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Sample records for 131i labeled 17-allylamino-17-demethoxygeldanamycin

  1. Hsp90 inhibitor 17-allylamino-17-demethoxygeldanamycin inhibits the proliferation of ARPE-19 cells

    Wang Lin

    2010-04-01

    Full Text Available Abstract Background The antiproliferative effect of the Hsp90 inhibitor 17-AAG (17-allylamino-17-demethoxygeldanamycin on human retinal pigment epithelial cells is investigated. Methods MTT and flow cytometry were used to study the antiproliferative effects of the 17-AAG treatment of ARPE-19 cells. 2D gel electrophoresis (2-DE and mass spectrometry were applied to detect the altered expression of proteins, which was verified by real-time PCR. Gene Ontology analysis and Ingenuity Pathway Analysis (IPA were utilized to analyze the signaling pathways, cellular location, function, and network connections of the identified proteins. And SOD assay was employed to confirm the analysis. Results 17-AAG suppressed the proliferation of ARPE-19 cells by inducing cell cycle arrest and apoptosis. Proteomic analysis revealed that the expression of 94 proteins was altered by a factor of more than 1.5 following exposure to 17-AAG. Of these 94, 87 proteins were identified. Real-time PCR results indicated that Hsp90 and Hsp70, which were not identified by proteomic analysis, were both upregulated upon 17-AAG treatment. IPA revealed that most of the proteins have functions that are related to oxidative stress, as verified by SOD assay, while canonical pathway analysis revealed glycolysis/gluconeogenesis. Conclusions 17-AAG suppressed the proliferation of ARPE-19 cells by inducing cell cycle arrest and apoptosis, and possibly by oxidative stress.

  2. Expression of interleukin-6 is downregulated by 17-(allylamino)-17-demethoxygeldanamycin in human prostatic carcinoma cells

    Ke-hung TSUI; Tsui-hsia FENG; Wen-chi HSIEH; Phei-lang CHANG; Horng-heng JUANG

    2008-01-01

    Aim: Interleukin-6 (IL-6) is a pleiotropic cytokine that is associated with tumor metastasis and prostate cancer. We evaluated the mechanism and effect of 17-(allylamino)-17-demethoxygeldanamycin (17AAG), a novel inhibitor of heat shock protein 90 (Hsp90), on the IL-6 gene expression in human prostatic carcinoma (PC-3) cells. Methods: Quantitative IL-6 and IL-6 receptor (IL-6R) expressions were assessed using RT-PCR. The deregulation of 17AAG and phor-bol 12-myristate 13-acetate (PMA) on the IL-6 gene was determined by ELISA and transient gene expression assays using an IL-6 reporter vector. Results: Although the IL-6R is ubiquitously expressed by prostatic epithelium cells, the IL-6 expression is only found in advanced prostatic carcinoma cells, such as PC-3 and DU145. Further studies using RT-PCR indicated that 17AAG downregulated the gene expression of IL-6. ELISA and the transient gene expression assay revealed that 17AAG blocked the stimulation of PMA of IL-6 gene expression in PC-3 cells. The PMA-induced IL-6 gene expression is dependent on the NF-κB response element. However, the effect of 17AAG appears to be mediated via a region located at -149 to +8 bp upstream of the transcriptional starting site of the IL-6 gene, and might not be through the NF-κB signaling pathway. Conclusion: The present study reveals that IL-6 is transcriptionally downregulated in human prostatic carcinoma cells in response to 17AAG. This result suggests the presence of a novel Hsp90 mediation pathway that is involved in the deregulation on the transcription of the human IL-6 gene in human prostate cancer.

  3. Inhibition of homologous recombination repair in irradiated tumor cells pretreated with Hsp90 inhibitor 17-allylamino-17-demethoxygeldanamycin

    In order to investigate the mechanism of radio-sensitization by an Hsp90 inhibitor 17-allylamino-17-demethoxygeldanamycin (17-AAG), we studied repair of DNA double strand breaks (DSBs) in irradiated human cells pre-treated with 17-AAG. DSBs are thought to be the critical target for radiation-induced cell death. Two human tumor cell lines DU145 and SQ-5 which showed clear radio-sensitization by 17-AAG revealed a significant inhibition of DSB repair, while normal human cells which did not show radio-sensitization by the drug indicated no change in the DSB repair kinetics with 17-AAG. We further demonstrated that BRCA2 was a novel client protein for Hsp90, and 17-AAG caused the degradation of BRCA2 and in turn altered the behavior of Rad51, a critical protein for homologous recombination (HR) pathway of DSB repair. Our data demonstrate for the first time that 17-AAG inhibits the HR repair process and could provide a new therapeutic strategy to selectively result in higher tumor cell killing

  4. The effect of 17-allylamino-17-demethoxygeldanamycin alone or in combination with paclitaxel on anaplastic thyroid carcinoma cells.

    Kim, Si Hyoung; Kang, Jun Goo; Kim, Chul Sik; Ihm, Sung-Hee; Choi, Moon Gi; Yoo, Hyung Joon; Lee, Seong Jin

    2015-04-01

    The effect of 17-allylamino-17-demethoxygeldanamycin (17-AAG), an hsp90 inhibitor, alone or in combination with paclitaxel on survival of anaplastic thyroid carcinoma (ATC) was evaluated. In 8505C and CAL62 cells, after treatment of 17-AAG, cell viability decreased, and the percentage of dead cells increased. 17-AAG did not cause cleavage of caspase-3 protein, and change expression of IAPs. Pretreatment of z-VAD-fmk did not alter cell viability and the percentage of dead cells. In 17-AAG-treated cells, knockdown of p53 rescued growth inhibition, while cycloheximide attenuated cell death. When cells were treated with both 17-AAG and paclitaxel, all of the combination index values were higher than 1, indicating antagonism between 17-AAG and paclitaxel. In 17-AAG- and paclitaxel-treated cells, compared with paclitaxel alone-treated cells, the protein levels of hsp90, hsp70, and hsc70 increased. In conclusion, our results suggest that 17-AAG induces non-apoptotic cell death requiring de novo protein synthesis in ATC cells. Moreover, these results demonstrate that 17-AAG antagonizes paclitaxel with concomitant alterations in hsp90 client proteins in ATC cells. PMID:25096912

  5. 17-Allylamino-17-demethoxygeldanamycin induces downregulation of critical Hsp90 protein clients and results in cell cycle arrest and apoptosis of human urinary bladder cancer cells

    17-Allylamino-17-demethoxygeldanamycin (17-AAG), a benzoquinone ansamycin antibiotic, specifically targets heat shock protein 90 (Hsp90) and interferes with its function as a molecular chaperone that maintains the structural and functional integrity of various protein clients involved in cellular signaling. In this study, we have investigated the effect of 17-AAG on the regulation of Hsp90-dependent signaling pathways directly implicated in cell cycle progression, survival and motility of human urinary bladder cancer cell lines. We have used MTT-based assays, FACS analysis, Western blotting, semi-quantitative RT-PCR, immunocytochemistry and scratch-wound assay in RT4, RT112 and T24 human urinary bladder cancer cell lines. We have demonstrated that, upon 17-AAG treatment, bladder cancer cells are arrested in the G1 phase of the cell cycle and eventually undergo apoptotic cell death in a dose-dependent manner. Furthermore, 17-AAG administration was shown to induce a pronounced downregulation of multiple Hsp90 protein clients and other downstream effectors, such as IGF-IR, Akt, IKK-α, IKK-β, FOXO1, ERK1/2 and c-Met, resulting in sequestration-mediated inactivation of NF-κB, reduced cell proliferation and decline of cell motility. In total, we have clearly evinced a dose-dependent and cell type-specific effect of 17-AAG on cell cycle progression, survival and motility of human bladder cancer cells, due to downregulation of multiple Hsp90 clients and subsequent disruption of signaling integrity

  6. Synergistic effect of heat shock protein 90 inhibitor, 17-allylamino-17-demethoxygeldanamycin and X-rays, but not carbon-ion beams, on lethality in human oral squamous cell carcinoma cells

    The purpose of this study is to clarify the effect of a heat shock protein 90 inhibitor, 17-allylamino-17-demethoxygeldanamycin (17-AAG), in combination with X-rays or carbon-ion beams on cell killing in human oral squamous cell carcinoma LMF4 cells. Cell survival was measured by colony formation assay. Cell-cycle distribution was analyzed by flow cytometry. Expression of DNA repair-related proteins was investigated by western blotting. The results showed 17-AAG to have synergistic effects on cell lethality with X-rays, but not with carbon-ion beams. The 17-AAG decreased G2/M arrest induced by X-rays, but not by carbon-ion beams. Both X-ray and carbon-ion irradiation up-regulated expression of non-homologous end-joining-associated proteins, Ku70 and Ku80, but 17-AAG inhibited only X-ray-induced up-regulation of these proteins. These results show that 17-AAG with X-rays releases G2/M phase arrest; cells carrying misrepaired DNA damage then move on to the G1 phase. We demonstrate, for the first time, that the radiosensitization effect of 17-AAG is not seen with carbon-ion beams because 17-AAG does not affect these changes. (author)

  7. Radiochromatographic Determination of 131I Labeled Eugenol

    F. Zümrüt Biber Müftüler

    2015-02-01

    Full Text Available Phenolic phytochemicals are a broad class of nutraceuticals found in plants which have been extensively researched by scientists for medicinal potential. Eugenol, a phenolic natural compound available in the essential oils primarily extracted from clove plants, has been exploited for various medicinal applications. It possesses antioxidant, antimutagenic, antigenotoxic, anti-inflammatory and anticancer properties. The goal of current study was to extract Eugenol compound from clove plant and radiolabel the eugenol with 131I which is a well known radioisotope for imaging and therapy in Nuclear Medicine by utilizing iodogen method. The yield of radiolabeling of Eugenol (131I-E was calculated over 80% by Thin Layer Radio Chromatography and High Performance Liquid Radio Chromatograpy methods. Structural analysis of Eugenol was confirmed by Liguid Chromatography Mass Spectroscopy. Lipophilicity and stability studies were performed. Due to the attachment of iodine to Eugenol, radioiodinated Eugenol was more lipophilic. Stability of 131I-E was appropriate for study period. All experimental results suggest that 131I labeled Eugenol compound may be used in the applications of Nuclear Medicine as a radiolabeled agent for imaging and therapy on various cancer types.

  8. Identification of genes involved in the sensitivity to antitumour drug 17-allylamino,17-demethoxygeldanamycin (17AAG).

    Barresi, Vincenza; Fortuna, Cosimo G; Garozzo, Roberta; Musumarra, Giuseppe; Scirè, Salvatore; Condorelli, Daniele F

    2006-05-01

    In the present study we analysed the gene expression database provided by the National Cancer Institute in an attempt to correlate activity profiles of geldanamycin, 17AAG and 11 other analogues in 60 human tumor cell lines with their gene expression profiles determined by the cDNA microarray technique. On the basis of the activity profiles two classes of geldanamycin analogues could be distinguished, having geldanamycin and 17AAG, respectively, as prototype compounds (denominated as gelda-like and 17AAG-like classes). Application of the "soft" statistical methodology of PLS (partial least squares modelling in latent variables or projections to latent structures) allowed us to evaluate the influence of each gene expression target in determining the therapeutical responses. The transcript encoding the translocating chain-associated membrane protein (TRAM) showed a significant statistical correlation with activity profiles of 17AAG. In order to validate the role of TRAM in determining sensitivity to 17AAG we induced a selective knocking-down of this transcript by the RNA interference methodology in H226 non-small cell lung carcinoma cell line. The efficiency of double-stranded RNA oligonucleotides (short-interfering RNAs, siRNAs) was determined by measuring TRAM mRNA levels by quantitative real-time RT-PCR at different times (24-72 hours) after siRNA lipotransfection. A significant increase in chemosensitivity to 17AAG was observed in siRNA-silenced cells. Although a number of factors may affect tumour sensitivity to 17AAG the present methodology allowed us to dissect out a single parameter which may be partly responsible for its activity. PMID:16880941

  9. Synthesis of 131I labeled diiodothyronine (131I-T2)

    Objective: To synthesise 131I-T2 as the basis for future synthesis of 131I-T2S with sulfation. Methods: Firstly 3-T1 was radiolabeled with 131I with chloramine-T(Ch-T) labeling method. Then gel column chromatography and paper chromatography were used for separation and purification. Measurement of the labeling efficiency, radiochemical purity,stability of labeled compound, and identification of the product of immune activity were carried out. Results: The radiolabeling yield of the labeled compound produced with the modified Ch-T method was about 65.1%±4.5% (n=5) and the radiochemical purity was about 96.5%±1.1% (n=5). After 10d storage at -20 degree C, the radiochemical purity of the product still remained above 90%. Conclusion: High rate of labeling efficiency and good stability could be obtained with Ch-T labeling method. (authors)

  10. 131I-Lipiodol labelling and its clinical application

    Lipiodol-131 I is used as a contrast agent in lymphangiography and it also acts as an immunosupress agent for the endolynphatic irradiation in patients who need renal transplant. The labelling of lipiodol with I-131 occurs by isotopic exchange and the separation of the labelled 131 I is carried out through a solvent extraction technique. Quality control tests (radiochemical, biological, microbiological and pyrogenic) were performed, and the result was that the compound is suitable for clinical application. The labelling yield varied from 70 to 85%. Doses of 925 MBq were injected into the dorsal paw of the patient's feet which permitted the visualization of all the lymphatic region. (author)

  11. Detecting inflammation with {sup 131}I-labeled ornidazole

    Asikoglu, M. E-mail: asikoglum@eczacilik.ege.edu.tr; Yurt, F.; Cagliyan, O.; Unak, P.; Ozkilic, H

    2000-09-15

    The aim of this study was to demonstrate the accumulation of {sup 131}I-labeled ornidazole ({sup 131}I-ORN) in experimental abscesses. {sup 131}I-ORN was prepared by electrophilic radioiodination of ORN, using radioiodide in the presence of Iodogen[reg]. An in vivo inflammation model was prepared by intramuscular injection of turpentine into the thigh of rabbits. Four days later {sup 131}I-ORN was intravenously administered to rabbits. Serial scintigrams were performed at different periods, using a Sophy DX Gamma Camera. {sup 131}I-ORN was visualized at 10 min after injection. {sup 131}I-ORN was also administered intraperitoneally to rats with turpentine-induced inflammation, for quantitative biodistribution studies. Counts of selected tissues were taken by a NaI(Tl) scintillation detector (gamma counter) after rats were decapitated. The target-to-non-target muscle ratios were 2.5, 2.6, 2.9 and 1.9 at 1, 3, 5 and 24 h, respectively.

  12. Pharmacodynamics of benziadarone labelled with 131-I

    Regarding the importance of benziodarone (Retrangor) - 2-ethyl-3-(3',5'-diiodo-4'-hidrovibenzoyl)benzofuran - in medical practice in respect of its vasodilator and uricosuric action, a working plan was developed intending to study the biological distribution of the drug rats Wistar and, using the plasmatic curve, to find out the existence of other compartments besides the intravascular one. With these data, the rhythms of benziodarone exchange were established, simulating its distribution in the organism. It was possible to develop this working project because the benziodarone structure could be labelled with iodine-131, using an isotopic exchange reaction, having chloramine T as an oxidant agent. The labelled compound was employed as radioactive tracer, and its specific activities varied from 18 uCi/mg to 20 uCi/mg

  13. Synthesis and labelling of 19-iodocholesterol 131I

    Considering the increasing interest in obtaining agents for vizualization of the adrenal gland with radioisotopic techniques, 19-iodocholesterol was prepared by means of chemical synthesis and radioiodine (131I) introduced by isotopic exchange reaction. The reaction product was identified by determination of the melting point and elementary spectroscopic analysis (infra-red absorption and magnetic nuclear ressonance). Radiochemical analysis of the labelled compound was performed by means of then-layer cromatography in silica-gel. In order to confirm its capacity of concentration in the adrenal gland, the distribution of 19-iodocholesterol 131I, after intravenous injection, was tested in rats. (Author)

  14. Distribution of 131 I- labeled Bothrops erythromelas venom in mice

    Bothrops erythromelas is responsible for many snake bites in northeastern Brazil. In the present study we determined the in vivo distribution of the venom following its subcutaneous injection into mice. B. erythromelas venom and albumin were labeled individually with 131 I by the chloramine T method, and separated in a Sephacryl S-200 column. The efficiency of labeling was 68%.Male Swiss mice (40-45 g), which had been provided with drinking water containing 0.05% KI over a period of 10 days prior to the experiment, were inoculated dorsally (sc) with 0.3 ml (2.35 x 105 cpm/mouse) of 131 I-venom (N = 42), 131 -albumin or 131 I (controls, N = 28 each). Thirty minutes and 1,3, 6, 12, 18 and 24 h after inoculation, the animals were perfused with 0.85% Na Cl and skin and various organs were collected in order to determine radioactivity content. There was a high rate of venom absorption int he skin (51%) within the first 30 min compared to albumin (20.1%) and free iodine (8.2%). Up to the third hour after injection there was a tendency for venom and albumin to concentrate in the stomach ( 3 rd h),small intestine (3 rd h) and large intestine (6th h). Both control groups had more radioactivity in the digestive tract, especially in the stomach, but these levels decreased essentially to baseline by 12-18 h postinjection. In the kidneys, the distribution profiles of venom, albumin and iodine were similar. Counts at 30 min postinjection were low in all three groups (1.37, 1.86 and 0.77, respectively), and diminished to essentially 0% by 12-18 h. Albumin tended to concentrate in muscle until the 3 rd h postinjection (1.98%).There was a low binding of labeled venom in the liver (B. erythromelas venom does not specifically target most internal organs. That is, the systemic effects of envenomation ar mainly due to an indirect action. (author)

  15. Detection of DNA-protein cross-links by 131I post labelling method

    131I post labelling method is developed to detect DNA-protein cross-links (DPCs) induced by environmental contaminants and carcinogens in the level of whole animal. The results demonstrate that RATS liver DPCs caused by carcinogens-aflatoxin B1(AFB1) and nitrosamine in food can be examined simply, effectively, rapidly and sensitively using the established optimum reaction conditions of 131I post labelling method. This reveals favorable prospects of 131I post labelling method to detect widely DPCs

  16. Design and construction of a shielded process box for the production of radiopharmaceuticals labelled with 131I

    A leakproof process box, shielded with a 5 mm lead wall, for the labelling, purification, pH adjutment and dispensing of Rose Bengal 131I, Hippuran 131I, Diprocon 131I, Hipaque 131I, Bromosuphthalein 131I, etc. is described. (author)

  17. Labeling of apigenin with 131I and bioactivity of 131I-apigenin in male and female rats

    Apigenin (4',5,7-trihydroxyflavone), one of the most common flavonoids, has been shown to possess a variety of biological activities including tumor growth inhibition and chemopreventation. In the present study, apigenin was labeled with 131I using iodogen method and investigated of its bioactivity. Radiolabeling yield is 98±0.2%, as determined by radio thin layer chromatography (RTLC), electrophoresis and radio high performance liquid chromatography (RHPLC). Besides, structure analysis of synthesized cold iodoapigenin complex were assessed with LCMS/ MS and 1H-NMR. Results of in vitro study indicated a high stability (3 hours) in human serum. Biodistrubition studies are performed in male and female albino Wistar rats. Biodistribution data related to the male rats showed significant uptake in the small intestine. The female rats biodistribution results indicated that the uptake of 131I-apigenin was high in the intestine and uterus. (author)

  18. Synthesis and 131I labelling of epidepride as a dopamine D2 receptor imaging agent

    S-(-)-N-[(1-ethyl-2-pyrrolidinyl)methyl]-5-iodo-2, 3-dimethoxybenzamide (Epidepride) and its iodine labeling precursor S-(-)-N-[(1-Ethyl-2-pyrrolidinyl)methyl]-5-tributyltin-2, 3-dimethoxybenzamide are synthesized from 3-methoxy salicylic acid. The labeling precursor is labeled with 131I by hydrogen peroxide method, and 131I-epidepride is gained, its radiolabelling yield (RLY) and the radiochemical purity (RCP) are all over 95%. The RCP of 131I-epidepride is over 90% under 4 degree C after 15 days. 131I-epidepride has high affinity to dopamine D2 receptor. The striatal uptake can be blocked completely by spiperone. The striatum and cerebellum uptake ratio can reach 237 at 320 min in rats. The results show that 131I-epidepride may be used as a dopamine D2 receptor imaging agent for SPECT

  19. Synthesis labeling and biological studies of 16-131I

    The increasing interest in obtaining radiopharmaceuticals for metabolic imaging of heart muscle led us to prepare 16-IODINE HEXADECANOIC ACID by tosilation of the corresponding hydroxy acid, following iodination with NaI and finally, introducing radioiodine (Na131I) by isotopic exchange reaction. The reaction products were identified by determination of melting point, elementary and spectroscopic analysis such as infra-red absortion and magnetic nuclear resonance. The radiopharmaceutical after radiochemical and other specific control procedures for injetable such as sterility and apyrogenicity, was firstly utilized in dogs: preferencial uptake by the heart, as well as by the liver was confirmed. Then, studies in patients with or without heart diseases were performed. The biodistribution of 16-131I-HEXADECANOIC ACID was carried out in Wistar rats. The scintigraphic images in animals and in humans demonstrated that 16-131-HEXADECANOIC ACID is suitable for studying viable areas as well as energetic exchange of heart muscle. (author)

  20. Therapeutic efficacy of intralesional 131I-labelled hyaluronectin in grafted human glioblastoma

    Girard, N.; Courel, M.N.; Vera, P.; Delpech, B. [Centre Henri-Becquerel, Rouen (France). Laboratoire d' Oncologie Moleculaire

    2000-07-01

    The grafted human glioblastoma cell CB109 was used as a model for intralesional therapy with 131I-labelled hyaluronectin glycoprotein (131I-HN). 131I-HN bound specifically to in situ hyaluronic acid (HA), a main component of the extracellular matrix which is involved in tumour invasion. Labelling experimental conditions were determined and, finally, 25 {mu}Ci/{mu}gHN, 1 {mu}g chloramine-T/{mu}gHN and a 60-s stirring period provided a 131I-HN preparation with an optimal affinity for HA (64% compared to unlabelled HN). Following intratumoral injection, 131I-HN was retained with a limited diffusion outside the tumour. On day 4 the radioactivity concentrated in the tumour was still 25 times greater than that in the liver, spleen and kidneys combined. For therapeutic assays, 65 {mu}Ci 131I-HN was injected into the tumour, resulting in a delivery of 6.8 Gy over a 7-day period. Controls received unlabelled HN, heat-inactivated HN, a mixture of inactivated HN plus free 131I or no treatment (six animals per group). Tumour volumes were evaluated every second day from treatment day and the rate of tumour growth was expressed as a ratio of tumour size at time intervals to the tumour size at the time of injection. Growth curves were compared: heat-inactivated with or without free 131I had no anti-tumour effect. Unlabelled HN-injected tumours had a slightly slower growth rate than untreated tumours (p < 0.02) and growth rate of 131I-HN-injected tumours was much lower (p < 0.00002). A pronounced inhibitory effect with intralesional 131I-labelled HN injection resulted from a combination of a) blockage of HA, a proliferation facilitating factor, and b) local irradiation of tumoral tissue, while uptake in normal tissues was minimized.

  1. An experimental study on labeling monoclonal antibody 4E5 with 131I and the lethal effects of 131I-4E5 against B cell lymphoma

    Objective: To label the monoclonal antibody 4E5 with 131I and to evaluate the lethal effects of 131I-4E5 against B cell lymphoma. Methods: 4E5 was radiolabeled with 131I using the Iodogen method at room temperature. The labeling efficiency and radiochemical purity was measured with trichloroacetic acid (TCA) precipitation, and the immune activity and stability of 131I-4E5 was analyzed. The lethal effects of 131I-4E5 and 4E5 against Raji cells were evaluated by 3-(4, 5-dimethylthiazol-2-yl)-2, 5-dipheny-lte-trazolium bromide (MTT) assay. Analysis of variance and t-test were used for data analysis with SPSS 13.0. Results: The labeling rate of 131I-4E5 was (78.3±2.4)%, and the radiochemical purity was (95.7±1.8)%. Its specific activity and radioactive concentration were 0.58 MBq/μg and 3.90 × 1010 Bq/L, respectively. The radiochemical purity of 131I-4E5 mixed with serum and PBS was over 90% after three days. The maximum specific binding efficiency of 131I-4E5 with Raji cells was (36.06±2.63)%. 131I-4E5 exhibited a dose-dependent cytotoxicity against Raji cells. The lethal effect of the high dose group was significantly stronger than that of the low dose group. When the radioactive concentrations were 1.48 × 1010, 7.40 × 109, 3.70 × 109, 1.85 × 109 and 9.25 × 108 Bq/L, the cell inhibition ratios were (52.98±5.19)%, (46.29±2.80)%, (41.05±4.83)%, (33.68±3.79)% and (17.89±2.78)%, respectively (F=33.882, P<0.001). In the 4E5 group, when concentrations of 4E5 were 20.0, 10.0, 5.0, 2.5 and 1.25 mg/L, the cell inhibition ratios were (32.98±3.99)%,(30.88±3.98)%, (27.14±2.05)%, (20.35±4.38)% and (8.42±1.05)%, respectively. Accordingly,significantly higher growth inhibition rates for Raji cells than 4E5 at all antibody concentrations were tested (t=5.290, 5.489, 4.596, 3.986 and 5.515, all P<0.05). Conclusions: The labeling efficiency and radiochemical purity of 131I-4E5 using Iodogen method is high,and the in vitro stability of 131I-4E5 is optimal. 131I-4E5

  2. Extraction, radiolabeling and in vivo biological evaluation of {sup 131}I labeled egonol glycosides extract

    Akguel, Yurdanur; Pazar, Erdinc [Ege Univ., Izmir (Turkey). Chemistry Dept.; Yilmaz, Habibe; Sanlier, Senay Hamarat [Ege Univ., Izmir (Turkey). Biochemistry Dept.; Lambrecht, Fatma Yurt [Ege Univ., Izmir (Turkey). Dept. of Nuclear Applications; Yilmaz, Osman [Dokuz Eyluel Univ., Izmir (Turkey). Dept. of Lab. Animal Science

    2015-09-01

    Crude extract of S. officinalis L. was found to have suspending agent, hemolytic, antitumor, antioxidant and antimicrobial activities. Its major components benzofurans and benzofuran glycosides have antifungal, anticancer, antibacterial and anticomplement activities and display acetylcholinesterase-cyclooxygenase inhibitory and cytotoxic properties. Recently, it has been reported that egonolgentiobioside is a valuable target for structural modification and warrants further investigation for its potential as a novel pharmaceutical tool for the prevention of estrogen deficiency induced diseases. The aim of the current study is to perform in vivo biological evaluation of a glycosides extract, which was isolated from the fruits endocarp of Styrax officinalis L, identified as egonolgentiobioside and homoegonolgentiobioside and labeled with {sup 131}I. The radiolabeled glycosides extract was labeled with {sup 131}I with high yield. The labeled obtained radiolabeled compound was found to be quite stable and lipophilic. In order to determine its tissue distribution, an in vivo study was performed using healthy female Albino Wistar rats injected by {sup 131}I-glycosides. The biodistribution results showed that clearance of the radiolabeled compound is through the hepatobiliary pathway. The experimental study indicated that the radiolabeled glycosides extract accumulated in the large intestine. Therefore, the potential of {sup 131}I-glycosides might be evaluated in colon cancer cell lines and this might be a promising of tumor-imaging agent.

