine) has been used as an antiestrogen drug for treatment and prevention of human breast cancer. The aim of this study is conjugation of hydrophilic glucuronic acid to the starting substance TAM and labeling with I-131 using iodogen as oxidizing agent. The reactions are completed in three steps, including enzymatic reaction, with the following sub-steps; preparation of microsomal fraction from rat liver and subsequent purification of UDP-glucuronyl transferase (UDPGT), estimation of protein amount in microsomal samples and glucuronidation reaction. Synthesized glucuronide derivative (TAM-G) was purified using high performance liquid chromatography (HPLC). Mass spectroscopy of cold standard showed that the labeling most probably occurs in ortho position to the aromatic ring containing the ether group of TAM-G as expected. Radiochemical yield of the I-131 labeled TAM-G ([I-131]TAM-G) is determined by using Thin Layer Radio Chromatography (TLRC). The radiopharmaceutical potential of [I-131]TAM-G is examined by biodistribution studies that is run on normal female Albino Wistar rats. According to biodistribution results I-131 labeled TAM-G may be proposed as a new antiestrogen glucuronide imaging agent for breast and uterus.T.R. Prime Ministry State Planning Organization [06 DPT 06]; Ege UniversityEge University [2007 NBE 006]This work financially supported by T.R. Prime Ministry State Planning Organization Contract No 06 DPT 06 and Ege University Research Fund contact no 2007 NBE 006