In vivo behavior of technetium-99m labeled ibuprofen in infection and inflamation animal models.

OBJECTIVE: The objective of this study was to develop radiolabeled ibuprofen (99mTc-ibu) for imaging and discrimination of inflammation and infection and compare its biodistribution in two different animal models. SIGNIFICANCE: The development of radiolabeled ibuprofen as an imaging agent for inflammation and infection may have significant clinical implications for the diagnosis and management of various inflammatory and infectious diseases. This study provides a promising approach to the detection of sterile infections. METHODS: Ibuprofen was radiolabeled with 99mTc using the stannous chloride method with a yield of 99.05 ± 0.83% (n = 5). The in vivo biological behavior of radiolabeled ibuprofen was determined in Wistar albino rat models of sterile inflammation and bacterial infection with Staphylococcus aureus gram-positive bacteria. Biodistribution studies were carried out at different time points, and the results were compared between the two animal models. RESULTS: The uptake of 99mTc-ibu in sterile inflammation sites at all time points was higher than that in the infection sites. This suggests that 99mTc-ibu can be used to discriminate between sterile inflammation and bacterial infection. CONCLUSIONS: The results of this study suggest that the detection of sterile infections with 99mTc-ibu is possible and highly encouraging.

Preparation of technetium-99m labeled ibuprofen by direct route and technetium-99m tricarbonyl route: a comparison of in vivo behaviors.

In the current study, ibuprofen (ibu) which is a non-steroidal anti-inflammatory drug (NSAID) was radiolabeled with 99mTc using two different methods: stannous chloride method (direct route) and technetium-99m tricarbonyl [99mTc(CO)3]+ route. Thus, it's aimed to investigate the radiolabeling potential of ibu for inflammation detection and to monitor if there is any difference in in vivo distribution depending on the radiolabeling route. Quality control studies of both radiolabeled ibu were performed by radiochromatographic methods (Thin Layer Liquid Radio Chromatography and High Performance Liquid Radio Chromatography). Radiolabeling yields of 99mTc-ibu and 99mTc(CO)3-ibu were determined as 99.05 ± 0.83% and 91.79 ± 3.30% (n = 5), respectively. Experimental lipophilicities of both radiolabeled ibu were determined. The biological behavior of both radiolabeled ibu was investigated in healthy Albino Wistar male rats by in vivo biodistribution studies. It was seen that both radiolabeled ibuprofen showed renal excretion while organ uptakes of 99mTc-ibu and 99mTc(CO)3-ibu differ against time.

Preparation and in vitro investigation of prostate-specific membrane antigen targeted lycopene loaded niosomes on prostate cancer cells.

In this study, it's aimed to develop prostate-specific membrane antigen (PSMA) targeted niosomes with a multifunctional theranostic approach. With this aim, PSMA-targeted niosomes were synthesized by a thin-film hydration method followed by bath sonication. Drug-loaded niosomes (Lyc-ICG-Nio) were coated with DSPE-PEG-COOH (Lyc-ICG-Nio-PEG) and subsequently anti-PSMA antibody conjugated to niosomes (Lyc-ICG-Nio-PSMA) with amide bond formation. Dynamic light scattering (DLS) analysis showed that the hydrodynamic diameter of Lyc-ICG-Nio-PSMA was approximately 285 nm and it was found with transmission electron microscopy (TEM) that the niosome formulation was spherical. Encapsulation efficiency was 45% and %65 upon dual encapsulation of ICG and lycopene. The results of fourier-transform infrared spectroscopy (FTIR) and X-ray photoelectron spectroscopy (XPS) demonstrated that PEG coating and antibody coupling were successfully done. In vitro studies showed that cell viability decreased when lycopene was entrapped into niosomes applied while the total apoptotic cell population rose slightly. When Lyc-ICG-Nio-PSMA was applied to cells, decreased cell viability and enhanced apoptotic effect were seen compared to those for Lyc-ICG-Nio. In conclusion, it was demonstrated that targeted niosomes displayed improved cellular association and decreased cell viability on PSMA + cells.