  3. Investigation of therapeutic efficiency of phenytoin (PHT) labeled with radioactive 131I in the cancer cell lines

    The aim of this study is to determine the incorporations of PHT radiolabeled with 131I (131I-PHT) on U-87 MG, Daoy and A549 cancerous cell lines. For this, cold and radio-labeling studies were carried out. The radiolabeling yield of 131I-PHT was obtained about 95 %. Subsequently, cell culture studies were carried out and radio-labeling yields of 131I, 131I-PHT on U-87 MG, Daoy and A549 cancerous cells were investigated. Cell culture studies demonstrated that the incorporation values of 131IPHT on the three cell lines decreased with increasing radioactivity. Consequently, 131I-PHT may be a good radiopharmaceutical for targeting radionuclide therapy of Central Nervous System Tumors. (author)

  4. Radioimmunoscintigraphy of human gastric carcinoma xenografts with 131I-labeled antigastric carcinoma monoclonal antibody, GL013

    Monoclonal antibody GL013 with specific binding reactivity in vitro to human tumors of the gastrointestinal tract was radioiodinated and injected intraperitoneally into nude mice bearing human gastric carcinoma xenografts SY86B (moderately differentiated glandular adenocarcinoma) and SY86D (signet ring cell carcinoma). Wholebody scintigraphy demonstrated tumor localization with 131I-labeled MAb GL013, but not with 131I-labeled normal mice immunoglobulin. Best tumor contrast was obtained between days 3 and 7 after injection. In confirmation of imaging results, 131I-GL013 preferentially localized in tumor tissue compared with normal tissue and 131I-GL013 gave higher tumor uptake ratio than did control 131I-NMIgG (at day 9 after injection), as determined by tissue counting of radioactivity. These results demonstrate that MAb GL013 does localize to the xenografts SY86D and SY86D and suggest the possible clinical application of MAb GL013 in radioimmunolocalization

  5. Radioimmunoimaging of ovarian cancer with 131I labelled CEA monoclonal antibody

    Objective: To investigate radioimmunoimaging with 131I labelled CEA McAb and its value in diagnosis and treatment of ovarian cancer. Methods: CEA McAb was labelled with 131I by standard chloramine T procedure. The radiolabeled McAb was given intravenously to the patients. The scintigraphy was performed at different time. Results: In 105 patients with histopathology proved ovarian cancers, for 96 patients the lesions were well located with RII (true positives), for the remaining 9 patients, the results were false negative. 22/23 cases with RII diagnosed benign ovarian tumors were proved to be true negative by surgical pathology in RII. Of 96 ovarian cancers 87 were stratified into identical stages by surgical pathology all RII. 141/151 metastatic tumors were found in RII and the positive rate was as high as 93.4%. The smallest tumor defected by RII was of 1 cm in diameter. Conclusions: RII is as good as ultrasonography and CT in distinguishing benignancy and malignancy. The location, size and number of the lesions can also be determined with RII. RII of ovarian cancer with 131I-CEA McAb is valuable and helpful in early detection of ovarian cancer. It is also helpful for clinical staging, treatment programing and prognosticating

  6. Phagocytosis of 131I labelled Salmonella typhymurium in splenic remnants. Experimental study in rats

    Forty-one male Wistar rats were divided into three groups, namely: Group I - Normal animals; Group II - Animals submitted to total splenectomy with subsequent intraperitoneal splenic autotransplantion; Group III - Animals submitted to partial 50% splenectomy with subsequent autotransplantation of the removed fragment. After 40 weeks of close observation all animals were administred 70 Micro Ci of an 131I - labelled ''Salmonella Typhymurium'' suspension. Twelve hours later all animals were sacrificed and a complete peritoneal cavity inventory was performed. Samples of both topic spleen and regenerated autotransplant were obtained, processed and autoradiographed. (M.A.C.)

  7. SPECT imaging of neuropilin receptor type-1 expression with 131I-labeled monoclonal antibody.

    Dou, Xiaofeng; Yan, Jianghua; Zhang, Yafei; Liu, Peng; Jiang, Yizhen; Lv, Sha; Zeng, Fanwei; Chen, Xiaoli; Wang, Shengyu; Zhang, Haipeng; Wu, Hua; Zhang, Hong; Ouyang, Lin; Su, Xinhui

    2016-09-01

    As a novel co-receptor for vascular endothelial growth factor (VEGF), neuropilin receptor type-1 (NRP-1) is overexpressed in several cancers and metastases, and serves as an attractive target for cancer molecular imaging and therapy. Previous single photon emission computerized tomography (SPECT) studies demonstrated that the small NRP-1-targeting peptides 99mTc-MA-ATWLPPR and 99mTc-CK3 showed poor tumor imaging quality, because of their rapid blood clearance and very low tumor uptake. Compared with small peptides, monoclonal antibodies (mAbs) can improve imaging of NRP-1-expression, due to their high affinity, specificity and slow extraction. A6-11-26 is a novel monoclonal antibody against NRP-1 b1b2 domain that exhibits inhibition of tumor growth in NPR-1-expressing preclinical models. The aim of the present study was to develop the 131I-labeled anti-NRP-1 monoclonal antibody A6-11-26 as a SPECT probe for imaging of NRP-1-positive tumor. An anti-NRP-1 monoclonal antibody (A6-11-26) was produced by hybridomas and was labeled with iodine-131 by the iodogen method. In vitro, the radiolabeling efficiency, radiochemical purity, immunoreactive fraction and stability were assessed. Binding affinity and specificity of 131I‑A6-11-26 to NRP-1 were evaluated using human glioblastoma U87MG cells. In vivo, biodistribution and SPECT/CT studies were conducted on mice bearing U87MG xenografts after the injection of 131I-A6-11-26 with or without co-injection of unlabeled A6-11-26 antibody. A6-11-26 was generated successfully by hybridoma with high purity (>95%) and was labeled with iodine-131 within 60 min with high labelling efficiency (95.46±3.34%), radiochemical purity (98.23±1.41%). 131I-A6-11-26 retained its immunoreactivity and also displayed excellent stability in mouse serum and PBS solution during 1 to 96 h. Cell uptake assays showed high NRP-1-specific uptake (15.80±1.30% applied activity at 6 h) in U87MG cells. 131I-A6-11-26 bound to NRP-1 with low nanomolar

  8. Advances on the treatment of solid tumor by 131I labeled mouse-human chimeric tumor necrosis therapy monoclonal antibody

    131I labeled mouse-human chimeric tumor necrosis therapy monoclonal antibody (131I-chTNT) is a kind of new drug targeting at degenerated or necrotic nuclei in the tumor necrosis zone,and may be applicable to the majority of human solid tumors, such as lung cancer, liver cancer,colon carcinoma and glioma, while conventional tumor cell monoclonal antibody can target only tumor cell surface antigen. Enhanced effects can be achieved by 131I-chTNT in combination with other therapies, such as radiotherapy,chemotherapy or radiofrequency ablation, which may increase tumor necrosis region and expose more combinative targets. (authors)

  9. Experience in immunoscintigraphy with 131I-labelled OC-125 F(ab')2 in patients with ovarian carcinoma

    In the specialized postoperative follow-up of patients with epithelial ovarian carcinoma, radioimmunoscintigraphy could usefully complete computed tomography and ultrasound results. Restrictions concerning the use of 131I labelled antibody fragments result, however, from radiation dosimetry and protection aspects: Although not more than 140 MBq of the 131I agent is administered because of the high thyroid and whole-body radiation exposure, for some days substantial excretion of 131I into urine occurs. This prevents us drastically from applying the method to the same extent as recommended in the literature. These limitations are expected to be overcome with 99mTc or 111In antibodies. (author)

  10. Labelling of meta-iodobenzylguanidine with iodine-131 (I-131-MIBG) for adrenal gland diagnosis

    Labelling of meta-iodobenzylguanidine with iodine-131 (I-131 MIBG, for adrenal gland diagnosis has been studied. The MIBG was synthesized from the reaction of meta-iodobenzylamine hydrochloride with cyanamide and labelled with iodine-131 by isotope exchange method using copper(II) as a catalyst. The percentage of labelling was about 98%, with a specific activity of 1.5-2.0 mCi/mg. The radiochemical purity was found to be greater than 99%. Biodistribution studies were performed on mice, the results showed great affinity for the adrenal gland uptake with highest radioactivity after 1 day of injection. The stability of the product with 1% benzyl alcohol was 7 days upon storing at 40C

  11. Migration behaviour of 14C labelled bicarbonate, HTO and 131I in boom clay

    Performance assessment studies for the deep geological disposal of radioactive waste in the Boom clay indicated the importance of the radionuclides 14C and 129I. The migration properties of these radionuclides in Boom clay are studied by Flow-Through type diffusion experiments. In the diffusion tests a mixture of 14C labelled bicarbonate, tritiated water (HTO) and carrier free 131C labelled bicarbonate, tritiated water (HTO) and carrier free 131I sodium iodide (NaI) is used. The isotope 131I is used as an equivalent for 129I. The mixture allows for a good comparison of the migration behviour of the three different species. The mean value of the diffussion constant for bicarbonate is 1.8x10-6, for iodide 4.2x10-6 and for tritiated water 6.2x10-6 cm2.s-1. For the interpretation of the experiments we consider sorption (isotopic exchange), diffusion and first order chemical reaction. The results of the diffusion tests are consistent with the concept of the diffusion accessible porosity and proves the importance of this concept. The diffusion accessible porosity for both bicarbonate and iodide is 0.11. The results are important for the safety assessment of a radioactive waste repository in the clay formation. (orig.)

  12. Experimental radioimmunotherapy of a xenografted human glioma using 131I-labeled monoclonal antibody to epidermal growth factor receptor

    131I-labeled F (ab')2 fragments of murine monoclonal antibodies (MAb) 425 specific to the epidermal growth factor receptor expressed on human gliomas were used in experimental human malignant glioma immunotherapy. Two injections of 150 μCi 131I-labeled 425 F(ab')2 achieved growth inhibition of U-87MG human malignant glioma xenografts in nude mice. This radiolabeled specific MAb F(ab')2 was significantly superior to radiolabeled fragments of an anti-hepatitis virus control MAb A5C3 in influencing tumor growth. However, similar treatment of established human malignant glioma xenografts did not inhibit progressive tumor growth significantly. No clear tumor inhibition was produced by unlabeled MAb 425F(ab')2. These studies suggest that 131I-labeled MAbs have a significant antitumor effect where unmodified antibody is ineffective. Multiple doses of antibody may achieve an increase in labeled MAb concentration in tumors. (author)

  13. Labeling of - N-Isopropil - p - I-Anphetamine (IMP-131I) and its biological distribution in rats

    The described labeling and purification preparation of N-Isopropil-p131I-anphetamine (131I-IMP) represents a fast and efficient method to obtains a compound that fullfills all criterions of purity for its application 'IN VIVO'. The labeling yield was 68-78% and the radiochemical purity performed by paper chromatography and electrophorese was 97-99%. As demostrated in animal experiments, the cerebral affinity offers a possibility to study brain diseases in clinical studies when the product will be labelled with 123I. (author)

  14. Synthesis, labelling and clinical studies of 131 I meta-iodobencylguanidine

    Radiolabelled meta-iodobencylguanidine (MIBG) is one of the most successful among recent radiopharmaceuticals. It has been shown to have high diagnostic sensitivity and specificity for many tumors of neuroectodermal origin. Synthesis, labelling and clinical studies of 131 I-MIBG are presented. Synthesis of the compound was carried out by condensation of meta-iodobenzylamine with cyanamide and sulphate salt formation. The radiolabelled compound was obtained by isotope exchange in an aqueous system at 150 Centigrade in presence of copper (II) as a catalyst. Clinical tests were carried out administrating the radiotracer to 13 patients (19 images) and comparing with those obtained from 5 patients to whom the study was made again with a commercial product. Results were similar for both products. Furthermore, it was possible to localize three neuroblastomas and one ganglioneuroblastoma. (Author)

  15. Radioimmunolocalization of human gastric carcinoma xenografts SY 86 B and SY 86 D with 131I-labeled monoclonal antibody

    The suitability of individual MAb for application in vivo should be carefully confirmed. The monoclonal antibody GL-013, with specific binding reactivity in vitro to human tumors of the gastrointenstinal tract, was radioiodinated and injected intraperitoneally into nude mice bearing human gastric carcinoma xenografts SY 86 B (moderately differentiated glandular adenocarcinoma) and SY 86 D (signet ring cell carcinoma). Whole body scintigraphy indicated tumor localization with 131I-labeled MAb GL-013, but not with 131I-labeled normal mice immunoglobulin. The best tumor contrast was obtained between days 3 and 7 after injection. As confirmation of the imaging results, 131I-GL-013 preferentially localized in tumor tissue compared with normal tissue and 131I-GL-013 gave a higher tumor uptake ratio than the control 131I-NMIgG (at day 9 after injection), as determined by tissue counting of radioactivity. These results demonstrate that MAb GL-013 localizes in xenografts SY 86 B and SY 86 D and the possible clinical application of MAb GL-013 to radioimmunolocalization. (author)

  16. Radioimmunotherapy for pancreatic carcinoma using 131I-labeled monoclonal antibody Nd2 in xenografted nude mice

    We investigated the biodistribution, radiolocalization, and radioimmunotherapeutic potential of 131I-labeled Nd2 in athymic nude mice bearing human pancreatic carcinoma xenografts. 131I-Nd2 was accumulated at high levels in the tumor, in contrast to blood, liver, spleen, and other normal organs. The tumor was clearly delineated in scintigraphs. The volumes of tumors of mice injected with 7.4 MBq of 131I-Nd2 were 80% less than those of tumors before injection of radiolabeled Nd2. Fibrous or vacuolar degeneration was seen in histological sections of tumors of 7-week-treated mice. The growth of tumors in mice treated with misonidazole, a hypoxic cell radiosensitizer, and then injected twice with 3.7 MBq of 131I-Nd2 was suppressed over 7 weeks. Neither leucocytopenia nor thrombocytopenia was severe after injection of radiolabeled Nd2. Thus 131I-labeled Nd2 may have clinical application in the radioimmunotherapy of pancreatic cancer. (author)

  17. Animal experiments in positive tumor scintigraphy based on the demonstration of clostridium rods using 131I-labelled antibodies

    Clostridial spores, applied i.v. to mice, grew out selectively to rods in transplanted tumors and could be demonstrated by 131I-labelled antibodies. An increased radioactivity was to be seen after additional application of Ig G. The decreased tumor activity compared to that of the blood depends probably on the inhibited blood flow of the tumor

  18. Thermal effect on photolysis in 203Hg, 35S and 131I labeled mercury (II) iodide thiocyanate powders

    203Hg, 35S or 131I labeled mercury (II) iodide thiocyanate (HgISCN) powders were prepared, respectively. When the powders were exposed to sunlight, some parts of the crystals of the powders were decomposed and the decomposed atoms diffused toward crystal surface. This diffusion velocity was accelerated by thermal treatment of the darkened powders. The velocity is larger in order of 35S, 203Hg, 131I. Decomposed products consist of colloidal mercury, mercury iodide, mercury sulfide, sulfur dioxide and iodine. Mechanism of photochromism of HgISCN was discussed. (author)

  19. Radiochemical and biological control for metaiodobenzylguanidine (MIBG) labelled with 131I

    This study shows the standardization of the radiochemical control of MIBG-131I in eletrophoretic system and also the biological control in Wistar rat for a period of time, not longer than 60 minutes after the tracer administration. (author)

  20. Radiochemical and biological control of metaiodobenzyl-guanidine (MIBG) labeled with 131I

    This study shows the standardization of the radiochemical control of MIBG - 131I in eletrophoretic system and also the biological control in Wistar rat for a period of time, not longer than 60 minutes after tracer administration. (author)

  1. Uptake and depuration of {sup 131}I from labelled diatoms (Skeletonema costatum) to the edible periwinkle (Littorina littorea)

    Wilson, R.C. [Westlakes Scientific Consulting Ltd., The Princess Royal Building, Westlakes Science and Technology Park, Moor Row, Cumbria CA24 3LN (United Kingdom)]. E-mail: richard.c.wilson@westlakes.ac.uk; Vives i Batlle, J. [Westlakes Scientific Consulting Ltd., The Princess Royal Building, Westlakes Science and Technology Park, Moor Row, Cumbria CA24 3LN (United Kingdom); Watts, S.J. [Westlakes Scientific Consulting Ltd., The Princess Royal Building, Westlakes Science and Technology Park, Moor Row, Cumbria CA24 3LN (United Kingdom); McDonald, P. [Westlakes Scientific Consulting Ltd., The Princess Royal Building, Westlakes Science and Technology Park, Moor Row, Cumbria CA24 3LN (United Kingdom); Parker, T.G. [British Nuclear Group, Sellafield, Cumbria CA20 1PG (United Kingdom)

    2007-07-15

    Uptake and depuration of {sup 131}I into winkles through consumption of the diatom Skeletonema costatum is described. The work follows on from previous studies that investigated the uptake of iodine into winkles from seawater and seaweed. Incorporation of {sup 131}I in S. costatum from labelled seawater followed linear first-order kinetics with an uptake half-time of 0.40 days. Iodine uptake in winkles from labelled S. costatum also followed linear first-order kinetics, with a calculated equilibrium concentration (C {sub {infinity}}) of 42 Bq kg{sup -1} and a transfer factor (TF) of 1.1 x 10{sup -4} with respect to labelled diatom food. This TF is lower than that observed for uptake of {sup 131}I in winkles from labelled seaweed. For the depuration stage, a biphasic sequence with biological half-lives of 1.3 and 255 days was determined. The first phase is biokinetically important, given that winkles can lose two-thirds of their activity during that period. This study shows that, whilst winkles can obtain radioactive iodine from phytoplankton consumption, they do not retain the majority of that activity for very long. Hence, compared with other exposure pathways, such as uptake from seawater and macroalgae, incorporation from phytoplankton is a relatively minor exposure route.

  2. Combination of microwave ablation and 131I labeled tumor necrosis therapy chimeric antibody in the treatment of lung cancer

    Microwave ablation (MWA) has been considered as an advanced, minimally invasive technique in the treatment of lung cancer with a high local efficiency. MWA can inactivate tumor cells based on microwave heating mechanisms. It has a high local control rate of primary peripheral lung cancer and metastatic lung cancer result from percutaneous microwave antennas injection under ultrasound, CT and MRI guidance. However, for the lesions those are greater than 3.0 cm in diameter or abutting the hilars and the diffuse lesions there is less effective. 131I labeled tumor necrosis therapy chimeric antibody (131I-chTNT), a novel radioimmunotherapy which uses cell of degeneration or necrotic tumor cell nuclear antigen as target provides a new therapeutic approach for lung cancer, but the complete response is low. MWA can induce a mass tumor necrosis under the action of microwave thermal effect which greatly increases the targeting area for 131I-chTNT radioimmunotherapy. Therefore, combination of MWA and 131I-chTNT will enhance the treatment efficacy of lung cancer. (authors)

  3. Labelling and pharmacokinetics of 131I-bleomycin with regard to tumor affinity and in comparison with 57Co- and 111In-bleomycin

    Bleomycin was labelled with 131I and checked electrophoretically and chromatographically as to its activity. The pharmacokinetics of 131I-bleomycin were tested in mice bearing different tumors. Its whole-body retention and organ distribution were determined in comparison to 57Co- and 111In-bleomycin, resp

  4. Sterility Study of 131I-Labelled Preparations Designed for Human Diagnostics

    Owing to the relatively long incubation period, no classical sterility tests can be applied for preparations containing radionuclides with short half-lives. An initial sterility testing of the working sites and materials used, completed by the quick testing of the end-product, might be used instead. The efficiency of the method is demonstrated by experiments performed with 131I-albumin and 131I-hippurane. Data are published on the time-dependent decline of colony-forming centres in radioactive products. (author)

  5. DOTA-Tyr3-octreotate labelled with 177Lu and 131I. A comparative evaluation

    The chemical structure of somatostatin receptor ligand 1,4,7,10-tetraazacyclododecane- N,N',N',N'''-tetraacetic acid-Tyr3-octreotate (DOTA-Tyr3-TATE), provides the means for radiolabelling with halogen, by electrophilic substitution, to the Tyr3 residue and with metal, by a coordination mechanism, to the DOTA chelator. In this study, the DOTA-Tyr3-TATE was radiolabelled with 177Lu and 131I of high radiochemical purity and specific activity. The in vitro study regarding the competitive and the saturation binding assays were performed using rat brain cortex membrane. The IC50 value was determined as 4.74nM for natLu-DOTA-Tyr3-TATE and the Kd value was 142.8pM for 177Lu-DOTA-Tyr3-TATE. The biodistribution data of 177Lu-DOTA-Tyr3-TATE and DOTA-131I-Tyr3-TATE in HRS1 (hepato-colangiom carcinomas) tumour bearing rats, show that the 177Lu-DOTA-Tyr3-TATE is more stable and has better uptake than DOTA-131I-Tyr3-TATE. Furthermore, the competitive localization index of 177Lu- DOTA-Tyr3-TATE is three times higher than that obtained for DOTA-131I -Tyr3-TATE. The results of work based on comparative experiments suggest that 177Lu-DOTA-Tyr3- TATE could be an effective targeted radiotherapy agent of SSTR tumours. (author)

  6. Distribution and radioimmunoimaging of 131I labeled anti-NPC monoclonal antibody BAC5 in tumor bearing nude mice

    To provide an evidence for clinical applications, the distribution and radioimmunoimaging of 131I labeled anti nasopharyngeal carcinoma (NPC) monoclonal antibody BAC5 in tumor bearing nude mice were studied. McAb BAC5, against NPC, was labeled with 131I and injected into nude mice bearing NPC cell line CNE-2. The biodistribution of 131I-BAC5 and whole body ECT imaging were studied at various intervals after injection. The % ID/g were 6.38, 11.27 and 14.19 for tumor and 7.78, 3.48 and 2.59 for liver at 48, 96 and 144h postinjection respectively. The T/NT ratios were 0.82, 3.24 and 5.47 for liver at 48, 96 and 144h postinjection respectively. Tumor showed clearly at 3 days after injection. The quality of tumor images was relevant to the T/NT ratio. The results demonstrated that McAb BAC5 has specifically bind to NPC tissue and may also possess the capability of leading to human NPC

  7. Labelling of Iomazenil with 123I and 131I to be used as neurotracer in nuclear medicine

    Iomazenil, a benzodiazepine analogue of Flumazenil, was labeled with 131I and 123I to enable SPECT (Single Photon Emission Computed Tomography) investigations of central benzodiazepine receptors in human brain. First, the bromoprecursor was characterized by means of elemental analysis and infrared spectrophotometry. The chromatography of this chemical was performed by means of HPLC - High Performance Liquid Chromatography. In order to optimize the labeling parameters of the Iomazenil, Iodine 123I was first used. The following parameters were investigated: temperature, time period, amount of precursor and radioactivity. The labeling parameters described in the literature were used during this study. Several chromatograms were evaluated; as a result, the chromatogram proposed by the literature achieved the best performance. After the establishment of the best labeling parameters and the determination of the radiochemical purity, the stability of the 131I-Iomazenil was studied. Studies using 123I solutions fi-om IEN/CNEN and IPEN/CNEN, were done and the last one showed the best result. Biological investigations were done using iomazenil labeled with 121I. Toxicity, biological distribution and cerebral uptake in mice were evaluated. This study showed that this labeled product cross the blood brain barrier, allowing benzodiazepine brain receptor imaging. (author)

  8. Iodobell in vivo kits for labelling with 123I or 131I

    Iodobell in vivo kits provide an easy and fast method for 'on the spot' radioiodination with 123I (or 131I). Until now three kits have been developed in the Institute of Isotopes Budapest, the heptadecanoic acid, the hippurate and the MIBG kits. From these, the heptadecanoic acid kit is being tested in humans in Hungary, the other two are under the registration procedure. The Iodobell in vivo kits may contribute to the application of 123I radioisotope in Hungary. (orig.)

  9. Monte Carlo microdosimetry of {sup 188}Re- and {sup 131}I-labelled anti-CD20

    Torres-GarcIa, E [Coordinacion de Posgrado, Facultad de Medicina, Universidad Autonoma del Estado de Mexico, Paseo Tollocan S/N, Toluca, Estado de Mexico 50180 (Mexico); Garnica-Garza, H M [Coordinacion de Posgrado, Facultad de Medicina, Universidad Autonoma del Estado de Mexico, Paseo Tollocan S/N, Toluca, Estado de Mexico 50180 (Mexico); Ferro-Flores, G [Instituto Nacional de Investigaciones Nucleares, Carretera Mexico-Toluca, Ocoyoacac, Estado de Mexico 52750 (Mexico)

    2006-10-07

    The radiolabelled monoclonal antibody anti-CD20 has the property of binding to the CD20 antigen expressed on the cell surface of B-lymphocytes, thus making it a useful tool in the treatment of non-Hodgkin's lymphoma. In this work, the event-by-event Monte Carlo code NOREC is used to calculate the single-event distribution function f{sub 1}(z) in the cell nucleus using the beta spectra of the {sup 188}Re and {sup 131}I radionuclides. The simulated geometry consists of two concentric spheres representing the nucleus and the cell surface embedded in a semi-infinite water medium. An isotropic point source was placed on the cell surface to simulate the binding of the anti-CD20 labelled with either {sup 188}Re or {sup 131}I. The simulations were carried out for two combinations of cell surface and nucleus radii. A method was devised that allows one to calculate the contribution of betas of energy greater than 1 MeV, which cannot be simulated by the NOREC code, to the single-event distribution function. It is shown that disregarding this contribution leads to an overestimation of the frequency-mean specific energy of the order of 9-12%. In general, the antibody radiolabelled with {sup 131}I produces single-event distribution functions that yield higher frequency-mean specific energies. (note)

  10. Localization of 131I-labelled monoclonal antibody ERIC1 in a subcutaneous xenograft model of neuroblastoma in SCID mice

    Our purpose was to evaluate a novel strategy of immunolocalization of human neuroblastoma by targeting the neural cell adhesion molecule (NCAM), which is over-expressed on neuroblastoma. Neuroblastoma is the most frequent solid extracranial childhood tumour and also the most common neoplasm in the first year of life. The most frequent metastatic sites are bone, bone marrow and liver. The neural cell adhesion molecule (NCAM) is constitutively expressed on nearly 100% of all neuroblastomas. NCAM has been successfully used as a target for immunotoxines and bi-specific antibodies in multiple myeloma, small cell lung cancer, glioma or neuroblastoma, in vitro and in vivo. NCAM expression was quantified on established neuroblastoma cells by real time PCR and NCAM expression on the cell surface shown by flow cytometry. A SCID mouse model using IMR5-75 neuroblastoma cells to induce subcutaneous tumour growth was established. 131I was used to label monoclonal NCAM specific ERIC1 antibodies generating the 131I-ERIC1 antibody, which shows a high affinity to NCAM also after labelling (KD= 9 x 10-8). Groups of five to six mice received intravenous injections of 3-9 MBq of 131I-ERIC1 on day 0 into the tail vein. At time points 2.5 h, 24 h, 48 h, 72 h and 96 h post injection mice were sacrificed by cervical dislocation. Blood, liver, spleen, kidneys, muscle, femur, thyroid, intestines, lung, tumour and urine were removed and weighed. Organ-specific radioactivity was measured in a well-counter as well as that of the tail and remnant cadavers. Data were calculated as dose per gram of tissue (%ID/g) and tumour to non-tumour ratios (T/NT ratio). For blocking experiments mice were pre-injected with 140μg of unlabelled ERIC1 into the tail vein 24 h prior 131I-ERIC1 application. Mice from these blocking experiments were measured after 72 h. Measurement of organ-specific radioactivity showed low organ-specific uptake (5.33 %ID/g after 72 h), which continuously decreased over the 96 hour

  11. Detection of experimental thrombi in rabbits with an 131I-labelled fibrin-specific monoclonal antibody

    The detection of thrombi in rabbits has been investigated with 131I-labelled DD-3B6/22, a monoclonal antibody (Mab) reactive at high affinity (Kd=2.68x10-10 M) with human D Dimer (DD). DD-3B6/22 bound well to both 'fresh' and 'aged' human clots in an in vitro assay but showed poor binding to rabbit clots. However, reactivity was restored to rabbit blood if it was seeded, before clotting, with human DD covalently coupled to Sepharose beads. Thus, a rabbit model was developed in which blood was allowed to clot around DD-Sepharose beads introduced into the jugular vein. Gamma camera imaging showed that intact 131I-labelled DD-3B6/22 localised to these clots within 24 h. Uptake at this time was 0.202%±0.012% injected dose per gram (%ID/g) compared with 0.086±0.018%ID/g after injection of control antibody. 131I-labelled F(ab')2 fragments of DD-3B6/22 allowed earlier scintigraphic detection of the clot which was evident 4 h after injection. Uptake in the clot at 24 h was 0.154±0.038% ID/g compared with 0.109±0.027% ID/g for a control F(ab')2. As antigen levels in the clot are estimated to be less than 300 μg DD, thus representing a very small human clot, the DD-3B6/22 Mab would appear to have a good potential for the sensitive detection of thrombi in a clinical setting. (orig.)

  12. Comparison of 131I- and 90Y-labeled monoclonal antibody 17-1A for treatment of human colon cancer xenografts

    The choice of radionuclide remains an important question in clinical radioimmunotherapy. Therefore, a study was initiated, using an in vivo model system, to assess the relative merits of 131I- and 90Y-labeled 17-1A monoclonal antibody as therapeutic agents in the treatment of colon cancer. 131I- and 90Y-labeled 17-1A were assessed in animal therapy trials using athymic nude mice bearing LS174T human colon cancer xenografts. 131I-labeled 17-1A decreased tumor growth in a dose-dependent fashion without lethality. In contrast, the doses of 90Y-labeled 17-1A which were required to produce a significant increase in tumor doubling time also caused marked toxicity. Although similar tumor growth inhibition was produced by 250 μCi 90Y- and 150 μCi 131I-labeled 17-1A, Medical Internal Radiation Dose calculations based on biodistribution data estimated that the dose delivered by 90Y was greater than that delivered by 131I. To investigate this discrepancy, 3-dimensional dose distributions within LS174T tumors were assessed using autoradiography and 3-dimensional calculational techniques. It was found that a greater fraction of the dose was deposited in the tumor after treatment with 131I- compared to 90Y-labeled 17-1A. When the Medical Internal Radiation Dose calculations were adjusted using the 3-dimensional dose distributions, 250 μCi of 90Y- and 150 μCi of 131I-labeled 17-1A were found to deliver similar tumor doses. These studies suggest that 131I-labeled 17-1A is superior to 90Y-labeled 17-1A, since 131I-labeled antibody produced less hematological and animal toxicity and was more effective at inhibiting LS174T tumor growth than 90Y-labeled antibody across the range of radionuclide doses tested. Furthermore, they suggest that it will be necessary to perform 3-dimensional dose calculations. 33 refs., 7 figs., 4 tabs

  13. Tumor necrosis treatment of ME-180 human cervical carcinoma model with 131I-labeled TNT-1 monoclonal antibody

    In contrast to normal tissues, many malignant tumors contain a high proportion of dead and dying cells. The loss of membrane integrity that accompanies cellular degeneration permits macromolecules, including antibodies, to freely enter the cell cytoplasm. Based upon these observations, it was hypothesized that monoclonal antibodies to intracellular antigens, which are integral structural components and are retained by degenerating cells, may be used to target a wide range of human malignancies. Previous studies by our laboratory utilizing these principles have demonstrated the feasibility of imaging four different histological types of human cancer in a nude mouse model, using monoclonal antibodies directed against insoluble intranuclear antigens. The present study describes the application of this approach, designated tumor necrosis treatment, for the radioimmunotherapy of transplantable ME-180 human cervical carcinomas in the nude mouse. Groups of tumor-bearing nude mice received three weekly treatments of 150 or 300 microCi of 131I-labeled experimental (TNT-1) or control (Lym-1) monoclonal antibodies. Detailed biodistribution data, dosimetric evaluations, and therapeutic results are presented to demonstrate the effective and preferential targeting of 131I-labeled TNT-1 monoclonal antibody within the tumor. In the experimental groups, the dose delivered to the tumor was sufficient to induce clinical regressions in 88% of treated animals, without evidence of toxicity to normal tissues. Complete regressions were obtained in 25% of the mice treated with high dose TNT-1. Microscopic examination of the implantation sites of these mice demonstrated the presence of acute radiation damage and residual keratin-positive tumor cells showing marked evidence of degeneration

  14. Study of labeling, biodistribution and scintilographic images in dog of the 15-p- iodophenyl pentadecanoic acid labeling with 131I

    The myocardium scintigraphy obtained after a radioactive tracer administration is a way to identify and quantify ischemic or infarct areas. The acid 15-p-iodophenyl pentadecanoic is marked with 131I (IPPA - 131I), through the isotopic exchange methodology in copper sulfate and ascorbic acid presence. The radiochemical purity will be evaluated by high performance liquid chromatography (HPLC) and rising chromatography in paper. The optimization of the mark conditions was done by varying time and marking temperatures where it was shown considerable mark revenue with high radiochemical purity at 120 deg C in 30 minutes. The marked mixture stays stable up the seventh day after marking. In the biological distribution studies is observed that right after the intravenous administration of the IPPA - 131I it is achieved a considerable capitation by the cardiac muscle. The radiopharmaceutical displays a fast blood metabolizing. The scintigraphy images obtained in dogs indicates that there is a stay in heart, allowing the identification of the cardiac muscle. (author)

  15. Pharmacokinetics of 131I-labeled-metuximab and transarterial chemoembolization for treatment of hepatocellular carcinoma

    Objective: To study the pharmacokinetics of 131I-Metuximab injection (Licartin) combined with transarterial chemoembolization (TACE) for treatment of hepatocellular carcinoma (HCC). Methods: Licartin (27.75 MBq/kg) and the mixture of anticancer drug and Lipiodol were sequentially administered with interval of 20 minutes to 15 patients with HCC via a transfemoral catheter. After the Licartin was administrated, the pharmacokinetic and biodistribution data were evaluated through venous blood samples, urine collections,and 4 γ-scintigraphies (SPECT) over 7 days. The pharmacokinetic parameters were determined from integration of the blood radioactivity-time curves using the SPSS 12.0 software. The tumor-no-tumor ratio (T/NT) was calculated by ROI. Absorbed doses in organ were estimated according to the medical internal radiation dose formalism. The biodistribution of licartin within patient's body at different time points was compared for various organs using analysis of variance for repeated measures, as well as the T/NT ratio. Results: The blood radioactivity-time curves followed the dynamics two-compartment model, with the major pharmacokinetic parameters including t(1/2) α (1.96 ± 1.65) h, and t1/2 α (19.07 ± 5.91) h, and t1/2 β (57.09 β 10.92) h, and Cmax 2.113 x 109min-1 · L-1, and AUC0-∞ 1.302 x 1011 h · min-1 · L-1, respectively. The accumulated urine radioactivity was 52.2% of administrated dosage during 144 h after administration. There were statistical significant difference of biodistribution of licartin and T/NT ratio between organs at different time points (F=6.583, P<0.01 and F=3.546, P<0.01). SPECT scans showed the significant accumulation of the radioconjugate in liver tumor and faint uptake in other organs for 14 days. Tumor-to-liver ratio decreased from 2.88 ± 1.02 at 3 h to 1.64 ± 0.40 at 168 h (n=7). Organ absorbed dose was (3.19 ± 1.01) Gy in liver (n=12) and (0.55 ± 0.09) Gy in red marrow (n=7). Conclusion: Licartin combined with

  16. Biological distribution of 131I-labeled anti-nucleus antigen monoclonal antibody chTNT in patients with pulmonary metastases from differentiated thyroid carcinoma

    MA Qingjie; GAO Shi; ZHAO Jie; WEN Qiang; BAI Lin; ZHANG Haoran; ZHAO Guoqing

    2008-01-01

    This work is to study the in vivo biological distribution of 131I-labeled mouse/human chimeric monoclonal antibody (131I-chTNT) in patients with pulmonary metastases from differentiated thyroid carcinoma.Ten patients with differentiated thyroid carcinoma were injected intravenously with a single dose of 131I-chTNT (5 MBq.kg-1 body weight).Radioactivity of blood and urine samples was measured at different time points.The in vivo stability and the metabolic status of 131I-chTNT were detected with supersaturated trichloroacetic acid.Continuous imaging was performed to outline the region of interest (ROD and estimate the intake level on the whole body,major organs and tumor lesions at different time points.The serum time-radioactivity curve of 131I-ehTNT accorded with the two-compartment model after a single intravenous injection:T1/2(h)=65.28±14.83,AUC0-t(MBq.h.mL-1)=8.93±1.32,AUC0-∞(MBq-h-mL-1)=10.58±2.19,and CL(mL.min-1.kg-1)=1635±359.The time-radioactivity percentage curve of 131I-chTNT urine excretion accorded with the one-compartment model after a single intravenous injection:T1/2(h)=99±10,and accumulative (31±9) % radioactivity of the injected dose was excreted in urine in one week.The percentages of serum 131I-ehTNT in radioactive components at 24,48 and 72 h were over 95% and it was still (88±7)% at 168 h.As for chemical composition of radioactive substances in urine,radioactivity in urine samples originated from free 131I by 100%.Radioactivity of 131I-chTNT after intravenous administration was mainly concentrated in the lung and liver,least in the brain.Radioactivity of tumor tissues reached the maximum at 24 h and the tumor/normal tissue (T/N) ratio reached the maximum (1.28~3.83) during 3~7 d.The characteristics of in vivo biological distribution of 131I-chTNT in patients with pulmonary metastases from differentiated thyroid carcinoma are favorable for its therapeutic application for the metastasis tumors.

  17. Biological distribution of 131I-labeled anti-nucleus antigen monoclonal antibody chTNT in patients with pulmonary metastases from differentiated thyroid carcinoma

    This work is to study the in vivo biological distribution of 131I-labeled mouse/human chimeric monoclonal antibody (131I-chTNT) in patients with pulmonary metastases from differentiated thyroid carcinoma. Ten patients with differentiated thyroid carcinoma were injected intravenously with a single dose of 131I-chTNT (5 MBq·kg-1 body weight). Radioactivity of blood and urine samples was measured at different time points. The in vivo stability and the metabolic status of 131I-chTNT were detected with supersaturated trichloroacetic acid. Continuous imaging was performed to outline the region of interest (ROI) and estimate the intake level on the whole body, major organs and tumor lesions at different time points. The serum time-radioactivity curve of 131I-chTNT accorded with the two-compartment model after a single intravenous injection: T1/2(h)=65.28±14.83, AUC0-t(MBq·h·mL-1)=8.93±1.32, AUC0-∞(MBq·h·mL-1)=10.58±2.19, and CL(mL·min-1·kg-1)=1635±359. The time-radioactivity percentage curve of 131I-chTNT urine excretion accorded with the one-compartment model after a single intravenous injection: T1/2(h)=99±10, and accumulative (31±9)% radioactivity of the injected dose was excreted in urine in one week. The percentages of serum 131I-chTNT in radioactive components at 24, 48 and 72 h were over 95% and it was still (88±7)% at 168 h. As for chemical composition of radioactive substances in urine, radioactivity in urine samples originated from free 131I by 100%. Radioactivity of 131I-chTNT after intravenous administration was mainly concentrated in the lung and liver, least in the brain. Radioactivity of tumor tissues reached the maximum at 24 h and the tumor/normal tissue (T/N) ratio reached the maximum (1.28-3.83) during 3-7 d. The characteristics of in vivo biological distribution of 131I-chTNT in patients with pulmonary metastases from differentiated thyroid carcinoma are favorable for its therapeutic application for the metastasis tumors. (authors)

  18. [131I]FIAU labeling of genetically transduced, tumor-reactive lymphocytes: cell-level dosimetry and dose-dependent toxicity

    Donor T cells have been shown to be reactive against and effective in adoptive immunotherapy of Epstein-Barr virus (EBV) lymphomas which develop in some leukemia patients post marrow transplantation. These T cells may be genetically modified by incorporation of a replication-incompetent viral vector (NIT) encoding both an inactive mutant nerve growth factor receptor (LNGFR), as an immunoselectable surface marker, and a herpes simplex virus thymidine kinase (HSV-TK), rendering the cells sensitive to ganciclovir. The current studies are based on the selective HSV-TK-catalyzed trapping (phosphorylation) of the thymidine analog [131I]-2'-fluoro-2'-deoxy-1-β-D-arabinofuransyl-5-iodo-uracil (FIAU) as a means of stably labeling such T cells for in vivo trafficking (including tumor targeting) studies. Because of the radiosensitivity of lymphocytes and the potentially high absorbed dose to the nucleus from intracellular 131I (even at tracer levels), the nucleus absorbed dose (Dn) and dose-dependent immune functionality were evaluated for NIT + T cells labeled ex vivo in [131I ]FIAU-containing medium. Based on in vitro kinetic studies of [131I ]FIAU uptake by NIT + T cells, Dn was calculated using an adaptation of the MIRD formalism and the recently published MIRD cellular S factors. Immune cytotoxicity of [131I ]FIAU-labeled cells was assayed against 51Cr-labeled target cells [B-lymphoblastoid cells (BLCLs) ] in a standard 4-h release assay. At median nuclear absorbed doses up to 830 cGy, a 51Cr-release assay against BLCLs showed no loss of immune cytotoxicity, thus demonstrating the functional integrity of genetically transduced, tumor-reactive T cells labeled at this dose level for in vivo cell trafficking and tumor targeting studies. (orig.)

  19. Survival in patients with hepatocellular carcinoma treated with intra-arterial {sup 131}I labelled lipiodol.

    Butler, S.P.; Morris, D.L.; Ring, M.T.; King, J.; Parks, S.L.; Glenn, D.W. [St George Hospital, Kogarah, NSW, (Australia). Department of Nuclear Medicine

    1997-09-01

    Full text: The prognosis of untreated hepatocellular carcinoma (HCC) is dismal with a median survival of less than two months having been reported. {sup 131}l labelled Lipiodol as a treatment for hepatocellular carcinoma (HCC) has been shown to be as efficacious as intraarterial chemotherapy but with less toxicity than chemotherapy. 23 patients (19 men and four women, mean age 69 years, range 28 to 80 years) with unresectable Okuda Stage I (n = 23) or 11 (n = 2) HCC were treated over a three-year period. All patients had biopsy proved HCC and had not received any prior therapy. Before therapy, all patients underwent CT scans of abdomen and thorax and scintigraphic bone scans to exclude extrahepatic disease. Further, CT scanning of the liver was performed following the hepatic artery injection of unlabelled Lipiodol to ensure that the HCC was Lipiodol avid. 1 GBq of {sup 131}l labelled Lipiodol was injected into the hepatic artery followed by CT liver scanning at day 1 and day 60 to calculate tumour response. Whole body scintigraphic scanning was performed on days 1 and 21 for dosimetry calculations. Ten patients had a second dose of {sup 131}l Lipiodol due either increasing serum alpha feto-protein levels and/or tumour progression on CT scanning. Minimal toxicity was seen with this dose regime. Survival time was estimated from the time of treatment by the Kaplan-Meier method. For Okuda I, the median survival length was 12 months with actuarial survival rates of 91 per cent, 65 per cent, 59 per cent and 20 per cent at 3,6,9,12 and 24 months respectively. All Okuda II patients died within five months. Iodine-131 Lipiodol therapy is well tolerated and may prolong survival in certain HCC patients.

  20. Quantitative uptake studies of 131I-labeled (E)-5-(2-iodovinyl)-2'-deoxyuridine in herpes simplex virus-infected cells in vitro

    We have synthesized a 131I-radiolabeled antiviral compound (E)-5-(2-iodovinyl)-2'-deoxyuridine (IVdU) and shown that this agent was selectively trapped within rabbit kidney cells, infected in vitro by thymidine kinase-positive (TK+) herpes simplex virus (HSV). The uptake of 131I-labeled IVdU was specific, as it was not concentrated within either HSV (TK-) or mock-infected cells. In certain conditions, over 40% of the radiolabel was selectively trapped within HSV (TK+)-infected cells. This was a 20- to 30-fold increase over the uptake of 131I-labeled IVdU by HSV (TK-) or mock-infected cells. The uptake of 131I-labeled IVdU varied directly with (i) the dose of the virus used to infect the rabbit kidney cells; (ii) the concentration of radiolabeled IVdU added to the system; and (iii) the time of exposure of IVdU to infected cells. The ability of this agent to be trapped within HSV (TK+)-infected cells merits further evaluation in animal models as it has potential as a noninvasive, herpes-specific diagnostic test, in particular for HSV encephalitis

  1. Comparative Study of Regional Lung Function With Intravenous Injection of 131I-Labelled Macroaggregated Albumin and 133Xe

    In each of 22 patients with known or suspected lung disease regional lung perfusion was assessed by measuring the radioactivity over the lower and upper part of each lung after intravenous injection of 133Xe and by scanning after intravenous injection of macroaggregated serum albumin labelled with 131I. The aim of the investigation was to decide which of the two methods was best suited as a clinical routine procedure in cases where information about regional lung function was required, e.g. in patients in whom lung surgery was considered. Direct comparison of results was possible only for lung perfusion. The xenon technique, but not the macroaggregated serum albumin technique, measures ventilation in addition. There was good agreement between the two methods in those instances where the perfusion ratio, left lung/(left lung+ right lung), was normal, i. e. near 0.5. On the other hand, there were discrepancies in patients with great difference between the perfusion of the two lungs. From the present limited material it is concluded that scanning after injection of macroaggregates is the method to be preferred in hospitals which have facilities for scintigraphy. Information on ventilation is not obtained by this method, but is probably often dispensable. (author)

  2. Targeting cancer stem cells with an 131I-labeled anti-AC133 monoclonal antibody in human colorectal cancer xenografts

    Introduction: Cancer stem cells (CSCs) are a subpopulation within a tumor, which possesses the characteristics of self-renewal, differentiation, tumorigenicity, and drug resistance. The aim of this study was to target the colorectal CSC marker CD133 with an131I-labeled specific monoclonal antibody (AC133 mAb) in a nude mouse xenograft model. Methods: Colorectal adenocarcinoma cells (LoVo cell line) were separated into CD133(+) and CD133(−) cells by magnetic activated cell sorting. CD133(+), CD133(−), and unsorted LoVo cells were cultured and then implanted subcutaneously into the lower limbs of nude mice (n = 5). AC133 mAb was labeled with 131I by the iodogen method. Results: The radiolabeled compound, 131I-AC133 mAb, showed high stability, specificity, and immunoactivity in vitro. Obvious accumulation of 131I-AC133 mAb was seen in nude mice bearing xenografts of CD133(+) and unsorted LoVo cells, but no uptake was found in mice bearing CD133(−) xenografts or specifically blocked xenografts. Biodistribution analysis showed that the tumor uptake of 131I-AC133 mAb was 6.97 ± 1.40, 1.35 ± 0.48, 6.12 ± 1.91, and 1.61 ± 0.44% ID/g (n = 4) at day 7 after injection of 131I-AC133 mAb in CD133(+), CD133(−), unsorted LoVo cell and specifically blocked xenografts, respectively. The results of immunofluorescence, autoradiography, and western blotting further verified the specific binding of 131I-AC133 mAb to CD133(+) tumors. Conclusions: This study demonstrates the possibility of targeting CSCs with a radiolabeled AC133 mAb in colorectal cancer xenografts based on in vitro, ex vivo, and in vivo experiments. Our findings suggest a new method for imaging CSCs non-invasively

  3. Establishment of 131I, 99mTc Labeling Methods to In-house Anti-CEA Antibodies and Evaluation of the Immunological Characteristics

    Cancer cells have several tumor-associated antigens on the cell surfaces, and antibodies against these antigens have been developed by many investigators. Radiolabeled antibodies have been used as new methods to diagnose and treat malignant tumors. Especially anti-carcinoembryonic antigen (CEA) is the most popular antibody for these purposes. In this investigation, we tried to label 131I and 99mTc to anti-CEA monoclonal antibodies which were developed in the Seoul National University College of Medicine. We found CEA-79 and CEA-92 antibodies had the better immunological characteristics among 8 anti-CEA monoclonal antibodies. And radioiodination of CEA-79 could be performed by chloramine-T method, while radioiodination of CEA-92 by iodogen method. To label these antibodies with 99mTc, we used pretargeting transchelation as direct labeling method. At first, 99mTc was bound to glucaric acid, and monoclonal antibody was reduced by β-mercaptoethanol. When these were incubated together, 99mTc bound to glucarate was switched to monoclonal antibody because of higher affinity. We established conditions of several steps in this method. Anti-CEA monoclonal antibodies labeled with 131I and 99mTc are expected to be used valuably in the detection and treatment of malignant tumors.

  4. Enzymatic synthesis of {sup 125/131}I labeled 8-hydroxyquinoline glucuronide and in vitro/in vivo evaluation of biological influence

    Yesilagac, Reyhan [Ege University, Institute of Nuclear Science, 35100 Bornova, Izmir (Turkey); Unak, Perihan, E-mail: perihan.unak@ege.edu.t [Ege University, Institute of Nuclear Science, 35100 Bornova, Izmir (Turkey); Medine, E. Ilker; Ichedef, Cigdem A. [Ege University, Institute of Nuclear Science, 35100 Bornova, Izmir (Turkey); Ertay, Turkan [Dokuz Eyluel University, Medical School, Department of Nuclear Medicine, Inciralti, Izmir (Turkey); Mueftueler, F.Z. Biber [Ege University, Institute of Nuclear Science, 35100 Bornova, Izmir (Turkey)

    2011-02-15

    8-Hydroxyquinoline (8-OHQ) is a long-known molecule which due to its metal-complexation ability is frequently used for analysis. It is also called oxine. Oxine and derivatives have been investigated to process antitumor and antimicrobial activities. 8-Hydroxyquinolyl-glucuronide (8-OHQ-Glu) was enzymatically synthesized using microsome preparates separated from Hutu-80 cells, labeled with {sup 125}I to perform a radionuclide labeled prodrug and investigated of its biological affinities on Hutu-80 (human duodenum intestinal adenocarcinoma), Caco-2 (human colorectal adenocarcinoma), Detroit 562 (human pharynx adenocarcinoma) cells and ACBRI 519 (primary human small intestine epithelial cells) in this work. UDP-glucuronyl transferase (UDPGT) rich microsome preparates, which are used for glucuronidation in enzymatic synthesis, were extracted from Hutu-80 cells. 8-OHQ-Glu components were labeled using iodogen method with {sup 125}I and {sup 131}I. Structural analyses were performed with LC/MS/MS, {sup 1}H NMR and {sup 13}C-MMR for identify and measure chemical constituents. Results confirmed expected molecular structure. 8-OHQ-Glu could successfully radioiodinated with {sup 125/131}I according to iodogen method. {sup 125}I-8-OHQ-glucuronide incorporated with human gastrointestinal cancer cells such as Detroit-562 (human pharynx adenocarcinoma) (12.6%), Caco-2 (human colorectal adenocarcinoma) (7.8%), Hutu- 80 (human duodenum intestinal adenocarcinoma) (9.5%) and ACBRI 519 (primary human small intestine epithelial cells) (6.40%). {sup 131}I-8-OHQ-Glu was tested in mice bearing subcutaneously implanted Caco-2 colorectal adenocarcinoma cells. The results demonstrated that radioiodinated 8-OHQ-Glu may be promising anticancer prodrug.

  5. Enzymatic synthesis of 125/131I labeled 8-hydroxyquinoline glucuronide and in vitro/in vivo evaluation of biological influence

    8-Hydroxyquinoline (8-OHQ) is a long-known molecule which due to its metal-complexation ability is frequently used for analysis. It is also called oxine. Oxine and derivatives have been investigated to process antitumor and antimicrobial activities. 8-Hydroxyquinolyl-glucuronide (8-OHQ-Glu) was enzymatically synthesized using microsome preparates separated from Hutu-80 cells, labeled with 125I to perform a radionuclide labeled prodrug and investigated of its biological affinities on Hutu-80 (human duodenum intestinal adenocarcinoma), Caco-2 (human colorectal adenocarcinoma), Detroit 562 (human pharynx adenocarcinoma) cells and ACBRI 519 (primary human small intestine epithelial cells) in this work. UDP-glucuronyl transferase (UDPGT) rich microsome preparates, which are used for glucuronidation in enzymatic synthesis, were extracted from Hutu-80 cells. 8-OHQ-Glu components were labeled using iodogen method with 125I and 131I. Structural analyses were performed with LC/MS/MS, 1H NMR and 13C-MMR for identify and measure chemical constituents. Results confirmed expected molecular structure. 8-OHQ-Glu could successfully radioiodinated with 125/131I according to iodogen method. 125I-8-OHQ-glucuronide incorporated with human gastrointestinal cancer cells such as Detroit-562 (human pharynx adenocarcinoma) (12.6%), Caco-2 (human colorectal adenocarcinoma) (7.8%), Hutu- 80 (human duodenum intestinal adenocarcinoma) (9.5%) and ACBRI 519 (primary human small intestine epithelial cells) (6.40%). 131I-8-OHQ-Glu was tested in mice bearing subcutaneously implanted Caco-2 colorectal adenocarcinoma cells. The results demonstrated that radioiodinated 8-OHQ-Glu may be promising anticancer prodrug.

  6. Indocyanine green labeled with /sup 123/I for dynamic studies of the hepato-biliary system. [/sup 131/I, /sup 125/I

    Lambrecht, R.M.; Ansari, A.N.; Wolf, A.P.; Atkins, H.L.

    1975-01-01

    This report summarizes the results to develop an iodine-123 labeled agent for dynamic studies of the hepato-biliary system. Iodine-123 is an ideal nuclide for radiopharmaceuticals, because of its short half-life (T/sub /sup 1///sub 2// = 13.3 hr); its decay with a high abundance (83%) of 159 keV photons; and the reduced patient radiation exposure (a factor of 100 less than iodine-131). Indocyanine green, a tricarbanocyanine dye, was introduced by Heseltine and co-workers in 1956, has several characteristics which suggested that iodine-123 labeled ICG might be potentially useful for hepatic functional evaluation. The plasma clearance and biliary excretion kinetics of /sup 123/I-ICG (in dogs) will be compared to /sup 131/I-rose bengal and bromosulphalein labeled with iodine-125.