In Vitro Incorporation of Radioiodinated Eugenol on Adenocarcinoma Cell Lines (Caco2, MCF7, and PC3).

Recently, the synthesis of radiolabeled plant origin compounds has been increased due to their high uptake on some cancer cell lines. Eugenol (EUG), a phenolic natural compound in the essential oils of different spices such as Syzygium aromaticum (clove), Pimenta racemosa (bay leaves), and Cinnamomum verum (cinnamon leaf), has been exploited for various medicinal applications. EUG has antiviral, antioxidant, and anti-inflammatory functions and several anticancer properties. The objective of this article is to synthesize radioiodinated (131I) EUG and investigate its effect on Caco2, MCF7, and PC3 adenocarcinoma cell lines. It is observed that radioiodinated EUG would have potential on therapy and imaging due to its notable uptakes in studied cells.

Investigation of therapeutic efficiency of bleomycin and bleomycin-glucuronide labeled with (131)I on the cancer cell lines.

The aim of this study is to determine the incorporations of radiolabeled bleomycin ((131)I-BLM) and bleomycin-glucuronide ((131)I-BLMGLU) on PC-3 (human prostate carcinoma cell line), Caco-2 (human colon adenocarcinoma cell line), Hutu-80 (Human Duodenum adenocarcinoma cell line), and A549 (Human lung adenocarcinoma epithelial cell line) cancerous cell lines. For this purpose, BLM and BLMGLU enyzmatically synthesized were labeled with (131)I, quality control studies were done and the incorporation yields of (131)I-BLM and (131)I-BLMGLU on these cell lines were measured. Quality-control studies showed that the radiolabeling yields were obtained as 95% and 90% for (131)I-BLM and (131)I-BLMGLU, respectively. Also, as a result of the cell culture studies, it was found that (131)I-BLM and (131)I-BLMGLU had higher incorporation on PC-3 cells than that of other cell lines. In addition to this, it was reported that the incorporation yield of (131)I-BLMGLU was higher than that (131)I-BLM. At the end of the study, cytotoxicities of BLM and BLMGLU on PC-3 cancerous cell line were inspected and fluorescent images of BLM and BLMGLU were taken on PC-3 cells by using fluorescein isothiocyanate. In conclusion, cell culture studies demonstrated that the incorporation values of (131)I-BLMGLU on the four cell lines were about five to six times higher than (131)I-BLM. Radiolabeled glucuronide derivatives can be used in cancer therapy and tumor imaging, depending on the properties of radioiodine for the ß-glucuronidase-rich tissues because glucuronidation leads to rapid and higher incorporation on adenocarcinoma cells.

Anti toxic effect of broccoli extract on stannous dichloride toxicity.

PURPOSE: Since Technetium-99m ((99m)Tc) has favorable physical and chemical characteristics, it is widely used radioisotope in Nuclear Medicine. However, stannous dichloride (SnCl(2)) has been widely used as a reducing agent in labeling procedure of pharmaceutical with radionuclide, it has been realized that SnCl(2) have genotoxic and cytotoxic effects on biological systems. In previous studies, it has been shown that some herbal extract can reduce genotoxic and cytotoxic effects of SnCl(2). In the present study, it is aimed to evaluate the effect of the broccoli extract on the survival of E. coli ATCC 25922 strain against to toxic effects of SnCl(2). METHODS: Broccoli was extracted with methanol extraction. HPLC and TLC analysis of broccoli extract were performed. Then antitoxicity and dose response assays were performed on bacterial strain. RESULTS: The broccoli extract had dose dependent protective effect against SnCl(2) toxic effect on E. coli. CONCLUSIONS: The consumption of broccoli may alter the stannous dichloride toxicity. Broccoli extract may use as a new protective strategies against the toxic effect of SnCl(2) on patients who were taken (99m)Tc radiopharmaceuticals.