  7. Second antibody clearance of /sup 131/I-labeled anti-carcinoembryonic antigen for improved tumor imaging

    The authors have investigated the use of a second antibody (SA) directed against the radiolabeled primary anti-tumor antibody (PA) to enhance the clearance rate of the PA from the circulation and nontarget tissues. Administration of 50 or 250 μg of anti-goat IgG (SA) hr after the administration of 10 μg of /sup 131/I-goat anti-carcinoembryonic antigen antibody (PA) to hamsters bearing human colonic tumor xenografts resulted in a 5-fold reduction in the level of circulating PA after 4 hr in comparison to the control group only given /sup 131/I-PA. The percentage of PA in the blood decreased rapidly over 72 hr in animals given 250 μg of the SA, but at 50 μg of SA the level of activity in the blood after 24 hr was similar to the control. Tumor accretion was identical after 4 hr, but after 24 hr the animals given 250 μg of SA had 2-3 fold less PA in the tumor than either the control group or the 50 μg dose of SA. Tumor/nontumor ratios for all major organs but the spleen improved 6-8 fold within 48 hr after injection of 250 μg of the SA with tumor/blood ratios as high as 40:1. A SA dose of 50 μg resulted in a significantly higher tumor/blood ratio after only 4 hr; tumor/nontumor ratios at later times were similar to the control group. Tumors located in the hind legs were visible in all groups by imaging 24 hr after injection of the SA, but only the 250 μg dose of SA showed a significant reduction in total body activity. These results suggest that the SA approach may be used to reduce the total background radioactivity while maintaining tumor accretion of /sup 131/I-PA to allow for selective tumor imaging

  8. Localization of tumors in vivo by scintigraphic identification of Clostridium butyricum using 131I-labelled antibodies and F(ab')2-antibody fragments

    Tumor-bearing mice injected with clostridial spores show enrichment and germination of the spores within the tumor. 131I-labelled anti-Clostridium-antibodies and anti-Clostridium-F(ab')2-fragments were used for a possible localization of tumors in vivo by scintiscanning. The application of the antibody revealed increased radioactivity in the tumors of mice pretreated with spores as well as in animals without pretreatment. In using F(ab')2-fragments instead of total antibody neither the apparently unspecific increase of radioactivity in not pretreated mice nor the specific fixation of labelled F(ab')2-fragments to clostridial rods in the tumors of pretreated animals could be demonstrated. The results are discussed with respect to further investigation

  9. Radioimmunoimaging of human colon carcinoma grafted into nude mice using 131I-labeled monoclonal anti-CEA antibody (C50)

    131I-labeled monoclonal anti-CEA antibody C50 was injected intraperitoneally into nude mice bearing human colon carcinoma xenografts for tumor localization and radioimmunoimaging studies. Radioimmunoimaging and biodistribution was performed at the 1st, 2nd, 3th, 4th and 6th day after injection and transplanted tumors were visualized in 24 hr by SPECT. Satisfactory tumor imaging was obtained at 48 hr after injection and at the 6th day T/NT (tumor/colon) reached 10.40 +- 0.69. These in vivo studies demonstrate the specificity of McAb C50 and indicate that it may be used for clinical diagnosis and targeting treatment of human colon carcinoma

  10. /sup 131/I-labelling of frozen ram sperma and distribution pattern of sperma in the genital tract of sheep, following artificial insemination

    Brueckner, G. (Karl-Marx-Universitaet, Leipzig (German Democratic Republic). Sektion Tierproduktion und Veterinaermedizin); Kaempfer, I. (Karl-Marx-Universitaet, Leipzig (German Democratic Republic). Radiologische Klinik)

    1983-04-01

    The method of /sup 131/I-labelling of ram sperma was applied to frozen sperma and used in experimental insemination to test the spermatozoa for both migratory capacity and distribution in the genital tract of sheep. The penetration rate of frozen sperma into the upper genital tract was found to be slower than that of native sperma. The two sperma variants were compared also for migratory performance, and the distance travelled into the upper genital tract by frozen sperma one hour after insemination amounted to only 40 per cent of the distance covered by native sperma in the same period of time. The ratio of native to frozen sperma in the tubal region was 100 : 75.3. Sperma population in the tubal region was higher than that in the uterus, two hours after insemination, which seems to indicate a certain reservoir function. Pronounced asymmetrical distribution patterns in the oviducts were equally recordable from native and frozen sperma.

  11. Effect of 22-hours liquid preservation on migration of /sup 131/I-labelled sperma in the genital tract of ewes, following artificial insemination

    Brueckner, G. (Karl-Marx-Universitaet, Leipzig (German Democratic Republic). Sektion Tierproduktion und Veterinaermedizin); Kaempfer, I. (Karl-Marx-Universitaet, Leipzig (German Democratic Republic). Radiologische Klinik)

    1984-02-15

    Comparative studies on migration and distribution of /sup 131/I-labelled ram sperma in the genital tract of estrus-synchronized ewes at different points of time after insemination (40, 120, 180, and 240 minutes). The sperma had been preserved in liquid condition for 4 or 22 hours. The results suggested that up to 2 hours after insemination the migration of sperma preserved 22 hours was clearly slower (lower transcervical passage and smaller amount in oviducts) than that of sperma preserved 4 hours. These differences were significant 2 hours after insemination and were reduced, with mutual adjustment of distribution patterns, between 2 and 4 hours after insemination. The pattern of migration was affected by certain physiological factors. Obviously the optimum timing of insemination is of great importance in applying 22 hours preserved ram sperma.

  12. Genotoxic evaluation of [DOTA,Tyr3]octreotate labeled with 131I and 177Lu in human peripheral lymphocytes in vitro by micronucleus assay

    The radiolabeled receptor-binding peptides have being used for cancer diagnosis and therapy. The octreotate, a somatostatin analogue peptide, bound to various tumors expressing sst receptors (thyroid, pancreas, prostrate, melanoma and lymphomas). The amount and the type of receptors for somatostatin influence the tissue uptake. The [DOTA, Tyr3]octreotate has been used because of its high affinity to somatostatin subtype receptors sstr2 and sstr5. The pharmacokinetic study showed that the blood clearance is rapid and only 9% of the intravenous injected activity remains in human blood after one hour. The aim of this study was to evaluate the cytogenetic effect of radiolabeled [DOTA, Tyr3]octreotate in blood cells in vitro, using the cytokinesis-block micronucleus (MN) assay. This technique allows evaluating the mutagenic effects of both endogenous and exogenous agents at chromosome level. Blood samples of healthy donors were collected in heparinized syringes and exposed to different activities of [DOTA, Tyr3]octreotate labeled with with 131I (n=3) and 177Lu (n=3), where radioactive concentration ranged from 600 to 5600 kBq/mL, corresponding to an injected activity of 3.1 to 28.9 GBq in a reference man of 70 kg weight. 131I and 177Lu are beta- and gamma-emitters. After one-hour exposition to radiopharmaceuticals at 37 deg C, the cells were washed with culture medium for removing the non internalised octreotate and cultivated for 72 hours, according to criteria adopted by the IAEA. The results showed a positive correlation between radioactive concentrations (X) and the frequency of binucleated cells with micronuclei (Y) (P131I-DOTA, Tyr3]octreotate was Y = (1.634 ± 0.236) + (0.912 ± 0.137) 10-3 X and for [177Lu-DOTA, Tyr3]octreotate was Y = (1.715 ± 0.342) + (0.743 ± 0.135) 10-3 X. The non labeled molecule, [DOTA, Tyr3]octreotate, has no influence in the induction of cytogenetic damage. The micronucleus assay with rat pancreatic tumor cells (AR42J) that express the

  13. 多巴胺D2受体显像剂Epidepride的合成及其131I标记%Synthesis and 131I Labeling of Epidepride as a Dopamine D2 Receptor Imaging Agent

    杨敏; 胡名扬; 裴著果; 王博诚; 周杏琴

    2001-01-01

    以3-甲氧基水杨酸为原料合成了Epidepride[S-(-)-N-[(1-乙基-2-吡咯烷基)甲基]-5-碘-2,3-二甲氧基苯甲酰胺]及其标记前体(S-(-)-5-(三正丁基锡)-N-[(1-乙基-2-吡咯烷基)甲基]2,3-二甲氧基苯甲酰胺),并采用双氧水法对标记前体进行131I标记,获得131I-epidepride,标记率和放化纯度均大于95%。131I-epidepride溶液体外稳定性好,4 ℃放置15 d放化纯度仍大于90%。131I-epidepride与D2受体亲和力高,大鼠脑内纹状体与小脑的摄取比在320 min时高达237;在脑内纹状体的吸收可被Spiperone完全阻断。因此,131I-epidepride有望成为多巴胺D2受体SPECT显像剂。%S-(-)-N-[(1-ethyl-2-pyrrolidinyl)methyl]-5-iodo-2,3-dimethoxybenzamide (Epidepride) and its iodine labeling precursor S-(-)-N-[(1-Ethyl-2-pyrrolidinyl)methyl]-5-tributyltin-2,3-dimethoxybenzamide are synthesized from 3-methoxy salicylic acid. The labeling precursor is labeled with 131I by hydrogen peroxide method, and 131I-epidepride is gained, its radiolabelling yield(RLY) and the radiochemical purity(RCP)are all over 95%. The RCP of 131I-epidepride is over 90% under 4 ℃ after 15 days. 131I-epidepride has high affinity to dopamine D2 receptor. The striatal uptake can be blocked completely by spiperone. The striatum and cerebellum uptake ratio can reach 237 at 320 min in rats.The results show that 131I-epidepride may be used as a dopamine D2 receptor imaging agent for SPECT.

  14. {sup 177}Lu- labeled MOv18 as compared to {sup 131}I- or {sup 90}Y-labeled MOv18 has the better therapeutic effect in eradication of alpha folate receptor-expressing tumor xenografts

    Zacchetti, Alberto [Unit of Molecular Therapies, Department of Experimental Oncology and Laboratories, Fondazione IRCCS Istituto Nazionale dei Tumori, Milan 20133 (Italy); Coliva, Angela [Department of Imaging and Nuclear Medicine, Fondazione IRCCS Istituto Nazionale dei Tumori, Milan 20133 (Italy); Luison, Elena [Unit of Molecular Therapies, Department of Experimental Oncology and Laboratories, Fondazione IRCCS Istituto Nazionale dei Tumori, Milan 20133 (Italy); Seregni, Ettore; Bombardieri, Emilio [Department of Imaging and Nuclear Medicine, Fondazione IRCCS Istituto Nazionale dei Tumori, Milan 20133 (Italy); Giussani, Augusto [Helmholtz Zentrum Muenchen, German Research Center for Environmental Health, Neuherberg (Germany); Figini, Mariangela [Unit of Molecular Therapies, Department of Experimental Oncology and Laboratories, Fondazione IRCCS Istituto Nazionale dei Tumori, Milan 20133 (Italy); Canevari, Silvana [Unit of Molecular Therapies, Department of Experimental Oncology and Laboratories, Fondazione IRCCS Istituto Nazionale dei Tumori, Milan 20133 (Italy)], E-mail: silvana.canevari@istitutotumori.mi.it

    2009-10-15

    Introduction: The mouse monoclonal antibody MOv18, directed against the {alpha}-isoform of folate receptor (FR), was investigated to identify the optimal radioconjugate for radioimmunotherapy of minimal residual disease in ovarian cancer. Methods: Pharmacokinetics, biodistribution, long-term therapeutic efficacy and toxicity of MOv18, labeled with the beta-emitters {sup 131}I, {sup 90}Y and {sup 177}Lu, were compared in a xenografted mouse model, composed by two cell lines, A431FR and A431MK, differing only for FR expression. Results: A shorter blood clearance and a higher tumor uptake were observed for {sup 90}Y- and {sup 177}Lu- compared to {sup 131}I-MOv18, and a shorter blood pharmacokinetics was recorded in A431FR-bearing animals. At equitoxic maximum tolerable doses, the general irradiation by {sup 131}I- and {sup 90}Y-MOv18 gives rise to strong targeted effects on A431FR and nontargeted effects on A431MK tumors, while {sup 177}Lu-MOv18 was able to eradicate small size tumor masses expressing the antigen of interest exerting only mild non-targeted effects. Conclusion: {sup 177}Lu-MOv18 at the maximal tolerated dose is the immunoradioconjugate with the best therapeutic window in experimental conditions of small tumor volume.

  15. 177Lu- labeled MOv18 as compared to 131I- or 90Y-labeled MOv18 has the better therapeutic effect in eradication of alpha folate receptor-expressing tumor xenografts

    Introduction: The mouse monoclonal antibody MOv18, directed against the α-isoform of folate receptor (FR), was investigated to identify the optimal radioconjugate for radioimmunotherapy of minimal residual disease in ovarian cancer. Methods: Pharmacokinetics, biodistribution, long-term therapeutic efficacy and toxicity of MOv18, labeled with the beta-emitters 131I, 90Y and 177Lu, were compared in a xenografted mouse model, composed by two cell lines, A431FR and A431MK, differing only for FR expression. Results: A shorter blood clearance and a higher tumor uptake were observed for 90Y- and 177Lu- compared to 131I-MOv18, and a shorter blood pharmacokinetics was recorded in A431FR-bearing animals. At equitoxic maximum tolerable doses, the general irradiation by 131I- and 90Y-MOv18 gives rise to strong targeted effects on A431FR and nontargeted effects on A431MK tumors, while 177Lu-MOv18 was able to eradicate small size tumor masses expressing the antigen of interest exerting only mild non-targeted effects. Conclusion: 177Lu-MOv18 at the maximal tolerated dose is the immunoradioconjugate with the best therapeutic window in experimental conditions of small tumor volume.

  16. Preparation of {sup 105}Rh labeled monoclonal antibody (MAb B72.3) using aminobenzylpropyleneamineoxime as the bifunctional chelating agent; comparison to {sup 131}I labeled MAb B72.3

    Venkatesh, M. [Bhabha Atomic Research Centre, Bombay (India). Isotope Div.; Schlemper, E.O.; Jurisson, S.S. [Missouri Univ., Columbia, MO (United States). Dept. of Chemistry; Ketring, A.R. [Missouri Univ. Research Reactor, Columbia, MO (United States); Volkert, W.A. [Missouri Univ., Columbia, MO (United States). Radiology Research; H.S. Truman Memorial VA Hospital, Columbia, MO (United States); Corlija, M. [H.S. Truman Memorial VA Hospital, Columbia, MO (United States)

    1999-07-01

    Monoclonal antibody(MAb) B72.3 was labeled with {sup 105}Rh using aminobenzylpropyleneamineoxime (PnAO-{phi}-NH{sub 2}) as the bifunctional chelating agent. {sup 105}Rh-PnAO-{phi}-NH{sub 2} was formed at {proportional{underscore}to} 80 C at pH 5-6 and purified by extraction into chloroform. The excess unreacted ligand was retained in the aqueous phase by addition of Cu{sup 2+} ions by forming a charged complex. The amine group on {sup 105}Rh complex was activated and conjugated with MAb at pH 8.5 {proportional{underscore}to}90% complexation and 40-60% conjugation were realised. Radiolabeled antibody was purified by gel filtration. B72.3 MAb was labeled with {sup 131}I and used for comparison of biodistribution in normal mice. (orig.)

  17. Labelling of Dotatate with 177Lu and 131I for diagnosis and targeted therapy: In vitro and In vivo comparative evaluation

    The studies focused on the radiolabelling of DOTA-Tyr3-TATE (DOTATATE) with 177Lu and 131I, on the biological behaviour of 177Lu-DOTATATE and 131IDOTATATE and on comparative evaluation of the results obtained to select an appropriate radiopeptide for potential application in somatostatin receptor radionuclide therapy. The radiopeptides were obtained with high purities and specific activities, but with different stabilities, with the 177Lu-DOTATATE being more stable than the 131IDOTATATE. The results of competition and saturation binding experiments using rat brain cortex membrane homogenates show a high in vitro affinity (IC50: 4.74nM, Kd: 142.8 for 177Lu-DOTATATE; IC50: 1.28nM, Kd: 157.6 for 131I-DOTATATE). The biodistribution of each radiopeptide as well as the competitive biodistribution of 177Lu- DOTATATE and 131I-DOTATATE in rats bearing HRS1 (Hepatom RS1, a hepatocolangiom carcinoma) tumours illustrate that 177Lu-DOTATATE is more stable and shows better tumour uptake than 131I-DOTATATE, and that the competitive localization index of 177Lu-DOTATATE is three times higher than that of 131I-DOTATATE. The flow cytometry measurements of the HRS1 tumour samples from rats treated with multiple doses of 177Lu-DOTATATE in combination with absorbed dose data show decreases of both the tumour cell proliferation index and DNA ploidy. These data indicate that 177Lu- DOTATATE is a good option for application in somatostatin receptor radionuclide therapy. (author)

  18. Addendum to report of the research co-ordination meeting on labelling techniques of biomolecules for targeted radiotherapy. Country report: Hungary. Preparation, quality control and animal testing of 125I and 131I labelled monoclonal antibody for radiotherapy

    Radiolabelled monoclonal antibodies (MoAbs) against tumour-associated antigens have been used to detect tumour deposits. Since gamma camera imaging of patients injected with radiolabelled MoAbs has demonstrated, selective tumour uptake of MoAbs, antibody-directed radiotherapy has gained greater interest. Prior to employing antibodies for radioimmunotherapy, their tumour and normal tissue uptake and pharmacokinetics as well as therapeutic efficacy in the animal tumour model must be determined. The therapeutic radiopharmaceuticals consist of two components the radionuclide (beta, alpha, Anger and conversion electron emitters) and the biological carrier (from peptide- to antibody). In the first step of our research program anti CEA MoAb inj. labelled with iodine-125 and 131I isotopes were used to study therapeutic efficacy in nude mice bearing human gastric adenocarcinoma xenografts

  19. Syntheses of several 99mTc and 131I labeled neoglycoalbumins and their differential uptake patterns in animal biodistribution experiments

    Several glycoconjugates, α-d-mannopyranosyl, β-l-fucopyranosyl, α-l-rhamnopyranosyl, β-d-glucopyranosyl and β-d-galactopyranosyl human serum albumin, were synthesized using C9-tether and radiolabeled with 99mTc and 131I. Both 99mTc and 131I radiolabeled neoglycoalbumins had considerable stability and exhibited similar biodistribution patterns within the experimental limits. The results of biodistribution studies can be explained from the in vitro observations that 99mTc-β-d-galactopyranosyl albumin binds to hepatic binding protein in liver in a dose-dependent fashion. The radiolabeled glycoalbumins derived from d-mannopyranose and l-fucopyranose also bind in a dose-dependent fashion to the receptors present in the liver sinusoidal cells and spleen macrophages. The β-d-glucopyranosyl and α-l-rhamnopyranosyl neoglycoalbumins accumulate nonspecifically in liver and spleen

  20. Hepatic artery injection of {sup 131}I-labelled metuximab combined with chemoembolization for intermediate hepatocellular carcinoma: a prospective nonrandomized study

    Wu, Lu; Yang, Ye-Fa; Ge, Nai-Jian; Shen, Shu-Qun; Liang, Jun [Second Military Medical University, The First Department of Interventional Radiology, Eastern Hepatobiliary Surgery Hospital, Shanghai (China); Wang, Yi [Second Military Medical University, The Second Department of Hepatic Surgery, Eastern Hepatobiliary Surgery Hospital, Shanghai (China); Zhou, Wei-Ping [Second Military Medical University, The Third Department of Hepatic Surgery, Eastern Hepatobiliary Surgery Hospital, Shanghai (China); Shen, Feng; Wu, Meng-Chao [Second Military Medical University, Eastern Hepatobiliary Surgery Hospital, Shanghai (China)

    2012-08-15

    Hepatocellular carcinoma (HCC) is the fifth and seventh most common cause of cancer in men and women, respectively. Transcatheter arterial chemoembolization (TACE) is the standardized therapy for the intermediate stage of HCC. However, the 3-year overall survival remains low (<30 %) in these patients. Thus, there is a critical need for the development of treatment modalities to improve the survival rate. This study aimed to evaluate whether the combination of {sup 131}I-metuximab with chemoembolization could improve treatment efficiency. Between January 2009 and January 2010, a prospective two-arm nonrandomized study was performed in patients with intermediate HCC. Of 138 patients, 68 (combination therapy group) received 132 courses of intraarterial {sup 131}I-metuximab injections combined with chemoembolization (mean 1.94 per patient, median 2, range 1-2), followed by 152 sessions of TACE (mean 2.24 per patient, median 2, range 0-4). The remaining 70 patients (monotherapy group) received 296 sessions of TACE (mean 4.23 per patient, median 4, range 1-7). The overall median survival times for the combination therapy group and the group treated only with TACE were 26.7 months (95 % CI 20.7-31.3 months) and 20.6 months (95 % CI 15.3-24.7 months), respectively. The combination therapy group had a significantly higher survival rate than the TACE-only group (P = 0.038). Age {>=}65 years, serum albumin {<=}35 g/l, and treatment category (combination therapy or TACE only) were independent prognostic factors for survival according to multivariate analysis. The combination of {sup 131}I-metuximab and chemoembolization extended survival in patients with intermediate HCC compared with TACE only, and was well tolerated by patients with Child-Pugh class A or B disease. This combination seems to be a promising treatment modality for patients with intermediate HCC. (orig.)

  1. The labelling of adriamycin-loaded human serum albumin immuno-nanoparticles led by monoclonal antibodies with 131I and its anti-hepatoma effect in vivo

    The pharmaceutics character, targeting to hepatoma and anticancer activity in nude mice of adriamycin-loaded human serum albumin immuno-nanoparticles (ADR-HSA-NP) against hepatoma led by anti-human hepatoma monoclonal antibodies HAb18 are studied. The results show that effective loaded drug dose of HAb18-ADR-HSA-NP is 1.44%, which is lower than ADR-HSA-NP (1.69%); HAb18-ADR-HSA-NP slowly releases drug ADR and its maximum releasing drug dose (41%) is obviously lower than ADR-HSA-NP (65%) (P 131I-HAb18-ADR-HSA-NP mainly accumulates in liver and its liver-taxis and stability are better than 131I-ADR-HSA-NP in nude mice by intravenous injection; HAb18-ADR-HSA-NP mainly accumulates in tumor and its accumulation amount of tumor is higher than ADR-HSA-NP (P < 0.05), and has obvious inhibiting cancer action and its inhibitory rate of cancer is also higher than ADR-HSA-NP (P < 0.05) by tumor injection. So, HAb18-ADR-HSA-NP can bind and inhibit hepatoma cell from growing in vivo

  2. Radiation dosimetry and first therapy results with a {sup 124}I/{sup 131}I-labeled small molecule (MIP-1095) targeting PSMA for prostate cancer therapy

    Zechmann, Christian M.; Afshar-Oromieh, Ali; Mier, Walter [University Hospital Heidelberg, Department of Nuclear Medicine, Heidelberg (Germany); Armor, Tom; Joyal, John [Molecular Insight Pharmaceuticals, Boston, MA (United States); Stubbs, James B. [Radiation Dosimetry Systems RDS, Inc., Apharetta, GA (United States); Hadaschik, Boris [University Hospital Heidelberg, Department of Urology, Heidelberg (Germany); Kopka, Klaus [Division Radiopharmaceutical Chemistry, DKFZ, Heidelberg (Germany); Debus, Juergen [University Hospital Heidelberg, Department of Radiation Oncology, Heidelberg (Germany); Babich, John W. [Molecular Insight Pharmaceuticals, Boston, MA (United States); Cornell University, Division of Radiopharmacy, Department of Radiology, New York, NY (United States); Haberkorn, Uwe [University Hospital Heidelberg, Department of Nuclear Medicine, Heidelberg (Germany); Clinical Cooperation Unit Nuclear Medicine, DKFZ, Heidelberg (Germany)

    2014-07-15

    Since the prostate-specific membrane antigen (PSMA) is frequently over-expressed in prostate cancer (PCa) several PSMA-targeting molecules are under development to detect and treat metastatic castration resistant prostate cancer (mCRPC). We investigated the tissue kinetics of a small molecule inhibitor of PSMA ((S)-2-(3-((S)-1-carboxy-5-(3-(4-[{sup 124}I]iodophenyl)ureido)pentyl)ureido) pentan edioicacid; MIP-1095) using PET/CT to estimate radiation dosimetry for the potential therapeutic use of {sup 131}I-MIP-1095 in men with mCRPC. We also report preliminary safety and efficacy of the first 28 consecutive patients treated under a compassionate-use protocol with a single cycle of {sup 131}I-MIP-1095. Sixteen patients with known prostate cancer underwent PET/CT imaging after i.v. administration of {sup 124}I-MIP-1095 (mean activity: 67.4 MBq). Each patient was scanned using PET/CT up to five times at 1, 4, 24, 48 and 72 h post injection. Volumes of interest were defined for tumor lesions and normal organs at each time point followed by dose calculations using the OLINDA/EXM software. Twenty-eight men with mCRPC were treated with a single cycle of {sup 131}I-MIP-1095 (mean activity: 4.8 GBq, range 2 to 7.2 GBq) and followed for safety and efficacy. Baseline and follow up examinations included a complete blood count, liver and kidney function tests, and measurement of serum PSA. I-124-MIP-1095 PET/CT images showed excellent tumor uptake and moderate uptake in liver, proximal intestine and within a few hours post-injection also in the kidneys. High uptake values were observed only in salivary and lacrimal glands. Dosimetry estimates for I-131-MIP-1095 revealed that the highest absorbed doses were delivered to the salivary glands (3.8 mSv/MBq), liver (1.7 mSv/MBq) and kidneys (1.4 mSv/MBq). The absorbed dose calculated for the red marrow was 0.37 mSv/MBq. PSA values decreased by >50 % in 60.7 % of the men treated. Of men with bone pain, 84.6 % showed complete or

  3. Comparison of 131I-TYR3-octreotate and 131I-DOTA-TYR3-octreotate: The effect of DOTA on pharmacokinetics and stability

    The authors compared the biodistribution, and in vivo and in vitro stabilities of 131I-Tyr3-octreotate and 131I-DOTA-Tyr3-octreotate. The peptides were radioiodinated by the chloramine T method and high radiochemical yields were obtained (greater than 97%). Both labelled compounds showed high stability when incubated in human plasma at 37 deg C. The 131I-Tyr3-octreotate showed significant hepatic uptake and biliary excretion. The biodistribution of 131I-DOTA-Tyr3-octreotate, however, can be compared with the distribution of radiometal labelled octreotide analogues. (author)

  4. 131I-chTNT-mediated radioimmunotherapy for non-uptaking 131I pulmonary metastases from differentiated thyroid carcinoma

    In this paper, the safety and efficacy of 131I-labeled mouse/human chimeric monoclonal antibody (131I-chTNT)-mediated radioimmunotherapy are evaluated because the patients have non-uptaking 131I pulmonary metastases from differentiated thyroid carcinoma (DTC). The 16 patients were injected intravenously by 29.6±3.7 MBq·kg-1 using 131I-chTNT. The chest computer tomography was performed before treatment, as well as 28 and 70 days after treatment. Responses and safety were assessed during the treatment. The results show that the 131I-chTNT infusion was well tolerated with the 12.5% complete response, 18.8% partial response, 25.0% progressive disease, and the 43.8% stable disease, indicating that most treatment-related adverse effects are mild transient and reversible. The 131I-chTNT is promising for patients with non-uptaking the 131I pulmonary metastases from DTC. (authors)

  5. Optimization of labelling conditions of 15-p-iodophenyl pentadecanoic acid with {sup 123}I and its pharmacokinetics evaluation; Otimizacao das condicoes de marcacao do acido 15-p-iodo fenil pentadecanoico com {sup 123/131} I e sua avaliacao farmacocinetica

    Oliveira, Ione Caselato; Colturato, Maria Tereza; Araujo, Elaine Bortoleti de; Barbosa, Marycel Figols de; Muramoto, Emiko; Pereira, Nilda Petrona Sosa de; Silva, Constanca Pagano Goncalves da; Almeida, Maria Aparecida T.M. de [Instituto de Pesquisas Energeticas e Nucleares (IPEN), Sao Paulo, SP (Brazil)

    1996-07-01

    The 15-p-iodo-phenyl pentadecanoic acid (IPPA) labelled with {sup 123} I is an important radiopharmaceutical for use in cardiology, due to its favorable physical characteristics and its labelling stability. The labelling procedure studies for the preparation of IPPA {sup 123/131} I was according to the procedures described by Dougan et col. The optimization of the labelling of the labelling condition and product stability were evaluated by radiochemical controls and by biological distribution study using animal models. (author)

  6. Thyroid stunning of 131I

    It is expatiated that the conception, determinant standard and the contributing factors on thyroid stunning, such as dose of diagnostic of 131I, the intervals between the diagnostic scan and administration of ablation dose, which is of important guide sense for establishing clinical protocol of imaging and treatment

  7. Therapeutical uses of 131I

    Physiology of thyroid gland, pathology of thyroid , papillary, follicular cancer is considered together as differentiated thyroid cancer with very good results under therapy with iodine, invitro determination of calcitonin, search of metastasis, anaplastic carcinoma, as indifferentiated carcinoma with similar results as medullary carcinoma. This work gives a protocol for therapeutical use of 131I , in hyperthyroidism due to Graves-Basedow disease, thyrotoxic adenoma or Plummer disease, toxic multi nodular goiter, subacute thyroiditis. Is studied too the treatment with pharmaceuticals, surgery and radioactive iodine. A recommended use of each and protocol for iodine administration, fixed dose technique, dose estimation,absorbed dose, recommendations about when to use and not use 131I are included in this work

  8. Production of fission 131I

    A method of iodine separation from other radionuclides generated by 235U fission has been developed in order to explore the possibilities to obtain 131I as by-product of the 99Mo routine production in the Ezeiza Atomic Centre. The experiments were designed to remove this element to gas phase, and the recoveries were investigated both with and without carrier addition. High volatilization percentages were achieved in the presence of iodine carrier. Some other alternatives to increase the iodine displacement to the gaseous phase, namely vacuum distillation, addition of hydrogen peroxide and use of a carrier gas, were also studied. The method developed, which employs a carrier gas stream, without carrier addition, allows the recovery of about 97% of the 131I, with high specific activity, in a simple and clean way. (author)

  9. Effect of pH of the cervico-vaginal secretion on distribution and migration of /sup 131/I-labelled sperma in the genital tract of sheep at the moment of insemination

    Brueckner, G. (Karl-Marx-Universitaet, Leipzig (German Democratic Republic). Sektion Tierproduktion und Veterinaermedizin); Kaempfer, I. (Karl-Marx-Universitaet, Leipzig (German Democratic Republic). Radiologische Klinik)

    1984-01-01

    /sup 131/I-labelled sperma was used to determine migration, distribution, transcervical passage, and intratubal residence of the semen in the genital tract of estrus-synchronized sheep at various times after insemination as well as for different pH values of the cervico vaginal secretion at the moment of insemination. The pH values of the cervico-vaginal secretion of ewes at the time of insemination were measured in vivo in six sheep herds, at the same time, and pregnancy rates were evaluated after lambing. Fertilisation was found to be about ten per cent above the average pregnancy rate in animals with pH values between 5.9 and 6.4. Tests, using radioactively labelled sperma, showed migration intensities to be generally improved, up to 60 minutes from insemination, when insemination coincided with good pH values. Evidence to that effect was produced by the amount of transcervical passage and by intratubal residence of labelled sperma.

  10. In vivo biological evaluation of {sup 131}I radiolabeled-paclitaxel glucuronide ({sup 131}I-PAC-G)

    Aslan, O.; Biber Muftuler, F.Z.; Yurt Kilcar, A.; Ichedef, C.; Unak, P. [Ege Univ., Izmir (Turkey). Dept. of Nuclear Applications

    2012-07-01

    Paclitaxel (PAC) is a natural occurring diterpene alkoloid originally isolated from the bark of Taxus Brevifolia. It is one of the most important antitumor agents for clinical treatment of ovarian, breast non-small cell lung and prostate cancers. It is known that these types of cancer cells have high {beta}-glucuronidase enzyme which can catalyze the hydrolysis of glucuronides. This is why the synthesis compounds which undergo glucuronidation come into question in the imaging and therapy of these cancer cells. The aim of current study is conjugation of glucuronic acid (G) to the starting substance PAC, labeling with {sup 131}I and to perform its in vivo biological evaluation. Glucuronic acid derived paclitaxel compound [paclitaxel-glucuronide (PAC-G)] was labeled with {sup 131}I using iodogen method. According to thin layer radio chromatography (TLRC) method, the radiochemical yield of {sup 131}I-PAC-G was 84.30 {+-} 7.40% (n=10). The biodistribution of {sup 131}I-PAC-G in healthy female and male Wistar Albino rats has been investigated. Imaging studies on male Balb-C mice were performed by using the Kodak FX PRO in vivo Imaging System. The range of the breast/blood, breast/muscle; ovary/blood, ovary/muscle ratios is approximately between 1.29 and 11.34 in 240 min, and between 0.71 and 8.24 in 240 min for female rats. The prostate/blood and prostate/muscle ratio is between 1.94 and 6.95 in 30 min for male rats. All these experimental studies indicate that {sup 131}I-PAC-G may potentially be used in breast, ovary and prostate tissues as an imaging agent. Also it is thought that {sup 131}I-PAC-G bears a therapy potential because of the {sup 131}I radionuclide and can be improved with further investigations. (orig.)

  11. Increase of the radiochemical purity of aqueous solutions of compounds labelled with 131I using a ClAg sterile column

    The use of a C1Ag sterile column that may be easily assembled at any nuclear medical center is proposed. The column is easy to handle and allows to obtain aqueous solutions of compounds labelled with radioactive iodine, with a radiochemical purity greater than 99%, conserving pH values, activity concentration, apyretogenia and sterility, the controls of toxicity and presence of heavy metals being negative. (C.A.K)

  12. Initial experience with locoregional radioimmunotherapy using 131I-labelled monoclonal antibodies against tenascin (BC-4) for treatment of glioma (WHO III and IV)

    Aim: None of the established treatments (surgery, radiotherapy, chemotherapy) for malignant glioma has improved its very poor prognosis. Adjuvant locoregional radioimmunotherapy (RIT) represents a new therapeutic approach. We present our initial experience with this therapeutic tool with respect to adverse effects, biokinetics and clinical follow-up. Methods: Following surgery and radiotherapy, 12 patients with glioma (4, WHO stage III; 8, WHO stage IV) underwent 1-5 RIT-cycles (average dose 1100 MBq 131labelled monoclonal BC-4 antibodies) at six week intervals. Follow-up included serial FDG-PET and MRI investigations. Evaluation of biokinetics included whole body scans, together with analysis of blood, urine and fluid from the tumor cavity. Results: Following RIT, four patients experienced temporary seizures, which, in one case, were associated with temporary aphasia. Eight patients developed HAMA (human anti-mouse anti-bodies) during follow-up. Mean biologic half-life of the radiopharmaceutical in the resection cavity was 3.9 d (range: 1.0-10.2 d) and remained stable intraindividually during further RIT-cycles. The antibody/radionuclide conjugate remain stable in the tumor cavity for at least 5 d. Median survival presently stands at 18.5 months compared to 9.7 months in a historical patient group (n=89) undergoing conventional therapeutic strategies. Five patients show no signs of recurrence. In three patients with post-surgical evidence of residual tumor, one patient showed partial remission, one stable disease, and one progressive disease during RIT. Four patients without evidence of residual tumor mass at the beginning of RIT developed recurrence during therapy. Conclusions: Initial experience demonstrates that locoregional RIT is a well tolerated treatment modality that may represent a promising new approach in the management of patients with malignant glioma. Advantages of local application include passage of the blood-brain barrier, high concentration of

  13. Radioimmunotherapy with Tenarad, a {sup 131}I-labelled antibody fragment targeting the extra-domain A1 of tenascin-C, in patients with refractory Hodgkin's lymphoma

    Aloj, Luigi [Istituto Nazionale Tumori ' ' Fondazione G. Pascale' ' - IRCCS, Struttura Complessa di Medicina Nucleare, Napoli (Italy); D' Ambrosio, Laura; Aurilio, Michela; Morisco, Anna; Caraco' , Corradina; Di Gennaro, Francesca; Lastoria, Secondo [Istituto Nazionale Tumori ' ' Fondazione G. Pascale' ' - IRCCS, Struttura Complessa Medicina Nucleare, Napoli (Italy); Frigeri, Ferdinando; Capobianco, Gaetana; Pinto, Antonio [Istituto Nazionale Tumori ' ' Fondazione G. Pascale' ' - IRCCS, Struttura Complessa di Ematologia Oncologica, Napoli (Italy); Giovannoni, Leonardo; Menssen, Hans D. [Philogen, SpA, Siena (Italy); Neri, Dario [Institute of Pharmaceutical Sciences, ETH, Zurich (Switzerland)

    2014-05-15

    The extra-domain A1 of tenascin-C (TC-A1) is highly expressed in the extracellular matrix of tumours and on newly formed blood vessels and is thus a valuable target for radionuclide therapy. Tenarad is a fully human miniantibody or small immunoprotein (SIP, molecular weight 80 kDa) labelled with {sup 131}I that is derived from a TC-A1-binding antibody. Previous phase I/II studies with a similar compound ({sup 131}I-L19SIP) used for radioimmunotherapy (RIT) have shown preliminary efficacy in a variety of cancer types. In this ongoing phase I/II trial, Tenarad was administered to patients with recurrent Hodgkin's lymphoma (HL) refractory to conventional treatments. Eight patients (four men, four women; age range 19 - 41) were enrolled between April 2010 and March 2011. All patients had received a median of three previous lines of chemotherapy (range three to six) and seven had also undergone autologous stem cell transplantation (ASCT) or bone marrow transplantation. In addition, seven patients received external beam radiation. All patients had nodal disease, constitutional B symptoms and some showed extranodal disease in skeletal bone (four patients), lung (three), liver (two) and spleen (one). Baseline assessments included whole-body FDG PET with contrast-enhanced CT and diagnostic Tenarad planar and SPECT studies. Patients were considered eligible to receive a therapeutic dose of Tenarad (2.05 GBq/m{sup 2}) if tumour uptake was more than four times higher than that of muscle. All patients were eligible and received the therapeutic dose of Tenarad. Only one patient developed grade 4 thrombocytopenia and leucocytopenia, requiring hospitalization and therapeutic intervention. All other patients had haematological toxicity of grade 3 or lower, which resolved spontaneously. At the first response assessment (4 - 6 weeks after therapy), one patient showed a complete response, one showed a partial response (PR) and five had disease stabilization (SD). Five patients

  14. Interventions in 131I-MIBG treatment of neuroendocrine tumours

    Full text: Specific targeting of neuroendocrine tumours for therapy may be achieved either via the metabolic route (MIBG), via receptor binding (peptides) or via the immunological route (antibodies). Any malignant neural crest tumour, showing sufficient uptake and retention of 131I-meta-odobenzylguanidine (MIBG) on a diagnostic tracer study is a candidate for therapy using this agent. The principle indications for 131I-MIBG therapy are malignant pheochromocytoma and paraganglioma, neuroblastoma stage III and IV, medullary thyroid carcinoma and symptomatic, metastatic carcinoid tumors. At an EANM Radionuclide Therapy Committee workshop on 131IMIBG therapy in 1999 the results of treatment in 534 patients with neural crest tumours were gathered, showing cumulative objective response rates of 51% for malignant pheochromocytoma, 48% for paraganglioma, 51% for neuroblastoma, 23% for medullary thyroid carcinoma and 8% for carcinoid tumors. Moreover, symptomatic palliation occurred in more than 60% of the patients. These results compare favorably with the best reported results of combination chemotherapy. An active uptake-1 mechanism at the cell membrane and neurosecretory storage granules in the cytoplasm of neural crest tumours are responsible for the uptake and retention of 131I-MIBG, respectively, resulting in high tumour/nontumour ratio's. Many drugs are known or may be expected to interfere with (i.e. have a negatively effect on) the uptake and/or retention of 131I-MIBG by the tumour cell. In contrast, there are also factors which may influence either the uptake/retention of 131I-MIBG or the results of therapy in a positive way. Possible interventions: 1. Use of other labels, for example 125I-MIBG, 211At-MABG and 76Br-MBBG, which, in view of their ultrashort pathway, may have a role in the treatment of micrometastases and bone marrow infiltration, particularly as the results of 131I-MIBG therapy under these circumstances are poor. 2. By increasing the specific

  15. Radiochromatographic Determination of 131I Labeled Eugenol

    F. Zümrüt Biber Müftüler; Emine Derviş; Buse Cetkin

    2015-01-01

    Phenolic phytochemicals are a broad class of nutraceuticals found in plants which have been extensively researched by scientists for medicinal potential. Eugenol, a phenolic natural compound available in the essential oils primarily extracted from clove plants, has been exploited for various medicinal applications. It possesses antioxidant, antimutagenic, antigenotoxic, anti-inflammatory and anticancer properties. The goal of current study was to extract Eugenol compound from clove p...

  16. Fast preparation of 131I mIBG at NRCAM

    The diagnostic value of meta-iodobenzyl-guanidine (MIBG) labeled with I-123 and I-131 in the detection and treatment of neuroblastoma and pheochromocytoma is well known. Currently studies of certain myocardial dysfunction as well as drenomedullary abnormalities have performed. In this work labeling with 123I or 131I has been optimized by modifying literature method s that involve on the nucleophilic exchange in presence of Cu (I) and an excess of reducing agents. MIBG was purchased from Sigma chemical Co and CuSO4.5H2O, tin sulfate, 2,5dihydroxy benzoic acid and sodium citrate from Merck. 131I solution in the form of 0.01 N, NaOH were supplied from Nuclear research center in Tehran. Activity in the vial was measured with an ionization chamber dosimeter until, and a pre-calculated volume of sterile water for injection was added to adjust the radioactivity concentration of 25mCi/ml at reference time.The production run proceeded as follows: a) 30μl copper sulfate solution containing 32.5 mg CuSO4.5H2O in 10ml demineralized water, was mixed with 500μl stock solution containing 1.5mg SnSO4, 20mg 2,5 dihydroxy benzoic acid, 45mg sodium citrate; b) The above solution was added to 1mg MIBG in a 10 ml glass vial. The solution on the vial was crystallized by liophilization and sealed; c) 1ml 131I solution containing 25 mCi 131I was purged with N2 for 5 min, 131I solution added to the lyophilized vial. Vial was transferred in an aluminum container then suspended in boiling water for 30 min. where the boiling water with container inside it was monitored with a detector that was installed inside the laminar. Upon cooling, the contents of the vial were made isotonic by 2ml oxygen free citrate buffer solution. The amount of buffer for deferent patients is shown. An acceptable radiochemical yield 90% is obtained at 100 deg. C within 30 min. Chemical and radiochemical purity of 131I -MIBG were determined by TLC. The developed kit followed by a simple radiochemical manipulation

  17. Preparation and stability of 131I-tetracycline

    A method for the iodination of tetracycline is presented which yields > 85% labeling efficiency. The product is stable for a minimum of 72 hr and appears to retain tetracycline-like properties when studied in vivo. The critical factors in the synthesis are reaction temperature, acidity, and drying temperature. The data suggest that 131I-TET can be studied as a tumor scanning agent without fear of product artifact. (author)

  18. Evaluation of 131I retention in several adsorbers

    Several iodine radioisotopes are used in nuclear medicine for treatment and diagnostic purposes. The radioisotope 131I is used both in diagnosis and therapy due to its physical characteristics of decay by β- and its γ-ray emissions suitable for diagnosis. It is routinely produced at IPEN through the irradiation of TeO2 targets in the IEA-R1m nuclear reactor. After the irradiation, the 131I is separated by dry distillation, where the targets are put in an oven, heated at 760 deg C for 2 hours and the 131I, volatile, is carried by an O2 gas stream. The aim of this work was to evaluate the retention and elution of 131I samples produced at IPEN in several adsorbers as part of a project aiming the purification of these radioisotopes, allowing the labeling of biomolecules. Samples of 131I were used for retention and elution studies with the following adsorbers: commercial cartridges, anionic resin columns and cationic resin column. The results showed that Ag cartridges and anionic resins Dowex 1X8, Dowex 3 and IRA 400 had a great iodine retention but no elution after using specific eluents. The QMA light, acid alumina, neutral alumina and cationic resin Dowex 50WX4 showed high retention and elution and QMA plus and cationic resin Dowex 50WX8 and Dowex 50WX12 had a good retention but lower elution. Regarding to the better retention and elution, Ag cartridges and resins showed a higher percentage of iodine retention but lower elution yield and QMA light, acid and neutral alumina cartridges showed better results. (author)

  19. Evaluation of {sup 131}I retention in several adsorbers

    Catanoso, Marcela F.; Osso Junior, Joao Alberto, E-mail: marcela.forli@gmail.co, E-mail: jaosso@ipen.b [Instituto de Pesquisas Energeticas e Nucleares (IPEN/CNEN-SP), Sao Paulo, SP (Brazil). Diretoria de Radiofarmacia

    2011-07-01

    Several iodine radioisotopes are used in nuclear medicine for treatment and diagnostic purposes. The radioisotope {sup 131}I is used both in diagnosis and therapy due to its physical characteristics of decay by {beta}{sup -} and its {gamma}-ray emissions suitable for diagnosis. It is routinely produced at IPEN through the irradiation of TeO{sub 2} targets in the IEA-R1m nuclear reactor. After the irradiation, the {sup 131}I is separated by dry distillation, where the targets are put in an oven, heated at 760 deg C for 2 hours and the {sup 131}I, volatile, is carried by an O{sub 2} gas stream. The aim of this work was to evaluate the retention and elution of {sup 131}I samples produced at IPEN in several adsorbers as part of a project aiming the purification of these radioisotopes, allowing the labeling of biomolecules. Samples of {sup 131}I were used for retention and elution studies with the following adsorbers: commercial cartridges, anionic resin columns and cationic resin column. The results showed that Ag cartridges and anionic resins Dowex 1X8, Dowex 3 and IRA 400 had a great iodine retention but no elution after using specific eluents. The QMA light, acid alumina, neutral alumina and cationic resin Dowex 50WX4 showed high retention and elution and QMA plus and cationic resin Dowex 50WX8 and Dowex 50WX12 had a good retention but lower elution. Regarding to the better retention and elution, Ag cartridges and resins showed a higher percentage of iodine retention but lower elution yield and QMA light, acid and neutral alumina cartridges showed better results. (author)

  20. 131I metabolism in the study of antithyroid drug

    The main purpose of the present report was to study the action of antithyroid drugs on different parameters of thyroid activity utilizing 131I, in the offsprings of rats treated during pregnancy and the perinatal period. Both PTU and MMI caused alterations in growth and thyroid activity, but they were more dramatic with the former. A significative increase in 131I thyroid uptake and in circulating radioactivity was observed. When % uptake was expressed as a function of thyroidal and body weights, a significative decrease was noticed. The ratio T/S and the percentage of labelled iodothyronines in pancreatin digests were also decreased. Neuromuscular maturation was evaluated, by means of the test of Schapiro. A group of animals treated with PTU plus T4 had a significant delay, reaching normal developement later than the controls or those treated with MMI. (author)

  1. Hypothyroidism following 131I therapy for hyperthyroidism

    Of 890 patients who received 131I therapy for hyperthyroidism, the results of therapy were examined on 584 who could be followed up. Of these 502 (86%), were sured including 3 patients who had been completely healed after recurrence, 9 patients are still under medical treatment, and 10 died. The incidence of hypothyroidism following 131I therapy was 1.6% after 1 year, 2.3% after 2 years, 4.7% after 5 years, 15.0% after 10-12 years, 22.1% after 13-15 years and 27.5% after 16-20 years. The incidence increased constantly with the passage of time. Factors influencing the response to treatment have been investigated. As a consequence, the number of rads delivered to the thyroid gland, the gland size, and previous surgery correlated with the incidence of hypothyroidism. The number of doses of 131I, uptake and half-life of 131I in the thyroid, previous antithyroid medication, time between the onset of hyperthyroid symptoms and 131I therapy, and the age or sex of the patients appeared unrelated. The times taken to become euthyroid following a single dose of 131I were 5.6 months with 2000-4000 rads, 4.4 months with 4001-7000 rads, 4.2 months with 7001-10000 rads and 3.5 months with more than 10001 rads. The time was prolonged with decrease of rads delivered to the thyroid gland. It was found that the patients who passed through a transient hypothyroid phase in the period of three to four months after administration of 131I had a high incidence of late permanent hypothyroidism. (Evans, J.)

  2. Therapeutic effect of 131I-histamine-indomethacin in mice with Lewis pulmonary tumor

    Histamine-indomethacin (HIS-IN) was labeled with 131I by chloramine-T method. Thin-layer chromatography (TLC) was performed to evaluate the labeling ratio, radiochemical purity and stability of 131I-HIS-IN, using silicagel GF254 coated on glass plates, with chloroform and methanol being the mobile phase. The biodistributions of 131I-HIS-IN in Lewis pulmonary tumor model mice and normal mice were examined, and therapeutic effect of 131I-HIS-IN on mice with Lewis pulmonary tumor was studied. The results showed that radiochemical purity of the 131I-HIS-IN was 98%, and the highest %ID·g-1 of tumor tissue was 4.73±0.07 at 4 h, while the tumor/blood ratios were 2.95±0.30 at 8 h, 2.67±0.62 at 12 h and 3.54±0.54 at 16 h. The ratios, and the necrotic tissue cells, increased with the post-injection hours. Therefore, 131I-HIS-IN can be a new radioactive drug for tumor therapy. (authors)

  3. The effect of 131I on salivary glands function in 131I treated thyroid cancer patients

    Salivary glands can accumulate 131I and may damage its function during 131I treated thyroid cancer. The purpose of this study is to understand the extent of the injury and its relation with dosage after high-dose radioiodine therapy. Radionuclide dynamic imaging is used to quantitatively calculate the absorption rate and excretion rate of salivary glands. There was no significant difference between patients group and normal controls in absorption rate (P > 0.05), but there existed difference in excretion rate (P 37 MBq but among the groups with dosage 131I treatment

  4. Radioiodine 131I metabolism in human

    Metabolic fate of orally administered 131I in human was studied. Chronological observations of whole body radioactivity distribution and thyroid 131I uptake curve revealed that 131I metabolism was greatly affected by the amount of dietary iodine intake. Under the high iodine intake exceeding 1 mg per day, uptake curve showed biphasic descending type, that is, rapid accumulation during 3 to 6 hours and rapid fall up to 48 hours and gradual decrease afterwards. While, ascending type, monophasic and maximal at 24 hours, was found universary under low iodine intake less than 500 μg per day. Thyroid function should not be affected by the amount of iodine intake, and we analysed 131I metabolism using a new four compartments which included intrathyroidal inorganic iodine pool. The results, especially hormone production rate, were found quite useful even under high iodine intake. Thyroidal organic iodine contents were calculated as approximately 2.5 mg and this value was much less than previously reported values from other countries. Administered radioiodine were mixed up with stable body iodine and reached equilibration by around 10 days. From seroimmunological, histological (microscopic and electron microscopic) studies, and irradiation studies to the cultured human thyroid cells, we concluded that this unexpected phenomenon was derived from chromosomal damage which induced gradual decrease in cell population because of inability to reproduce. Carcinogenic and genetic effects were not serious, and only three leukemic patients were reported in this country and 484 normal babies were born from 7,500 treated parents. Thus, therapeutic dose of 131I was proved rather safe, and even when exposed to radioiodine, administration of perchlorate or thiocyanate, excessive iodine and TSH seemed effective to avoid radiation injuries. (auth.)

  5. 131I-m IBG preparation and clinical applications

    The factors affecting the preparation of 131I-mIBG were studied and the optimal labelling and preparation conditions were determined in a manner that the requirements of GRP and GMP are satisfied. The m-IBG was labeled by isotopic exchange method where in situ produced Cu (II) was used as a catalyst. The Cu (II) was in situ produced by the effect of thiosulfate on Cu(II) ions in the presence of acetic acid. The optimal conditions were determined as: (The ratio of acetic acid to the iodide-131 solution is 0.5-1.5, the reaction temperature is (160 Centigrade), the reaction period is 60 minutes, and the quantity of m-IBG must be more than 1mg). At these conditions, high labelling yield of 98% was obtained. Further purification lead to an increase in the RCP to more than 99%. All preparations produced sterile and Pyrogen free solutions. The biodistribution studies in rats showed random distribution, which were slightly higher than that were shown in literature. These differences were attributed to the absence of stable iodine saturation of the rats prior to the injection of 131I-mIBG in this study. Clinical studies using our products showed high localization in the tumors in case of neuroblastoma patients and in adrenal gland in case of pheochromocytoma patients. (author)

  6. 131I Metaiodobenzylguanidine (131I MIBG) kinetics in a carcinoid tumor

    The 131I-MIBG kinetics was studied in vivo in patients with carcinoid tumors and liver metastases. Activity curve analysis showed that the maximum uptake of 131I-MIBG in a carcinoid tumor occurred after 48 hours, while its biological half time was of 8 days and a half. Although more data are necessary to understand a significant variation in 131I-MIBG kinetics between the different kinds of APUD neoplasms, it is thought that a dynamic-funtional study allowing the evaluation of the different biological half-time, could be helpful for the selection of these neoplasms, which could be treated with 131I-MIBG. Radiation doses required for the treatment are also estimated. (M.E.L.)

  7. Disposition of 131I proinsulin in the rat comparisons with 131I insulin

    The patterns of disposition of intravenously injected doses of 131I proinsulin and 131I insulin were compared in the rat with respect to plasma clearance, uptake, and degradation in selected organs and tissues, and rates of accumulation of degraded products in plasma and urine. The studies indicate that the differences in dose dependency in plasma clearance and degradation of 131I insulin and 131I proinsulin can be attributed to differences in relative uptakes and degradation by the liver and kidneys. The liver appeared to be the major organ involved in the removal and degradation of insulin, whereas the kidney appeared to be the major organ involved in the case of proinsulin. The hepatic process was rapid but relatively saturable, whereas the kidney process was slower but relatively unsaturable. The inverse relationship between initial concentration of hormone in plasma and uptake by liver suggests that the ratio may provide a sensitive index of the role of the liver in plasma hormone clearance

  8. Localization of 131I-chTNT in a nude mice model with human hepatoma

    Purpose: In order to evaluate the targeting activity in the animal model with human hepatoma, the 131I-chTNT radioimmunoimaging was explored. Methods: Radioimmunoimages were taken on different intervals after injection of 131I-chTNT 5.55 MBq to the nude mice, and tissue distribution was measured. The results of 131I-chTNT monoclonal antibody group were compared with that of 131I control group. Results: The experimental group developed tumor positive images after one day of radio-labelled monoclonal antibodies injection and held on until the end of the experiment. The radioactivity in tumor mass was stable, and the half life of 131I-chTNT in hepatoma mass was 6.0 +- 1.6 days. there was no special radioactivity accumulation in normal liver tissue in the nude mice and the radioactivity in it disappeared rapidly. Statistics indicated the tumor/liver ratio in 1, 2, 3, 5, 7 days were 1.03, 2.43, 5.71, 7.96, 10.67, respectively. Conclusions: The results suggest that 131I-chTNT monoclonal antibody has a considerable targeting activity, and provide an evidence for that it can be used as a new radiopharmaceutical agent for the imaging and radio therapy of hepatoma

  9. A monitor of airborne 131I

    An experimental study was conducted of the designing problems of a monitor for air contamination by 131I, i.e., choice of the detector, optimization of the configuration of the adsorbent-detector system, choice of the pump and the interaction of the pump and the adsorbent. A comparison was made of beta and gamma detectors suitable for 131I monitoring. The background was determined for each detector and their sensitivity determined using a 131I source of known activity. The relative sensitivity of the individual detectors was calculated with regard to detector SKW U 04. The ambient area of the SKG-1 detector (45 mm diameter by 50 mm thick) was scanned using a 131I point detector (1x1 mm) to assess the effect of adsorbent shape, size and location on detector efficiency, and the dependence of the sensitivity of well-type scintillators on the position of the source along the well axis was determined. The pumping characteristics of four different pumps are given, i.e., the dependence of the volume flow rate of pumped air on the pressure loss at the pump inlet, the dependence of pressure losses on the flow rate of pumped air for selected adsorption materials, and the values of the specific resistance of filtration materials. Based on the experiments, two monitor designs are suggested, one portable and the other stationary. The portable monitor is equipped with a semiconductor PSC detector and a diaphragm pump, and filtration paper impregnated with activated carbon is used as the adsorbent. The stationary monitor uses a transversely bored 60 mm diameter by 50 mm thick NaI(Tl) crystal. The adsorbent bed is located in the crystal's through-hole which is 16.5 mm in diameter. A stationary air-pump is used. (B.S.)

  10. Comparison of 131I-tetracycline and 67Ga-citrate as abscess localizing agents

    Previous studies have shown that radiolabeled tetracyclines tend to accumulate in infarcts and necrotic tumors. These results suggested that radiolabeled tetracyclines might also accumulate in necrotic abscesses or areas of inflammation. In order to develop a better abscess scanning agent, we compared the efficiency of 131I-tetracycline with 67Ga-citrate in labeling experimentally induced staphylococcal aureus abscesses in rats 24 and 72 hours after injection. In addition to evaluating 131I-tetracycline as an abscess scanning agent, we hoped to obtain data which might clarify the controversy regarding early versus late gallium scanning in suspected infection. 131I-tetracycline was chosen over sup(99m)Tc-tetracycline because the longer half-life of 131I would allow 72 hour imaging. Absolute concentrations of gallium in the abscess contents and in the surrounding areas of inflammation were significantly greater than the concentration of 131I-tetracycline at both 24 and 72 hours. With the exception of blood, muscle, and bone, the abscess-to-tissue activity ratios for gallium and 131I-tetracycline were similar; however, the ratio of gallium activity in the inflammed tissue to other tissues was greater than that of 131I-tetracycline for every tissue examined at both time periods. The data suggest that 131I-tetracycline has little potential as a general abscess scanning agent. The gallium tissue concentrations and tissue ratios suggest that abscesses which can be imaged at 72 hours can probably be imaged at 24 hours, thus allowing earlier initiation of appropriate therapy. Because of the higher lesion-to-blood ratio at 72 hours, a 72-hour scan would appear to be indicated before a scan is interpreted as normal. (orig.)

  11. Adrenal scanning with 131I-19-cholesterol

    The purpose of this paper is to describe our clinical experience of adrenal scanning with 131I-19-cholesterol and discuss its clinical usefulness. Adrenal scanning was performed for 21 patients with hypertension. One millicurie of 131I-19-cholesterol was injected intravenously and adrenal scannings were taken 6 to 11 days after injection with a rectilinear scanner or a gamma camera. No patient had an untoward reaction to the radiopharmaceutical. Confirmed diagnosis was obtained in 7 of 21 patients, i.e., 3 cases of primary aldosteronism, 1 idiopathic aldosteronism, 1 Cushing's syndrome and 2 cases of the essential hypertension. Among all of the primary aldosteronism and Cushing's syndrome, adrenal scanning gave clear evidence of concentration of radioactivity at the site of tumor. In the idiopathic aldosteronism of our study, uptake of radioactivity was brightly visible on the right, while uptake by the left gland was inhibited, so this case was diagnosed incorrectly as primary aldosteronism. The kidney scan with 203Hg-chlormerodrin obtained without moving the patient after an adrenal scan was very useful for getting information of anatomical site of the activity. The effective half-life was calculated as 1.83 days by means of sequential profile whole-body scannings, and the total-body absorbed radiation dose was estimated as 0.65 rad/mCi by using MIRD pamphlets. Our conclusion is that the adrenal scanning with 131I-19-cholesterol is very useful for localization of the functional adrenal cortical tumor. (author)

  12. In Vitro Activities of Moxifloxacin, 127I-Moxifloxacin and 131I-Moxifloxacin Against Staphylococcus Aureus Biofilms

    Hasan Demiroğlu

    2015-02-01

    Full Text Available Objective: The aim of the study was to investigate the antimicrobial effect of Moxifloxacin (MXF, radio (Na131I and cold (K127I iodinated MXF on methicillin susceptible Staphylococcus aureus ATCC 35556 (MSSA biofilms. Methods: MXF was labeled with Na131I using the iodogen method. The optimum radiodination conditions for 131I-MXF was determined by thin-layer radio chromatography studies. Thin-layer radio chromatography (TLRC chromatograms were obtained by using Cyclone Plus Storage Phosphor System. The MICs of MXF, 127I-MXF and 131I-MXF were determined using the microdilution broth method according to CLSI criteria. Time kill curves were performed over 24 h using an inoculum of 2×105 (CFU/mL. Biofilms were grown in microtitre plates, dyed with crystal violet and the mean optical density (OD630 was used for quantification. Biofilms were incubated MXF, 127I-MXF and 131I-MXF at various concentration (0.03 to 64 µg/mL. Results: MXF was labeled with 131I iodogen method. 131I-MXF was obtained with high a yield 95±3%. The MIC values for MXF, 127I-MXF and 131I-MXF was 0.06 µg/mL. Bactericidal activity was demonstrated at 0.25 µg/mL 4 hour for MXF, 127I-MXF and 131I-MXF. At MIC levels, MXF, 127I-MXF and 131I-MXF was not showed a marked reduction of metabolic activity in the S. aureus biofilm. The ODs of biofilm after incubation with an increasing antibiotic concentration were significantly lower than the ODs of biofilms without antibiotic p≤005. The radiolabeled MXF was most effective than MXF, 127I-MXF in reducing the number of bacteria in biofilm. After 24 h incubation Log10 CFU/mL values for 32 µg/mL antibiotic concentration: Control, MXF, 127I-MXF and 131I-MXF were 9.5, 4.3, 4.8 and 3.1, respectively. Conclusion: 131I and 127I were used alone there was no penetration of the S. aureus biofilm and no damage. In contrast our results demonstrate that the radiolabeled Moxifloxacin (131I-MXF have potent anti-biofilm activity against S. aureus

  13. Chrono- and pyro- pharmaceutics (stability) of aqueous 131I-MIBG injectable

    Full text: Stability of a radiopharmaceutical is an important parameter of quality assurance. 131I-mIBG is used for Dx and Rx of neural crest tumours, but its efficacy and even safety (of the patient) depends to a great extent on the integrity of the molecule in the dispensed dosage form because of the nature of the label, 131I. In the case of 131I-mIBG, the structure of the molecule including the specific activity and bonding characteristics of the iodine carrying the hot label are the intrinsic factors, while the aqueous environment, composition, temperature and time of storage serve as the external determinants. For a specific species, it is far easier to control the latter than the former. Since 131I-mIBG is composed of a reactive guanidine moiety, there is a possibility that it could break down into stabler organic component species with or without the radiolabel and free 131I. We have investigated the stability of radiodiagnostic dosage forms at 37 MBq/ml radioactive concentration of 131I-mIBG formulated in acetate buffer at 5 different temperatures (-37,-20,0,20 and 37 deg C) for up to 56 d. We found that the product is relatively stable at -37 deg C for up to 56 d. (8-10% impurity was 131I). The one stored at +37 deg C was the least stable (∼ 75% impurity), the others were of intermediate stability characteristics. The stability of the dosage form could be greatly enhanced by the addition benzyl alcohol; a formulation containing 1% was superior to 0.1%, only the rate of decomposition was slowed down. The former afforded a better shelf life to most of the dosage forms. Thus it can be seen that by changing the external milieu, one could obtain a superior dosage form

  14. Investigation of Radioiodination of Meta-Iodobenzylguanidine Compound with 131I Isotope in Solid Phase Using Cu Catalyzer

    In this study the radioiodination process of meta-iodobenzylguanidine with 131I isotope in presence of ammonium sulphate and Cu(II) Catalyzer was investigated. In order to optimize the process, the influence of different parameters on labeling yield was studied. The results of experiments showed that the use of oil bath with temperature of 160degreeC is necessary. After the labeling process, purification step of the final product was carried out using Dowex-1 x 8 resin. The mean labeling yield was 97.2percent. In this method radiolabelling of MIBG with 131I (185 MBq for diagnostic dose and 3330 MBq for therapeutic dose) is quite simple and it complies with the requirements of routine production of 131I-MIBG radiopharmaceutical for diagnostic and therapeutic purposes. This paper is a narration of industrial scale production of 131I-MIBG radiopharmaceutical.

  15. Measurements of 131I-Labelled Triiodothyronine Uptake by a Resin as a Means of Diagnosing Iodine-Basedow Produced by Intramuscular Administration of Iodized Oil in an Area of Endemic Goitre

    The authors gave intramuscular injections of iodized oil with a view to studying its prophylactic effects on endemic goitre and related defects (such as endemic cretinism) in isolated areas where more traditional techniques have serious limitations. This system had been tried earlier in New Guinea, where the results showed a reduction in the prevalence of goitre and proved the technique to be both safe and practical. However, because of the remoteness of the population in question it was impossible to continue the observations and no information was obtained regarding the effectiveness of iodized oil in reducing the incidence of defects associated with endemic goitre, Ecuador's program, involving studies of the whole population of two rural communities in the Andes, was begun in March 1966. The final control check came three years later. Ethiodol (37% iodized oil, 450 mg iodine per cm3, obtained from Fougera, Hicksville, Long Island, N.Y. United States of America) was injected intramuscularly, 2 cm3 being administered to subjects 12 years of age and older and proportionately smaller doses to younger children. The ethiodol produced extensive changes in the physiological behaviour of the thyroid. 131I uptake was depressed for six months and afterwards remained normal. Similarly, BEI and T4 returned to and stayed at normal levels from the very first control checks onwards, which indicated that even during the first few months the thyroid glands of these subjects were maintaining a normal capacity to secrete thyronines, i.e. that they were not exhibiting the effect described by Wolff and Chaikoff, PBI and BII maintained high livels in all the controls. Urinary excretion of iodine followed a double exponential path: calculations indicated that the subjects would still be excreting significant amounts five years after the injection. Six months after injection there was an unequivocal diagnosis of Iodine-Basedow in three older women with large nodular goitres. Among the

  16. Adrenal scintigraphy using 131I-Adosterol

    131I-Adosterol (6β-iodomethyl-19-norcholest-5(10)-3β-ol) was administered to evaluate adrenal grand in 20 patients including 9 patients with primary aldosteronism, 5 with Cushing's syndrome, one with pheochromocytoma, one with retroperitoneal tumor, 3 with essential hypertension and one with obesity. Standard scintigraphies were performed at 3rd day and again 6th day after administration of 131I-adosterol (1-1.5 mCi). Suppression scintigraphies were obtained while the patients were taking dexamethasone 2 to 3 mg daily from 3 days prior to injection of the tracer until adrenal imaging. In the cases with essential hypertension and obesity, both adrenal glands were delineated equally by standard scintigraphy, and in one patient, undergone suppression scintigraphy, the uptake of 131I-adosterol by both glands were completely inhibited by dexamethasone administration. In primary aldosteronism, six of the 9 patients demonstrated the increased radioactivity in one side, and were diagnosed as aldosteronoma. In 3 cases, failed to show the lesions on standard scintigraphy, the lesions could be detected by suppression scintigraphy, and aldosteronomas measuring 1 x 1 x 0.7, 2 x 2 x 1 and 1.7 x 1.5 x 0.8 cm were confirmed by operation. In Cushing's syndrome, standard scintigraphy could easily distinguish between adenoma (one case) and bilateral hyperplasia (4 cases). Adrenal scintigraphy was also a useful method in order to assess the effect of pituitary irradiation therapy in the case of hyperplasia. In pheochromocytoma and retroperitoneal tumor, the side of the lesion was identified by the absence of a functioning gland. Suppression scintigraphy was particularly useful in detecting the localization of the small tumor in primary aldosteronism. (auth.)

  17. Adverse effects of 131I therapy for differentiated thyroid cancer

    DTC is considered the most common endocrine neoplasm, and 131I therapy has been proven to be an important component in the management strategy. Currently, most research focuses on the adverse effects of radiation exposure to 131I therapy. Some results, based on large-scale and long-term investigation,show new information. Although 131I therapies are usually well tolerated, clinicians involved in the management of DTC need to be aware of the potential toxicity of 131I and take all measures to reduce these effects to a minimum. The aim of this review is to present the adverse effects of 131I therapy for DTC. (authors)

  18. Study on novel peptide probe 131I-RRL for tumor molecular imaging

    To study the potential application value of Ary-Ary-Leu(RRL) specially combined with tumor derived endothelial cells in tumor molecular imaging for melanoma bearing mice, a novel peptide RRL was designed and labeled with 131I by chloramine-T method, and mice bearing melanoma tumor were injected 131I-RRL to imaging. The labeling results showed that the optimized condition were following: 50 μg RRL, 10 μL (74 MBq) Na 131I, 90 μg chloramine-T, total reaction volume 100 μL, and reaction time 3 min, the labeling yield was over 69%. The labeling compound was purified by Sephadex G25, its radiochemical purity was > 95%. In vitro binding experiments, FITC-RRL was mainly combine with tumor cells and tumor angiogenesis endothelial cells, and in the SPECT imaging, 131I-RRL peptide could successfully image the tumor in nude mice bearing melanoma tumor for 24 h after injection. The results indicated that small molecular peptide RRL was a promising carrier for tumor molecular imaging and radioimmunotherapy. (authors)

  19. Efficient production of therapeutic doses of [131I]-metaiodobenzylguanidine for clinical use

    [131I]-metaiodobenzylguanidine (mIBG) is a known radiopharmaceutical used for the treatment of neuroendocrine tumors. The development of therapeutic [131I]-mIBG doses at production level is highly challenging due to rapid product degradation and high radiation exposures to the production plant personnel. In the present work, a working module for the production of 10 doses (100 mCi each) in a single operation was developed following copper (I) assisted isotope exchange. The labeled product complies with the pharmaceutical specifications suitable for in-vivo patient use.

  20. Efficient production of therapeutic doses of [{sup 131}I]-metaiodobenzylguanidine for clinical use

    Prabhakar, G.; Mathur, Anupam; Shunmugam, G.; Teje, Y.D.; Sachdev, S.S. [Radiopharmaceuticals Program, Board of Radiation and Isotope Technology (BRIT), Sec. 20, Vashi, Navi Mumbai 400705 (India); Sivaprasad, N., E-mail: drnsivaprasad@rediffmail.co [Radiopharmaceuticals Program, Board of Radiation and Isotope Technology (BRIT), Sec. 20, Vashi, Navi Mumbai 400705 (India)

    2011-01-15

    [{sup 131}I]-metaiodobenzylguanidine (mIBG) is a known radiopharmaceutical used for the treatment of neuroendocrine tumors. The development of therapeutic [{sup 131}I]-mIBG doses at production level is highly challenging due to rapid product degradation and high radiation exposures to the production plant personnel. In the present work, a working module for the production of 10 doses (100 mCi each) in a single operation was developed following copper (I) assisted isotope exchange. The labeled product complies with the pharmaceutical specifications suitable for in-vivo patient use.

  1. Disposition of /sup 131/I proinsulin in the rat comparisons with /sup 131/I insulin

    Izzo, J.L.; Roncone, A.M.; Helton, D.L.; Izzo, M.J.

    1978-04-01

    The patterns of disposition of intravenously injected doses of /sup 131/I proinsulin and /sup 131/I insulin were compared in the rat with respect to plasma clearance, uptake, and degradation in selected organs and tissues, and rates of accumulation of degraded products in plasma and urine. The studies indicate that the differences in dose dependency in plasma clearance and degradation of /sup 131/I insulin and /sup 131/I proinsulin can be attributed to differences in relative uptakes and degradation by the liver and kidneys. The liver appeared to be the major organ involved in the removal and degradation of insulin, whereas the kidney appeared to be the major organ involved in the case of proinsulin. The hepatic process was rapid but relatively saturable, whereas the kidney process was slower but relatively unsaturable. The inverse relationship between initial concentration of hormone in plasma and uptake by liver suggests that the ratio may provide a sensitive index of the role of the liver in plasma hormone clearance.

  2. Tumor model studies of 131I-tetracycline and other compounds

    Iodine-131-tetracycline (131I-TET) was prepared by allowing tetracycline hydrochloride to react with radioiodide in acidic methanol (labeling efficiency greater than 85 percent). This preparation was found to be stable at --40C for at least 72 hr. Some minimal in vivo breakdown did occur. The 131I-TET, 67Ga, and several /sup 99m/Tc compounds were studied in a rat hepatoma model. The incorporation of the radiopharmaceuticals into the tumor occurred rapidly, with peak levels at 0.5 and 24 hr after injection for 131I-TET and 67Ga, respectively. The clearance of the radiopharmaceutical from nonviable tumor was slower than for viable tumor, and by 72 hr after injection the greatest concentration of radioactivity appeared in the nonviable fraction. All normal tissues showed faster clearance than did tumor tissue, regardless of viability. Decreasing the quantity of 131I-TET injected increased the percent of uptake in the nonviable tumor tissue but had no effect on the viable tumor uptake. Of the /sup 99m/Tc compounds studied, the phosphates developed the highest tumor-to-background ratios. Unfortunately these ratios were not as high as those achieved for 67Ga or 131I-TET

  3. Production of 131I gelatin capsules

    Radioiodine (131I) hard-gelatin capsules are widely used for the diagnosis and treatment of various thyroid disorders. Until 1980 radioiodine was supplied by us as a liquid dosage. This proved to be a rather inconvenient form since it resulted in inaccurate dosing by the physicians and caused frequent contamination of the patients and the hospital personnel. In an attempt to overcome these problems we have designed and constructed a production facility for capsules in which 1311 is packaged. Because of the extreme precautions necessary in handling radioactive compounds, encapsulation of radioactive materials requires specifically designed production techniques, special instrumentation and unique quality control procedures that are not encountered in the standard capsule production processes in the pharmaceutical industry

  4. Separation And Purification Of Radioiodine 131I by Means of wet Distillation Method From By-Product of U-235 Fission Produced 99Mo Process

    The production of 99Mo from 235U fission also produces radioiodine fraction as by product. The radioiodine fraction can be expected to be a complement for radioiodine 131I produced by neutron activation on TeO2 target. Separation and purification were therefore carried out from radioiodine fraction obtained from production process of 99Mo fission product. The radioiodine 131I fraction was separated and purified by means of wet distillation method that is often used for separating 131I from post-neutron activated TeO2. The quality control of the resulting products indicates that the resulting radioiodine 131I solution was suitable to be used for labelling or synthesis of 131I labelled compounds. Although the efficiencies of separation and purification were found to be low ranging between 25 to 37%, the result of the presented experiment generally affirm the consideration to exploit the 131I fission product for labelling or synthesis of 131I radiopharmaceuticals. Key word : distillation, radioiodine 131I , 235U

  5. An alternative intraarterial therapeutic agent for hepatic tumors. 131I lipiodol/histoacryl mixture

    Lipiodol has excellent retainable ability in hepatoma cells. This agent can be labeled with radioisotope (131I) and mixed with tissue adhesive (Histoacryl), and then attached on the lesion of liver by intrahepatic arterial administration. In this study, we attempt to obtain the optimal ratio of Lipiodol to Histoacryl and evaluate the consolidation of blood in vitro and toxicity and biodistribution in vivo. The ratio of 131I Lipiodol/Histoacryl mixture (L/H), concentration of heparin and flow rate of blood are varied by simulating the installation of bloodstream to test the time of consolidation. In addition, the optimal ratios of the L/H mixtures are assessed in vitro in heparinized human blood. According to those results, Lipiodol and Histoacryl mixed with 1:1 or 2:1 ratio have an ideal time of 13 to 15 seconds in vitro; in addition, 1.2:1 ratio is an optimal ratio in the biodistribution study. Interestingly, heparin and acetic acid does not alter the consolidation time, in addition, no variation occurs when varying the flow rate of blood. The consolidation of L/H mixture with blood is incubated in the 37 deg C, normal saline bath for 24 hours. No dissociation of free 131I is found. The optimal mixture is also injected into the hepatic artery of the Sprague-Dawley rats carrying hepatocellular carcinoma (N1S1 cell line). Radioactive consolidate is well confined in the tumor without evidence of leakage of the mixture to the lung or distribution of free 131I in the thyroid. In conclusion, this mixture has the merits of both irradiation and embolization of the tumor. The 131I Lipiodol/Histoacryl mixture (1.2:1) is a promising alternative for intrahepatic arterial administration to treat hepatic tumors. Histoacryl can confine the 131I and, also, embolize the tumor vessels. (author)

  6. Suppression of the growth of human colorectal carcinoma cells (LS174T) by radiolabeled monoclonal antibody (131I-MAbC27) in tissue culture and nude mice

    A monoclonal antibody against carcinoembryonic antigen (CEA), MAbC27, and its F(ab')2 fragments were prepared and labeled with 131I. They effectively suppressed the growth of a human colorectal carcinoma cell line, LS174T, both in culture medium and in inoculated nude mice, whereas 131I-labeled normal mouse immunoglobulin or 131I itself did not have similar effects. Intravenous injection of 131I-MAbC27 or 131I-MAbF(ab')2 following inoculation of carcinoma cells suppressed their growth in vivo. The suppression effect was even more effective when intact antibody rather than its F(ab')2 fragments was used, especially when the treatment was repeated. This study indicates that radiolabeled MAbC27 may be used as a therapeutic agent in CEA-secreting human colorectal carcinomas

  7. Chemical and physical quality control of the HIPPURAN-131I

    Some physico-chemical methods for analytical control of Hippuran-131I are compared. The most convenient to applicate in hospitals and in more specialized quality control laboratories are recommended. The quality of Hippuran-131I produced by ISOTOP (USSR) is also evaluated. The product met the requirement of the International Pharmacopeia

  8. Dose assessment of medical staff taking care of patients treated with 131I due to the intake of 131I

    Aim: Legislation requires that patient receiving 131I in activities greater than 550MBq have to be hospitalized in special closed department. Medical staff taking care of these patients can be exposed to external irradiation and internal contamination with 131I. The aim of this study was to assess the annual effective dose of medical staff taking care of patients treated with 131I due to the occupational intake of 131I. Material - Medical Staff: 6 nurses took care of 6 patients (placed into two rooms) treated with 131I in activities between 550 and 1100 MBq. 131I was normally delivered to patients once per week. After patients received 131I nurses were in contact with patients in average 4 hours per day, 4 days per week. Methods: Direct Method - whole body counting (WBC) of staff was performed daily after they finished their work and indirect method - determination of air 131I concentration in patient's rooms (AC) were used to assess the intake of 131I by staff. Measurements were done in winter period.Results and Dose Assessment: Results of measurements of medical staff and determination of 131I air concentration are presented. Average daily 131I intake of staff assessed from WBC results was 315 Bq; average daily 131I air concentration for first four days was 35 Bq/m3. Assessment of annual effective dose due to the internal contamination (realistic approach): - Direct method: 315 Bq/day x 208 days/year x 7,6 Sv/Bq x 10-9 = 0,498 mSv/year. - Indirect method: 35 Bq/m3 x 1,5 m3/hour x 832 hours/year x 7,6 Sv/Bq x 10-9 = 0,332 mSv/year. Conclusion: Medical staff taking care of patients treated with 131I received effective dose less than 0,5 mSv/year due to the intake of 131I. In the some time period they received 1,65 to 2,24 mSv due to the exposure to the external radiation coming from patients treated with 131I

  9. Toxicity of upfront 131I-metaiodobenzylguanidine (131I-MIBG) therapy in newly diagnosed neuroblastoma patients: a retrospective analysis

    In the treatment of patients with high-risk neuroblastoma, different doses of 131I-metaiodobenzylguanidine (131I-MIBG) are administered at different time points during treatment. Toxicity, mainly haematological (thrombocytopenia), from 131I-MIBG therapy is known to occur in extensively chemotherapy pretreated neuroblastoma patients. Up to now, acute toxicity from 131I-MIBG as initial treatment has never been studied in a large cohort. The aim of this retrospective study was to document acute toxicity related to upfront 131I-MIBG. All neuroblastoma patients (stages 1-4 and 4S) treated upfront with 131I-MIBG at the Emma Children's Hospital, Academic Medical Centre (1992 - 2008) were included in this retrospective analysis. The acute toxicity (during therapy) and short-term toxicity (1st month following therapy) of the first two 131I-MIBG therapies were studied. Of 66 patients (34 boys, 32 girls; median age 2.2 years, range 0.1 - 9.4 years), 49 had stage 4 disease, 5 stage 4S, 6 stage 3, 1 stage 2 and 5 stage 1. The median first dose was 441 MBq/kg (range 157 - 804 MBq/kg). The median second dose was 328 MBq/kg (range 113 - 727 MBq/kg). The most frequently observed symptoms were nausea and vomiting (21 %, maximum grade II). The main toxicity was grade IV haematological, occurring only in stage 4 patients, after the first and second 131I-MIBG therapies: anaemia (5 % and 4 %, respectively), leucocytopenia (3 % and 4 %) and thrombocytopenia (2 % and 4 %). No stem cell rescue was needed. The main acute toxicity observed was haematological followed by nausea and vomiting. One patient developed posterior reversible encephalopathy syndrome during 131I-MIBG therapy, possibly related to 131I-MIBG. We consider 131I-MIBG therapy to be a safe treatment modality. (orig.)

  10. Radiation shielding of 131I therapeutic ward in department

    Objective: To rebuild an 131I therapeutic ward of the department of nuclear medicine in the hospital, and design the radiation shielding to make the radiation safety achieve the national standards. Methods: According to the protection demands of national relating standards, the design of the ward was based on the basic principles and methods of radiation shielding of 131I, and combined the distribution of radioactive sources, rooms and people. Results: The design parameters and radioprotection data of the rebuilt ward were obtained and the radiation shielding was safe by monitoring. Conclusion: The design of the 131I therapeutic ward achieved the anticipated target that the radiation safety could be controlled. (authors)

  11. Analysis of pelvic 131I uptake after 131I whole body scan in patients with thyroid cancer

    Objective: To analyze and explore the possible mechanism for pelvic 131I uptake after 131I post treatment whole body scan (Rx-WBS)in patients with differentiated thyroid cancer. Methods: (1) Data were retrospectively reviewed from 168 female patients with differentiated thyroid cancer (everyone has a Rx-WBS). (2) 46 patients were accepted by analyzing the characteristics of Rx-WBS and combing with some inclusion criteria,and then followed up. Results: Among the 46 patients (46 positions accumulated 131I) with significant pelvic 131I uptake, 6 patients had two reasons leading to pelvic 131I uptake, and 2 patients had no specific reason. Among the 50 reasons for pelvic 131I uptake, 41 reasons related with uterus, 3 reasons related to rectum, 5 related to bladder and 1 related to ovarian chocolate cyst. Among the 41 reasons related to uterus, by combining the examinations of SPECT/CT, ultrasound, CT and the follow-up results, 18 were uterine leiomyomas, 9 were intrauterine devices, 2 were endometrial thickening, 3 were uterine cavity effusion, 7 were menstrual periods, 1 were uterine adenomyosis, 1 were gestational sac. Conclusions: (1) In the Rx-WBS of female, the significant pelvic 131I uptake is generally caused by uterus, but not bladder. And it usually means gynecological disease, especially uterine leiomyomas when excluding physiological factors. (2) It is generally easy to differentiate bladder from rectum because they have different characteristic features of the pelvic 131I uptake. (3) SPECT/CT plays a very important role in locating 131I uptake in uterus. (authors)

  12. Variations in soil texture and levels of 131I contamination on the 131I uptake and transfer in sunflower (Helianthus annus L.)

    The effects of soil texture and levels of 131I contamination on 131I uptake and soil to crop transfer factor (TF) in sunflower were studied in a pot experiment. The 131I uptake and tf were significant in root and in the sandy soil. With increase in the level of '131I contamination 131I uptake tended to increase, but the TF decreased. (author)

  13. Adrenal scanning with {sup 131}I-cholesterol; Diagnostik von Nebennierenrindenerkrankungen mit {sup 131}I-Cholesterol

    Hahn, K. [Klinik und Poliklinik fuer Nuklearmedizin, Klinikum der Ludwig-Maximilians-Univ. Muenchen (Germany)

    2009-03-15

    Adrenal scanning with {sup 131}I-19-cholesterol is used in patients with various forms of adrenal malfunction (adreno-cortical carcinoma or adenoma, hypothalamic-hypophyseal form of Cushing's syndrome, adrenal hirsutism, primary or secondary adrenocortical insufficiency). Adrenal scanning is optimal between the fourth and tenth day after intravenous injection of {sup 131}I-19-cholesterol. This method makes it possible to estimate the size and functional status of the adrenals. Limitation of the method is the relatively high radiation dose of {sup 131}I-19-cholesterol. (orig.)

  14. Clinical evaluation of 131I in treatment hyperthyroidism

    The clinical value of 131I in the treatment of hyperthyroidism is observed. The weight of the thyroid was evaluated by palpation, 131I was taken orally by one dose method. The dose was calculated by actual absorption of 131I/per gram of thyroid. 3 - 6 months after drug administration, the symptom, clinical manifestation and the serum hormone of the pituitary-hypothyroid axis were observed. In 105 cases, 80(76.2%) were nearly recovered, among them 16(15.2%) had hypothyroidism in the early period. The all over recovering rate was 91.4% in one dose, but 9(8.6%) were recurred and can be controlled at a second dose. Therefore 131I for the hyperthyroidism had a high recovering rate, low recurring rate and was very convenient. If prospect on the Chinese effort the controlled, the occurrence of hypothyroidism can be reduced to the acceptable level

  15. Management of thyroid carcinoma with radioactive 131I

    Purpose: To evaluate the role of radioactive 131I in the management of patients with well differentiated carcinoma of the thyroid. Methods and Materials: Between 1965 and 1995, a total of 117 patients with well-differentiated carcinoma of the thyroid underwent either lobectomy or thyroidectomy followed by 100-150 mCi of 131I. Results: With a median follow-up of 8 years, only four patients (3%) developed a recurrence of their disease. The 5-year actuarial survival was 97% with a 10-year survival of 91%. There were no severe side effects noted after 131I therapy. Conclusions: Radioactive 131I is a safe and effective procedure for the majority of patients with well-differentiated thyroid carcinoma. We currently recommend that all patients undergo a subtotal or total thyroidectomy followed by 131I thyroid scanning approximately 4 weeks after surgery. If the thyroid scan shows no residual uptake and all disease is confined to the thyroid, we recommend following patients with annual thyroid scans and serum thyroglobulin levels. If there is any residual uptake detected in the neck or if the tumor extends beyond the thyroid, we recommend routine thyroid ablation of 100-150 mCi of radioactive 131I

  16. 131I treatment in patients undergoing renal dialysis: our experience

    Radiation Protection issues concerning patients, public and staff must be considered carefully in hemodialysis for chronic renal failure patients scheduled for 131I high dose therapy. In order to assess the risks related to this medical procedure, hemodialysis clearance of 131I and contamination measurements were carried out. We have studied 12 hemodialysis procedures corresponding to 2 cases of hyperthyroidism disease (555MBq of 131I administered) and 3 patients with carcinoma of the thyroid (5550 MBq of 131I administered). The arterio-venous difference of 131I across the artificial kidney and dose rate reduction at one meter of patient were measured. Contamination levels of the dialyser machine, filters and tubes were measured after dialysis with a contamination monitor. Direct read-out dosimeters were used to assess the radiation doses to nursery staff involved. The result obtained for mean 131I clearance in blood was 75±11%. The mean dose rate reduction at one meter of the patient was 58±18%. We also checked that contamination levels for the dialyser machine, filters, tubes and accessories were lower than 10Bq/cm2. For the nursery staff the radiation dose was found to be lower than 0.1mSv. (author)

  17. Thyroid uptake and radiation dose after 131I-lipiodol treatment: is thyroid blocking by potassium iodide necessary?

    In radionuclide therapy with iodine-131 labelled pharmaceuticals, free 131I may be released and trapped by the thyroid, causing an undesirable radiation burden. To prevent this, stable iodide such as potassium iodide (KI) can be given to saturate the thyroid before 131I is administered. The guidelines of the European Association of Nuclear Medicine do not, however, recommend special precautions when administering 131I-lipiodol therapy for hepatocellular carcinoma. Nevertheless, some authors have reported 131I uptake in the thyroid as a consequence of such therapy. In this study, the influence of prophylactic KI on the thyroid uptake and dose (MIRD dosimetry) was prospectively investigated. 131I-lipiodol was given as a slow bolus selectively in the proper hepatic artery or hyperselectively in the right and/or left hepatic artery. Patients were prospectively randomised into two groups. One group received KI in a dose of 100 mg per day starting 2 days before 131I-lipiodol administration and continuing until 2 weeks after therapy (KI group; n=31), while the other group received no KI (non-KI group; n=37). Thyroid uptake was measured scintigraphically as a percentage of administered activity 7 days after 131I-lipiodol (n=68 treatments). The absorbed radiation dose to the thyroid was assessed by scintigraphy after 7 and 14 days using a mono-exponential fitting model and MIRD dosimetry (n=40 treatments). The mean activity of 131I-lipiodol administered was 1,835 MBq in a volume of 2 (n=17) or 4 (n=51) ml. Thyroid uptake was lower in the KI group, being 0.23%±0.06% of injected activity (n=31) compared with 0.42%±0.20% in the non-KI group (n=37); the mean thyroid dose was 5.5±1.6 Gy in the KI group (n=19) versus 11.9±5.9 Gy in the non-KI group (n=21). These differences were statistically significant (P131I-lipiodol administration was evident (P>0.1). 131I-lipiodol is associated with a generally low thyroid uptake and dose that may be significantly decreased by KI

  18. Comparison of [131I]-Tyr3-octreotate and [131I]DOTA-Tyr3-octreotate: the effect of DOTA on the pharmacokinetics and stability

    The introduction of radiolabeled somatostatin analogs for peptide receptor imaging and therapy of neuroendocrine cancer have become a primary focus of interest in nuclear medicine. In this work we studied the possibility of preparing radioiodinated octreotate derivatives, with high stability and favourable kinetic in vivo, because 131I-iodide is most frequently used in therapeutic nuclear medicine and aviable. We studied molar peptide to radionuclide ratio in order to obtain the mono-iodinated peptide (di-iodinated no longer binds to the somatostatin receptor). Like other radioiodinated proteins labeled on constituent tyrosine residues, it was important to study the possibility of dehalogenation in vivo. Despite DOTA chelating group was not necessary to the radioiodination procedure, we intended to evaluate the influence of the chelating group on the pharmacokinetic and the in vivo stability of the labeled peptide. 131I radiolabeling of Tyr3-octreotate and DOTA-Tyr3-octreotate was performed using Chloramine T method. A solution of 10 μg of peptide/40 μL of PBS (0.05M phosphate-buffered saline pH 7.5) was transferred to an Eppendorf cap. After addition of 10 μL (74 MBq) radioiodine and 5 μL of chloramine T solution (1mg/mL PBS), the cap was carefully stirred and the labeling reaction was allowed to proceed for 3 minutes at room temperature; 5 μL of sodium methabisulfite solution (2mg/mL PBS) was introduced as reducing agent. Radiochemical purity was determined by HPLC (Waters) using a RP C18 column (4.2 x 50 mm, 5 μm, Waters) with UV (230 nm) and radioactivity (Packard Canberra) detection, flow rate of 0.5 mL/minute with a linear gradient of 40-80% (v/v) methanol in 50 mM sodium acetate buffer (pH 5.5) for 20 minutes, maintained for another 25 minutes. Free radioiodine was also determined by horizontal zone electrophoresis (Amershan Pharmacia) on Whatman 1 paper, 0.05M barbital buffer, pH 8.6, 300V, 40 minutes. The stability of the compounds were evaluated

  19. 131I imaging and Tg levels: values of 131I therapy in patients with lung metastases from differentiated thyroid carcinoma

    Objective: To explore the value of 131I imaging and serum Tg levels for assessment and monitoring of 131I therapy in patients with lung metastases from DTC. Methods: From 2007 to 2011,50 patients with DTC lung metastases were investigated. Diagnostic 131I imaging, Tg levels and 131I imaging + Tg levels were used to monitor and assess the outcomes of 131I treatment, respectively. The effective rates between patient lesions with diffuse configuration and focus configuration in PET/CT images, patients with and without extra lung metastases,and among patients with different Tg levels (< 100 μg/L, 100-1000 μg/L, >1000 μg/L) were compared. Statistical analyses by χ2 test, Fisher exact test and Wilcoxon rank sum test were performed using SPSS 11.5. Results: Forty-eight DTC patients with pulmonary metastases were observed by positive findings based on 131I imaging. Eleven cases were negative and 24 cases got better after 131I treatment. The effective rate was 73% (35/48). No difference was found between diffuse configuration or focus configuration (69 % (11/16) vs 75 % (24/32), χ2=0.211, P>0.05). Patients without extra lung metastases had better prognosis than those with extra lung metastases (70% (28/40) vs 3/10, χ2=3.868, P<0.05). The Tg levels decreased to 78.3 μg/L from 108.7 μg/L after 131I treatment (Z=-0.698, P>0.05). Tg levels decreased in 66% (33/50) patients and increased in 17 cases. Patients with Tg levels <100 μg/L had better efficiency than those with Tg levels > 1000 μg/L (80% (20/25) vs 3/10, P=0.015). However, the effective rate was 67% (10/15) in the 100-1000 μg/L group, which was not significantly different from those in the other 2 groups (χ2=0.320, P>0.05; P=0.111). Considering the combined results of 131I imaging and Tg levels determination, the effective ratio was 62% (31/50) with 6 clinically cured patients and 25 partially responsive patients. Conclusions: 131I imaging and Tg level analysis are both important procedures for lung

  20. 131I rose bengal hepatography and sequential liver scintigraphy in the differential diagnosis between congenital biliary atresia and infantile hepatitis

    For the purpose of the differentiation between congenital biliary atresia and infantile hepatitis, 30 hepatographies and 140 sequential liver scintigraphies with 131I rose bengal were performed. In 140 cases of sequential liver scintigraphies (72 with congenital biliary atresia and 68 with infantile hepatitis) scintigraphies were usually obtained at 30 minutes, 5 hours and 48 hours after the injection of 131I rose bengal, and the criteria used for the diagnosis of congenital biliary atresia were 1) visualization of the kidney, 2) no detectable radioactivity in the intestine, 3) prolonged retention of the 131I rose bengal on the liver scintigram. Several sup(99m)Tc labeled hepatobiliary agents, for example sup(99m)Tc FPI, sup(99m)Tc HIDA and sup(99m)Tc EHIDA, were tried to use for the infants with jaundice to compare with 131I rose bengal. As the result, it is conceivable that the sequential liver scintigraphies with 131I rose bengal were the most suitable method for the diagnosis of congenital biliary atresia, and the criteria described above were available for the decision of indication for surgery. (author)

  1. Effects of combined 131I- and CT-BAC5 immunotherapy on NPC CNE-2 multicellular spheroids

    Objective: To develop a new specific therapeutic method for treating nasopharyngeal carcinoma (NPC) and to evaluate its effects on an in vitro tumor spheroid model. Methods: The human NPC cell line CNE-2 spheroids were grown in culture medium, on a thin layer of 0.75% agarose. The average volume of the spheroids was estimated by 1/2 (short dimension)2 x (long dimension). Anti-NPC BAC5 MAb was labelled with 131I using chloramine-T method. Cytotoxin from Chinese cobra (CT) was conjugated with BAC5 by hetero bifunctional cross-linking reagent (SPDP). The spheroids were treated with either 131I-BAC5 or CT-BAC5 separately or with both of them together by incubating in culture medium. Results: The conjugated rate of BAC5 and CT was 32.4%. CT-BAC5 significantly inhibited the growth of CNE-2 multicellular spheroids comparing with control agent (normal saline) (P 131I-BAC5 did more than CT-BAC5 (P131I-BAC5 with CT-BAC5 treatment showed even stronger destructive effect on the spheroids (vs. normal saline, P 131I-BAC5 with CT-BAC5 is better than either of them working separately

  2. Differential role of Rad51 in repair of DNA damage induced by β-rays of 131I in Raji cells: a comparison with the γ-rays

    Radioiodine is one of the oldest radionuclide used in therapy of thyroid disorder. The scope of application of radioiodine increased tremendously due to simple method of labeling of biomolecules with 131I without significant changes in biological properties. Thus, biomolecules labeled with 131I promised immense potential as therapeutic radiopharmaceuticals for cancer. The therapeutic efficacy depends on the characteristics of the β-emitter attached. The mechanisms of cell death and DNA damage repair induced by β-emitting radionuclide are not well known. In this experiment, the authors have attempted to investigate the underlying mechanism causing cell death in Raji cells and have compared the therapeutic efficacy of beta emitter, 131I, to γ-radiation by exposing the cells to an equivalent dose of γ-. Raji cells were incubated for 2h with 1.85 MBq of 131I radioactivity. Equal numbers of cells were exposed to an equivalent dose (0.4 Gy) and a therapeutic dose of 2 Gy from gamma radiation. Cell toxicity was assessed by trypan blue dye and MTT assay. Apoptosis was assessed by estimation of DNA fragmentation and cleaved PARP proteins. Radiosensitivity and DNA damage repair gene expression were analyzed by real time q-PCR. Cell viability and proliferation study confirms that Raji cell line showed comparatively higher radiosensitivity with beta emitter (131I) compared to γ-rays. In the case of apoptosis, beta emitter (131I) showed significantly high DNA fragmentation and PARP cleavage. RAD51 gene expression does not change with time in the case of 131I while it changes in the case of γ-radiation. Beta radiation from 131I is observed to be more potent in induction of cell toxicity and apoptosis in Raji cells than the γ-rays. However, RAD51 does not take part in the DNA DSB repair pathway induced by 131I and therefore play a major role in discriminating the effect of gamma rays. (author)

  3. 131I treatment for brain metastases from differentiated thyroid carcinoma

    YU Yong-Li; LU Han-Kui; ZHU Rei-Sen; MA Ji-Xiao

    2004-01-01

    To assess the clinical value of treatment with 131I for brain metastases from differentiated thyroid cancer (DTC), we have observed 8 cases of brain metastases from DTC who received follow-up after 131I therapy (2male, 6 female, aged 12~65 years). The results of 131I therapy were evaluated with clinical presentation, imaging scan and survival analysis. The main results are as follows. (1) All cases had been survival for 2~35 years in follow-up. (2)A space-occupying lesion in right cerebellum was reduced after taking 20.65 GBq and disappeared after 23.61 GBq,demonstrated by computed tomography. (3) The sequences and doses of 131I therapy were clearly decreased for the cases with total thyroidectomy in comparison with those with semithyroidectomy (p<0.01). (4) The brain metastases with lung and/or bone metastasis from DTC were 75% (6/8) and it was difficult to cure these metastases at the same time. It is concluded that the postoperative treatment of 131I for brain metastases from DTC after undergoing thyroidectomy may improve clinical symptoms and life quality, reduce lesions, and prolong survival.

  4. Preparation of 131I-BmK CT and bio-distribution and imaging in glioma-bearing rats

    In this work,we explored the method of radiolabeling scorpion toxin peptide BmK CT, and investigated the stability,the ability of cell conjugation of 131I-BmK CT, and its distribution and imaging in glioma-bearing Wistar rats. After cloning, expression, and purification, BmK CT was labeled with 131I by indirect labeling (Bolton -Hunter method). 131I-BmK CT was injected into the tail vein of glioma-bearing rats,and imaged at 1, 4, 8, 24 and 48 h. The rats were sacrificed by cervical dislocation,and tissue samples were studied. 131I-BmK CT was successfully prepared with the overall yield of 37.8 ±8.9%. The radiochemical purity was more than 95%. The specific binding efficiency of 131I-BmK CT with C6 glioma cell was 39.62%. In the first 24 h after injection, the bio-distribution in rats showed rapid blood clearance. Most of the radioactivity was observed in liver, lung and kidney. After 24 h, the bio-distribution showed renal clearance, especially at the peak time of accumulation,when the tumor could be viewed clearly. The largest uptake ratio of tumor to non-tumor (background)(T/NT) at 4 h was 6.79 ±0.29. In conclusion, 131I-BmK CT can be prepared and specifically conjugate with C6 glioma cell. Good bio-distribution was observed in glioma-bearing rats. Nevertheless, great deal of research work needed to be done before clinical application of the medicine. (authors)

  5. Effects of specific activity on meta-[131I]iodobenzylguanidine kinetics in isolated rat heart

    The effects of specific activity of meta-[131I]iodobenzylguanidine (MIBG) were studied in uptake-2 blocked isolated perfused rat heart. [131I]MIBG was administered in the perfusate as an 8-min pulse, followed by an 80-min washout period. Kinetic analysis of the externally monitored time-activity curves gave estimates of uptake rate and multiexponential clearance. Uptake rate showed an MIBG concentration dependence that is sigmoidal, yielding Michaelis-Menten constants KM = 52 nM and Vmax = 0.23 nmol/min/g. Clearance rate was also dependent on loading MIBG concentrations; the primary effect of increasing loading concentration was an increase in the rate of the slowest clearance component, possibly reflecting nonspecific turnover. No effect of specific activity was observed on tissue uptake and retention of [131I]MIBG for loading concentrations of MIBG in the heart tissue under 0.5 nmol/g. Extrapolation of these results to human studies indicates that isotope-exchange-labeled [123I]MIBG has a specific activity sufficiently high to avoid mass effects on its heart retention

  6. Prototype development of filter monitor for 131I processing plant

    Iodine-131 (131I) is used extensively in nuclear medicine because of its short half-life and useful beta emission. Isotope Production and Applications Division (IP and AD) of BARC produces 131I in its processing plant. The charcoal filters that are capable of extracting high levels of radioactive iodine and particulates in the suction flow are installed in the plant. The radioactive iodine is fully removed and deposited onto activated charcoal impregnated with potassium iodide. These charcoal filters get saturated over a period of use and need to be replaced with fresh ones. A 5-channel Filter monitor for online measurement of radiation level of trapped 131I on the charcoal filter is being developed by IP and AD, BARC. The unavailability of this type of instrument motivated to undertake this development. Current paper deals with a prototype filter monitor developed with single detector. Some results prove the functionality of the system. (author)

  7. 131I-19-iodocholesterol adrenal scanning in Cushing's syndrome

    7 patients were investigated: 2 bilateral hyperplasia due to pituitary ACTH excess showed bilateral adrenal activity. 1 post-surgical remnant with recurrent Cushing's syndrome was detected. 1 adenoma showed unilateral intense activity and absent activity in the controlateral gland, even after ACTH treatment. 2 carcinomas were weakly imaged. In 1 case, hepatic metastasis showed 131I-19-iodocholesterol uptake. Adrenal imaging with 131I-19-iodocholesterol is not a good procedure for assessing hormonal function. It is a valuable and safe tool in the localization and diagnosis of adrenal lesions causing Cushing's syndrome, perhaps better than radiologic procedures. Radiation dosimetry is acceptable

  8. Development of a recovery method of 131I in the 99Mo process through the fission of 235U

    131I is an iodine radioisotope widely used in nuclear medicine that can be used either for diagnostic or for treatment due to its physical decay by β- and its high emission of y-rays. It is produced at IPEN using the indirect reaction: 130Te(n,y)131mTe → 131Te → 131I where TeO2 targets are irradiated in a Nuclear Reactor. There is also the possibility of producing 131I by the fission of 235U, where about 300 different elements are produced together with 131I. The 131I produced through this method presents high specific activity and radioactive concentration suitable for the labeling of molecules. The aim of this work was to develop a recovery method of 131I with the required quality to be used in Nuclear Medicine in the 99Mo production process through the route of acid dissolution of metallic 235U targets. 131I can appear in two phases of the process, both in the gaseous phase produced during the dissolution of metallic U targets and in the dissolution solution. This work studied the recovery of 131I in these two phases. Several materials were used for the capture and recovery of 131I at the two phases of the process, the gaseous one and the solution of dissolution of U targets. Columns of alumina with Cu, acid alumina with Cu, Ag microspheres, Cu microspheres, Ag nanospheres, anionic cartridges, Ag cartridges, anion exchange resin and activated charcoal columns were tested. Solutions containing 131I in 0.1 mol.L-1 NaOH were percolated through the materials and the eluted solutions were analyzed in a dose calibrator. The precipitation of AgI was also studied wth further dissolution of this precipitate with 0.1 mol L-1 NH4OH and 5% Na2S2O3. The recovery results varied according to the material, activated charcoal showed recovery yields between 42% and 83% but the recovery yield of the alumina column with Cu ranged from 20% to 85%. Tests with Ag nanospheres showed recovery yield of 26% using 0.1 mol L-1NaOH and 72% for Na2S2O3. Tests with anionic cartridges

  9. Stability studies of therapeutic 131I-meta-iodobenzylguanidine (131I-mIBG) using high performance liquid chromatography

    BRIT is a manufacturer and supplier of therapeutic doses (100 mCi) of the radiopharmaceutical 131I-mIBG to various nuclear medicine centers in India. The therapeutic formulation is of high radioactive concentration (>10 mCi/ml) and is thus prone to radiolytic damage during transport, storage until administration. Earlier stability studies at this laboratory were done using conventional methods like Thin Layer Chromatography (TLC) which has an inherent limitation in terms of resolution. In view of this, a suitable HPLC method has been developed and the stability of therapeutic 131I-mIBG was monitored at various conditions

  10. Therapeutic Feasibility Study and Clinical Trial of Intrahepatic 131I-Lipiodol on Patients with Hepatocellular Carcinoma

    An iodized oil such as Ethiodol or Lipiodol was selectively retained in the tumor vessels of the large hepatomas as well as in the small daughter hepatomas for long periods following the intra-arterial hepatic injection of such contrast material. The specific aim of the study is to deliver a high internal radiation dose to hepatocellular carcinoma (HCC) in an attempt to control the disease. We were able to replace a small fraction of the stable iodine (I-127) of the 37% iodine in Lipiodol by the 131I with 100% exchange efficiency. 131I labeled Lipiodol was injected through the super-selected tumor feeding artery under superselection or into the proper hepatic arterial level of patients who have malignant hepatomas confirmed by aspiration cytology, serum AFP and various imaging modalities, Clinical trail was performed on 43 cases during recent 6 months and follow-up observation was carried out. No severe complications or other adverse reactions were encountered until nowadays. 131I-Lipiodol was stable in vivo and no significant activity was noted in the thyroid, stomach, blood and urine after the injection. Only small fraction of radioisotope activity was noticed in the both side of lungs. Tumor to normal liver radio was very high. Therefore, 131I-Lipiodol (or P-32-Lipiodol) will be effective delivering high internal radiation dose to the tumor while delivering small radiation doses to normal tissues. Labeling, tumor dose calculation and preliminary findings will be presented.

  11. Biodistribution of 131I-Herceptin in breast cancer xenograft

    Objective: to establish Her-2 positive SK-BR-3 human breast cancer xenografts in athymic mice. To explore the biologic distribution of 131I-herceptin in human breast cancer xenografts. Methods: Implant SK-BR-3 cells subcutaneously to BALB/c-neu athymic mice to establish animal model. To measure the radiocounting per minute (cpm) of every organ on a γ arithmometer at 4, 12, 24, 48 h postinjection of 131I-Herceptin or 131I-mIgG, then to gain the T/NT ratios and the uptakes percentage per gram of the injection dose (% ID/g). Results: After subcutaneously planted, a 96% of tumor forming rate was achieved. Compared with the control group, bigger T/NT and % ID/g was obtained in the experimental group (P<0.05 and <0.01). Conclusion: A high tumor forming rate can be get by implanting SK-BR-3 cells subcutaneously to athymic mouse, 131I-Herceptin is obviously concentrated in tumor tissues. (authors)

  12. Radiation danger (131I, milk, thyroid, children - why?)

    The influence of reactor accidents on environment contamination by iodine isotopes is described. The main ways of man contamination are presented. The role of milk contamination is stressed. 131I kinetics in man and its effects are considered. The absorbed doses are assessed. 1 fig., 6 tabs. (A.S.)

  13. Determination of 131I and thorium in urine

    Methods for the determination of 131I and Thorium in urine have been developed taking into account the monitoring needs for people who handle with these radioisotopes. The method for determining 131I is based in the use of silver chloride to separate iodine by precipitation from the sample; the detection was carried out in a Nal (Tl) well type scintillator connected to a single channel analyser. This method has the following advantages; it is easy and relatively fast as well as selective, showing a separation yield higher than 80%. Thorium in urine was determined by colorimetry after the mineralization of the sample using nitric acid, and sulphuric acid, and then oxygen peroxide. The chromophore reagent used was Thoron (disodium salt of 2-(2-hydroxy-3,6-disulfo-l-naphthylazo) benzenearsonic acid).The absorbance was measured in a spectro colorimeter at a fixed wavelength (530 nm). The method proved to be simple allowing a separation yield of about 80%. The most representative sample for a monitoring program in a 131I production laboratory has been established. The 131I concentration in urine of individuals with chronic contamination have also been measured; an interpretation of these results is discussed. (author)

  14. Therapeutic Effect of 131I for 230 Patients with Hyperthyroidism

    To evaluate the therapeutic effect of 131I in treatment of patients with hyperthyroidism and analysis the factors that influence the effect, 230 cases of hyperthyroidism were treated with 131I, and were followed-up at 1.5, 3, 6, 12 months and even longer time after 131I radiotherapy. The serum levels of FT3, FT4 and TSH were detected in all cases. The results showed that 181 patients were cured (78.6%), 22 patients were improved (9.5%), 23 cases developed early hypothyroidism(10.0%),and 4 cases developed later hypothyroidism. 12 cases in 27 patients with hypothyroidism treated with thyroxin were recovered, but the other 15 cases need to be given permanent treatment. The factors which influence 131I radiotherapeutic effect include the patient age, course of disease,application of ATD, size and quality of thyroid, and the level of thyroid hormone. The patients should be followed up to prevent occurrence of hypothyroidism. The early hypothyroidism should be treated in order to decrease the permanent hypothyroidism rate. (authors)

  15. Determination of 131I-hippuran and its main contaminants by thin-layer cromatography

    Thin-layer elution-spectrophotometric and densitometric methods were developed for the simultaneous determination of orthoidohippuric acid and its main contaminant, orthoiodobenzoic acid after their chromatographic separation using a methanol-chloroform-acetic acid 100:75:2.5 solvent mixture and Kieselgel 60 F254 layer. Benzyl alcohol, also present in the pharmaceutical preparation, does not interfere. The precision of the procedures corresponds to that of radio paper chromatography. It is pointed out that, besides the orthoiodobenzoic acid, traces of other similar 131I-labelled organic contaminants may be present in the preparation. (author)

  16. Lymphatic pathways and rate of absorption of 131I-albumin from pericardium of dogs

    Labeled albumin diluted to 4.0 ml with normal saline solution was instilled into the pericardium of 14 dogs. Lymph from the right lymphatic duct (RD) and thoracic duct (TD) was collected at intervals as well as blood samples, and radioactivity measured. Radioactivity was found in both RD and TD lymph, indicating a multiple efferent lymphatic system for drainage of the heart and pericardium. The level of 131I-albumin absorbed from the pericardium reached a peak in 6-22 1/2 hours in RD and TD lymph, and in 2-22 1/2 in blood stream. (orig.)

  17. Two kinds of biological dosimeters applied to 131I-treated thyroid cancer patients

    We investigated 10 thyroid cancer patients after 131I oral medication at the range of (3.7-27.5 GBq) total activity with dicentric chromosome aberration analysis and the T-cell antigen receptor (TCR) mutation assay. We compared and evaluated both methods on their accuracy and applicability. The 10 thyroid cancer patients are at 30-50 years old, and we got 5 ml peripheral blood individually for the investigations. We worked the dicentric aberration analysis with the conventional giemsa method. The first division cells were observed, and 100 or 200 metaphase cells of each patient were investigated. The background level of dicentric analysis is 1 in 500 metaphase cells. For the TCR mutation assay, we applied the FACS caliber flow cytometer manufactured by Becton Dickinson Co. to measure the CD3-CD4+ mutant frequency. Only 0.1 ml blood were needed and stained with fluorescein-labeled anti-leu3a(CD4) and phycoerythrin-labeled anti-leu4(CD3) antibodies as specified by the supplier (BD Co.). The Mf values were calculated as the number of CD3-CD4+ in the mutant cell windows divided by the total number of CD3-CD4+ T cells in the flow distribution. The average coefficient of variation(CV) on the mutant CD3-CD4+ T cell frequency (x10-4) in 10 normal donors aged 27-50 is 34%. The background rate of CD3-CD4+ mutant cells is 1.16x10-4 on 13 healthy unexposed persons. In general, the results or dicentric analysis and TCR mutation assay with total activity 3.7-27.5 GBq or 131I oral administration on 10 thyroid cancer patients are in coincidence, but the 131I treated the affects the results. The earlier 131I exposure (around 6 years), No. 6, 7, 9 patients showed obviously a decrease in data of TCR mutant. No.7, 8, 9, 10 patients also showed a decrease in TCR rate and no. of dicentric per cell because of the early and long period (on more than 5 years) 131I treatment. But nevertheless the No.10 patient was taken 131I 27.5 GBq total activity still has the highest TCR rates and

  18. Two kinds of biological dosimeters applied to {sup 131}I-treated thyroid cancer patients

    Ma, Ming-Shia; Chen, Li-Hsiang [Health Physics Division, Institute of Nuclear Energy Research, Taiwan (China)

    2000-05-01

    We investigated 10 thyroid cancer patients after {sup 131}I oral medication at the range of (3.7-27.5 GBq) total activity with dicentric chromosome aberration analysis and the T-cell antigen receptor (TCR) mutation assay. We compared and evaluated both methods on their accuracy and applicability. The 10 thyroid cancer patients are at 30-50 years old, and we got 5 ml peripheral blood individually for the investigations. We worked the dicentric aberration analysis with the conventional giemsa method. The first division cells were observed, and 100 or 200 metaphase cells of each patient were investigated. The background level of dicentric analysis is 1 in 500 metaphase cells. For the TCR mutation assay, we applied the FACS caliber flow cytometer manufactured by Becton Dickinson Co. to measure the CD{sub 3}{sup -}CD{sub 4}{sup +} mutant frequency. Only 0.1 ml blood were needed and stained with fluorescein-labeled anti-leu3a(CD{sub 4}) and phycoerythrin-labeled anti-leu4(CD{sub 3}) antibodies as specified by the supplier (BD Co.). The Mf values were calculated as the number of CD{sub 3}{sup -}CD{sub 4}{sup +} in the mutant cell windows divided by the total number of CD{sub 3}{sup -}CD{sub 4}{sup +} T cells in the flow distribution. The average coefficient of variation(CV) on the mutant CD{sub 3}{sup -}CD{sub 4}{sup +} T cell frequency (x10{sup -4}) in 10 normal donors aged 27-50 is 34%. The background rate of CD{sub 3}{sup -}CD{sub 4}{sup +} mutant cells is 1.16x10{sup -4} on 13 healthy unexposed persons. In general, the results or dicentric analysis and TCR mutation assay with total activity 3.7-27.5 GBq or {sup 131}I oral administration on 10 thyroid cancer patients are in coincidence, but the {sup 131}I treated the affects the results. The earlier {sup 131}I exposure (around 6 years), No. 6, 7, 9 patients showed obviously a decrease in data of TCR mutant. No.7, 8, 9, 10 patients also showed a decrease in TCR rate and no. of dicentric per cell because of the early and

  19. Quantitative study about influence of 131I diagnostic dose on uptake of 131I for differentiated thyroid carcinoma

    There are 52 patients with DTC who were referred to our department for radioiodine ablation for the first time were adopted. 30 patients (experimental group) were given a diagnostic scan (Dscan) 24 hours after the administration of 74 MBq 131I before radioiodine therapy, and a therapeutic scan (Tscan) was performed after radioiodine therapy. The fractional concentrations of 131I in remnants or functional metastases were quantified on Dscan and Tscan, and were expressed as Dx and Tx respectively. 22 patients (control group) received 131I therapy directly after thyroidectomy. And Tscan was performed after the radioiodine ablation. As a result the mean Tx (experimental group) was lower both than Dx (experimental group) and Tx (control group). According to the interval time between the diagnostic dose and therapy dose was 1-2, 3-7 and 8-32 days, the experimental group patients were divided into three subgroups A, B, C. The mean Tx/Dx of subgroup B was lower than Tx/Dx of subgroups A and C. There was no statistically significant difference of Tx/Dx between subgroup A and C. In conclusions that 74 MBq 131I for diagnostic scan can cause thyroid stunning. And the stunning effect is more significant when the radioiodine ablation was performed on 3 to 7 days after diagnostic dose. (authors)

  20. Pinhole imaging of 131I-metaiodobenzylguanidine (131I-MIBG) in an animal model of neuroblastoma

    To evaluate 131I-MIBG scintigraphic localization of xenotransplanted and spontaneously arising neuroblastomas in murine models of high-risk neuroblastoma. Neuroblastoma xenografts were created by inoculation of human neuroblastoma cell suspensions into the subcutaneous flanks of athymic nude mice. In addition, spontaneous paraspinal neuroblastomas were detected by direct palpation in MYCN transgenic mice. After measured tumor volumes exceeded 200 mm3, each mouse received an intraperitoneal injection of 18 μCi/g 131I-metaiodobenzylguanidine (131I-MIBG). Pinhole scintigraphy was performed to evaluate the MIBG biodistribution and to attempt to visualize the tumors. Each mouse was imaged on a gamma camera equipped with a 3-mm pinhole on one head and an HEGP collimator on the other. Images demonstrated absorption of radiolabeled MIBG and visualization of tumors. Analysis of the images allowed for quantification of relative MIBG uptake and for determination of linear and area measurements of the tumors. High-energy pinhole imaging effectively demonstrates uptake of radiolabeled MIBG by human neuroblastoma tumors in murine laboratory models. This technique allows for in vivo assessment of tumor burden. In the future, we plan to use this method to evaluate sensitivity for detecting metastatic spread as well as investigating the therapeutic efficacy of high-dose 131I-MIBG in combination with radiosensitizing agents. (orig.)

  1. Effect of antilymphoma antibody, 131I-Lym-1, on peripheral blood lymphocytes in patients with non-Hodgkin's lymphoma.

    Schillaci, Orazio; DeNardo, Gerald L; DeNardo, Sally J; Goldstein, Desiree S; Kroger, Linda A; O'Donnell, Robert T; Lamborn, Kathleen R

    2007-08-01

    Anti-CD20 monoclonal antibodies (mAbs), unlabeled rituximab (Rituxan, Biogen Idec Inc., Cambridge, MA; and Genentech Inc., South San Francisco, CA) or radiolabeled 90Y-ibritumomab (Zevalin, Biogen Idec Inc., Cambridge, MA) and 131I-tositumomab (Bexxar; Glaxo Smith Kline, Research Triangle Park, NC), have proven to be effective therapy for non-Hodgkin's lymphoma (NHL), but also induce immediate and persistent decreases in normal peripheral blood lymphocytes (PBLs). Lym-1, a mAb that selectively targets malignant lymphocytes, also has induced therapeutic responses and prolonged survival in patients with NHL when labeled with iodine-131 (131I). We have retrospectively examined its effect on PBLs in 41 NHL patients that had received 131I-Lym-1 therapy. Absolute lymphocyte counts (ALCs) were evaluated before and after the first and last 131I-Lym-1 infusion. Modest decreases in PBLs were observed in most of the patients. Using strict criteria to define recovery, time to recovery was determined for 19 patients, with the remainder censored because of insufficient follow-up (median follow up for censored patients: 22 days). Using Kaplan-Meier estimates, it would be predicted that 31% of patients would recover by 28 days and that median time to recovery would be 44 days after the last 131I-Lym-1 infusion. No predictors were found for time to recovery, considering such factors as the administered Lym-1 or 131I dose, spleen volume, or radiation doses to the body, marrow, or spleen. The data suggest that the effect of 131I-Lym-1 on ALC is the result of a nonspecific radiation effect, rather than a specific Lym-1 mAb effect. The shorter time required for ALC recovery after 131I-Lym-1 when compared to that reported for anti-CD20 mAbs, whether radiolabeled or otherwise, is probably related to differing mechanisms for lymphocytotoxicity and lesser Lym-1 antigenic density on normal B-lymphocytes. PMID:17803447

  2. Production of 131-I iodide capsules in Argentina

    It is well known that 131I iodide capsules are better suited to be taken by the patient than the corresponding solution. Therefore most Pharmacopeias have monographs for 131I in both pharmaceutical forms: solution or capsules, for diagnosis but principally for therapeutic purposes. In Argentina this radiopharmaceutical has been made commercially available in November 2007. At this time Bacon Laboratories SAIC started its production, authorized by the Health and Nuclear Regulatory Authorities. 131I, in the pharmaceutical form of capsules, have evident advantages in radioprotection for the patients and the personnel involved in its administration. The intake of a 131I provokes frequently that the external part of the mouth (principally if there is a beard and/or a moustache) undergoes an external contamination. This problem is enhanced if the patient has some motor difficulties to take the glass with the solution. In this case he will need assistance from the medical or technical staff, who will receive a much greater radiation dose than in normal cases. In the capsule of 131I iodide, the solution is adsorbed on a sodium phosphate matrix. The capsule is in a plastic tube contained in an appropriate lead shielding. To take the capsule, the patient inclines the open lead shielding containing the capsule in the direction of the mouth. Once the capsule is in the mouth it is swallowed with a little portion of water. After its intake, the radiopharmaceutical is absorbed from the gastrointestinal tract. If a patient is unable to carry out the intake, the assistance by medical or technical staff is easy with practically no radiation harm, since the 131I is shielded by an adequate lead thickness. It is evident that the hands and external face of the patient are also protected since no possibility of contamination exists. The aim of this work is to present the production procedure, the packaging of the capsules and the decrease of the dose received by the involved personnel

  3. Matched pairs dosimetry: {sup 124}I/{sup 131}I metaiodobenzylguanidine and {sup 124}I/{sup 131}I and {sup 86}Y/{sup 90}Y antibodies

    Lopci, Egesta; Fanti, Stefano [Policlinico S.Orsola-Malpighi and University of Bologna, Bologna (Italy); Chiti, Arturo; Pepe, Giovanna; Antunovic, Lidija [IRCCS Humanitas, Nuclear Medicine, Rozzano, MI (Italy); Castellani, Maria Rita; Bombardieri, Emilio [Istituto Nazionale per lo Studio e la Cura dei Tumori, Milan (Italy)

    2011-06-15

    The technological advances in imaging and production of radiopharmaceuticals are driving an innovative way of evaluating the targets for antineoplastic therapies. Besides the use of imaging to better delineate the volume of external beam radiation therapy in oncology, modern imaging techniques are able to identify targets for highly specific medical therapies, using chemotherapeutic drugs and antiangiogenesis molecules. Moreover, radionuclide imaging is able to select targets for radionuclide therapy and to give the way to in vivo dose calculation to target tissues and to critical organs. This contribution reports the main studies published on matched pairs dosimetry with {sup 124}I/{sup 131}I- and {sup 86}Y/{sup 90}Y-labelled radiopharmaceuticals, with an emphasis on metaiodobenzylguanidine (MIBG) and monoclonal antibodies. (orig.)

  4. Specific energy from Auger and conversion electrons of 131I, 188Re-anti-CD20 to a lymphocyte's nucleus

    Torres-García, E.; Carrillo-Cazares, T. A.

    2011-01-01

    The typical radionuclides used to label anti-CD20 in the treatment of non-Hodgkin's lymphoma are 90Y, 131I, and 188Re, with the emission of beta particles, Auger electrons, and conversion electrons for the latter two. The aim of the present work was to calculate the contribution of high linear energy transfer radiation as Auger electrons (AE) and conversion electrons (CE) of 131I and 188Re-anti-CD20 to mean specific energy into the cell nucleus by Monte Carlo simulation (MCS), so as to infer therapeutic effectiveness on a dosimetric basis. MCS was used to quantify the frequency-mean specific energy into the cell nucleus, where the cell was modeled by two concentric spheres, considering two cell models. The results showed that 10% and 33% of the mean-specific energies (z¯) per disintegration imparted to the cell nucleus for both geometries are due to AE and CE; on the other hand, if the hit of AE and CE occurs, the contribution to (z¯) is about 64% and 86% for 131I and 188Re, respectively. According to the amount of specific energy from AE and CE into the cell nucleus by positive event, they can cause catastrophic effects in the nuclear DNA in the treatment of non-Hodgkin's lymphoma with 131I, 188Re-anti-CD20.

  5. Hypothyroidism caused by 131I treatment for Graves disease

    The refollow-up has been carried out in hypothyroidism caused by 131I treatment for Graves disease. The serum HS-TSH(IRMA), FT3, TSH(RIA), TT3, TT4, FT4I, MCA, TGA, Cholesterol and Triglyceride has been measured in 26 patient after 131I treatment for 9.5 years in average. At the same time TRH stimulation test was also performed, and the clinical symptoms and signs assessed. The results showed that TSH is the most sensitive criterion for hypothyroidism, followed by Cholesterol and FT4I. The occurence of hypothyroidism may be related to the presence of thyroid antibody as demonstrated by the elevation of serum MCA, TGA. Therefore measurement of serum TSH, FT4I and Cholesterol during long term follow-up is beneficial for early diagnosis of hypothyroidism and evaluating the effect of substitution treatment

  6. Cancer of the thyroid and 131I fallout in Norway

    From 1953 to 1962 Norway received relatively high levels of radioactive fallout. On the basis of extensive measurements in air, precipitation, food and humans, the dose to the thyroid due to 131I has been calculated. Cancer registration in Norway is practically completely efficient because of obligatory notification of the Cancer Registry by physicians, pathology laboratories, and the Central Bureau of Statistics of all cases or death certificates concerning cancer. Analysis of the Cancer Registry data from 1953 to 1980 concerning birth cohorts 1936 to 1961 indicates an overall increasing trend in thyroid cancer morbidity, most pronounced in female cohorts born 1930-50. The highest, most abrupt irregularities reveal a coincidence of high numbers with high 131I content in milk consumed during the years of prepuberty and puberty. Possible interpretations are discussed. (author)

  7. Preparation of an imaging agent for cerebral muscarinic acetylcholine receptor, (R,S)131I-QNB

    2003-01-01

    The method to synthesize a high affinity muscarinic receptor antagonist (R,S)I-QNB[(R)-(-)-1-azabicyclo [2,2,2]oct-3-yl-(S)-(+)-α-hydroxy-α-(4-[127I]iodophenyl)-α-phenyl acetate] from 4-nitrobenzophenone with improvement compared to literatures was reported in this article. IR, MS and 1HNMR characterized the final product. (R,S)131I-QNB was prepared using Cu(I) assisted iodine exchange labeling, and showed by TLC that the radiolabeling yield(RLY) was over 80%, and radiochemical purity(RCP) was over 95%. Stability of the labeled compound was also determined. It was found that (R,S)131I-QNB dried by nitrogen blowing can stay at 4-10℃ for a week without change of RCP.

  8. 131I-19-iodocholesterol scintigraphy and suprarenal pathology

    The methods used and results obtained by 131I-19-iodocholesterol scintigraphy (dose 2mCi) are given for 24 patients with various kinds of suprarenal hyperactivity (primary hyperaldosteronism, Cushing's syndrome, malignant adrenocortical tumour, pheochromocytoma). The morphological and quantitative aspects of suprarenal scintigraphy are examined. A technique to determine the iodocholesterol uptake ratio of the two adrenal glands, considered more important than the fixation rate of each is described

  9. Hypertension complicating 131I-meta-iodobenzylguanidine therapy for neuroblastoma

    Radiolabelled meta-iodobenzylguanidine (mIBG), used as targeted therapy for neuroblastoma, is known to have effects on blood pressure (BP). In this study we audited BP changes in patients receiving 131I-mIBG therapy for neuroblastoma to identify BP-related adverse events (AE) and possible predictive factors. Between 2003 and 2010, 50 patients with neuroblastoma received 110 131I-mIBG administrations. BP measurements before and after administration were compared with age- and sex-matched centile values. AE were analysed, and possible predisposing factors identified. This population had a baseline BP distribution higher than that of their age- and sex-matched peers, with 16% of preadministration systolic BP values above the 95th centile. Changes in BP after administration showed an approximately normal distribution with similar numbers of reduced and increased values. Four AE, all related to hypertension, occurred with one patient having generalized seizures. One AE was immediate, others occurred between 20 and 25 h after administration. No significant association between AE and patient age or sex was demonstrated. However, a significant association between AE and high preadministration BP was shown, both above the 90th centile (p = 0.0022) and above the 95th centile (p = 0.0135). Clinically relevant hypertension following 131I-mIBG therapy affected less than 5% of administrations, but was more common in those patients with preexisting hypertension. As hypertensive episodes may occur many hours after treatment, close monitoring of BP needs to be continued for at least 48 h after administration of 131I-mIBG. (orig.)

  10. Radiological data of the animal experimentation with 131I in cancer gene therapy studies

    The Na/I symporter (NIS) gene is expressed mainly in the thyroid and is responsible for iodide accumulation in this organ. Historically, radioiodine (131I) is used for the treatment of thyroid cancer as a result of native thyroidal expression of NIS. Currents studies of gene therapy experimentation carried out with animal models have allowed the expression of the NIS gene in various types of non thyroid cancer (prostate, lung, breast) making it possible the iodide uptake in these cancer and the therapeutic use of 131I. In the Instituto de Investigaciones Biomedicas 'Alberto Sols' (CSIC - UAM) different studies of gene therapy experimentation have been carried out in animal models, using the Na/I symporter (NIS). In the first place the non thyroid cancer is induced in the nude mice, then, Adenovirus (as expression vector) infection allows the NIS gene expression. Finally, the 131I is administrated to the animals. This therapeutic use of 131I may cause in some cases tumor regression or reduction in tumor volume. The therapeutic label of nude mice using the solution containing Na 131I involves irradiation risk due to the radionuclide (iodine-131 is a high-energy gamma emitter) and the amount of activity used (in the range of MBq). Besides, there is a contamination risk caused by the administration of unsealed radionuclide and animal models handling (bites, aerosols, etc.). A specific radiological procedure is applied during the technique development. This document established, among others aspects, the protection measurements to reduce the exposure of workers and public and the contamination and radiation measurements. The monitoring for external exposure has been carried out using TLD dosimeters and making radiation measurements in realtime, during the technique development. Monitoring of radiation dose of different workplaces (controlled areas and public areas) has been carried out using TLD dosimeters. The aim of this work has been to collect and to analyse the

  11. Changes in percentage of lymphocyte subsets after 131I treatment in patients with differentiated thyroid cancer

    LUO Quan-Yong; CHEN Li-Bo; YU Yong-Li; LU Han-Kui; ZHU Rui-Sen

    2005-01-01

    To monitor the extent and the duration of lymphocyte subset changes in patients with thyroid carcinoma undergoing therapeutic 131I administration, the percentage of lymphocyte subsets were serially analyzed before and after 131I treatment. In patients who received 1850 MBq of 131I for ablation of thyroid remnants, only for NK cells and B cells showed a significant reduction. In patients received 3700 MBq of 131I for treatment of local lymph node metastases, NK cells, B cells and CD4+ were found decreased. In patients received 7400 MBq of 131I for treatment of distant metastases, NK cells, B cells and CD4+ and CD8+ were all affected. However, there is no significant reduction compared to the baseline in the percentage of all lymphocyte subsets three months after 131I treatment. The results show that the sensitivity of lymphocytes to 131I internal radiation depends upon lymphocyte phenotype and 131I activity. The immunosuppression effects are temporary and reversible.

  12. Observation of radioactive iodine ((131)I, (129)I) in cropland soil after the Fukushima nuclear accident.

    Fujiwara, Hideshi

    2016-10-01

    During the early stages of the Fukushima nuclear accident, the temporal variations of (131)I deposited on the ground and of (131)I accumulated in cropland soil were monitored at a fixed location in Japan. Moreover, concentrations of long-lived radioactive iodine ((129)I) in atmospheric deposits and soil were measured to examine the feasibility of retrospectively reconstructing (131)I levels from the levels of accident-derived (129)I. The exceptionally high levels of (131)I in deposits and soil were attributed to rainfall-related deposition of radionuclides. In the crop field studied, the losses of deposited (131)I and (129)I due to volatilization were small. The atomic ratio (129)I/(131)I in the topsoil corresponded to the same ratio in deposits. The (131)I concentrations measured in the topsoil were very consistent with the (131)I concentrations reconstructed from the (129)I concentrations in the soil. PMID:27320744

  13. The clinical significance of measuring the thyroid 131I uptake rate to identify the type of premature hypothyroidism for hyperthyroid after 131I treatment

    The 3 h thyroid 131I uptake rate and the content of serum TT3, TT4, TSH are measured in 63 patients of premature hypothyroidism (consisting of 33 provisional hypothyroids and 30 perpetual hypothyroidism) before and after thyroxine substitutes treatment for six moths. The results show that there is obvious difference in 131I uptake rate compared provisional hypothyroidism with perpetual hypothyroidism, and no difference in the content of serum TT3, TT4, TSH before the treatment. Compared with normal conditions, there is no difference in 131I uptake rate of provisional hypothyroidism, but the 131I uptake rate of perpetual hypothyroidism has obvious decrease before and after the treatment. Therefore the type of patients who suffer from premature hypothyroidism can be distinguished according to the 131I uptake rate: if the 3 h thyroid 131I uptake rate is normal, it is provisional hypothyroidism; if not, it is perpetual hypothyroidism

  14. The development and current status of 131I treatment for hyperthyroidism

    Hyperthyroidism is an autoimmune diseasein which excessive amounts of thyroid hormones circulate in the blood. The treatments for hyperthyroidism mainly include antithyroid drugs, 131I treatment, and surgery. 131I had been verified as an effective, safe, simple method to treat adult and children hyperthyroidism. Current research trends of 131I treatment mainly are problems of 131I treatment of hyperthyroidism and its long-term security. (authors)

  15. Superparamagnetic iron oxide nanoparticles mediated 131I-hVEGF siRNA inhibits hepatocellular carcinoma tumor growth in nude mice

    Hepatocellular carcinoma (HCC) is a primary liver tumor and is the most difficult human malignancy to treat. In this study, we sought to develop an integrative approach in which real-time tumor monitoring, gene therapy, and internal radiotherapy can be performed simultaneously. This was achieved through targeting HCC with superparamagnetic iron oxide nanoparticles (SPIOs) carrying small interfering RNA with radiolabled iodine 131 (131I) against the human vascular endothelial growth factor (hVEGF). hVEGF siRNA was labeled with 131I by the Bolton-Hunter method and conjugated to SilenceMag, a type of SPIOs. 131I-hVEGF siRNA/SilenceMag was then subcutaneously injected into nude mice with HCC tumors exposed to an external magnetic field (EMF). The biodistribution and cytotoxicity of 131I-hVEGF siRNA/SilenceMag was assessed by SPECT (Single-Photon Emission Computed Tomography) and MRI (Magnetic Resonance Imaging) studies and blood kinetics analysis. The body weight and tumor size of nude mice bearing HCC were measured daily for the 4-week duration of the experiment. 131I-hVEGF siRNA/SilenceMag was successfully labeled; with a satisfactory radiochemical purity (>80%) and biological activity in vitro. External application of an EMF successfully attracted and retained more 131I-hVEGF siRNA/SilenceMag in HCC tumors as shown by SPECT, MRI and biodistribution studies. The tumors treated with 131I-hVEGF siRNA/SilenceMag grew nearly 50% slower in the presence of EMF than those without EMF and the control. Immunohistochemical assay confirmed that the tumor targeted by 131I-hVEGF siRNA/SilenceMag guided by an EMF had a lower VEGF protein level compared to that without EMF exposure and the control. EMF-guided 131I-hVEGF siRNA/SilenceMag exhibited an antitumor effect. The synergic therapy of 131I-hVEGF siRNA/SilenceMag might be a promising future treatment option against HCC with the dual functional properties of tumor therapy and imaging

  16. The success of 131I ablation in thyroid cancer patients is significantly reduced after a diagnostic activity of 40 MBq 131I

    Objective: Dosimetry studies have shown that activities of 131I as small as 10-20 MBq may cause a stunning effect. A result of this stunning effect may be a lower success rate of the ablative 131I therapy for differentiated thyroid carcinoma (DTC). The aim of this study was to determine whether pre-therapeutic uptake measurement with 40 MBq 131I causes a lower success rate of ablation. Design: retrospective chart review study. Patients, methods: In two hospitals the ablation protocols differed in one respect only: in the one hospital no diagnostic 131I was applied before ablation (group 1, n = 48), whereas in the other hospital a 24-h uptake-measurement with 40 MBq 131I was performed (group 2, n = 51). Included were all DTC patients without distant metastases who had undergone 131I ablation between July 2002 and December 2005, and who had returned for 131I follow-up. Successful ablation was defined as absence of pathological 131I uptake on diagnostic whole-body scintigraphy and undetectable thyroglobulin-levels under TSH stimulation. Results: Overall, ablation was successful in 31/48 patients (65%) in group 1 and in 17/51 patients (33%) in group 2 (p=0.002). Multivariate analysis showed that pre-therapeutic uptake measurement using 40 MBq 131I was an independant determinant for success of ablation (p = 0.002). Conclusions: After applying a diagnostic activity of 40 MBq 131I before ablation, the success rate of ablation is severely reduced. Consequently, the routine application of 131I for diagnostic scintigraphy or uptake measurement prior to 131I ablation is best avoided. (orig.)

  17. Comparative biodistribution profile of [131I]VIP and [131I]VIP10-28

    Maria Tereza Colturato

    2005-10-01

    Full Text Available Various tumor cells express significantly higher amounts of VIP receptors (VIPR that provided the basis for the clinical use of radiolabeled VIP for the in vivo localization of tumors. This work studied the labeling of VIP and VIP10-28 with iodine-131 to compare the biological distribution of the labeled compounds in Nuce mice and the affinity for tumor cells. Both VIP and VIP10-28 peptides contain two tyrosine residues, in positions 10 and 22, that are theoretically equally susceptible to radioiodination employing oxidative electrophilic substitution using oxidizing agents like Chloramine T. Radiochemical purity of the reaction mixture was determined by electrophoresis and HPLC. The VIP peptide and the fragment were labeled with radioiodine with good radiochemical yield (above 96%. Suitable, but important differences can be observed in biological distribution studies. Comparatively, blood clearance was faster for labeled VIP and perhaps because of this, the uptake in tumor was lower, especially during the first hour. These differences observed in the biological distribution of the compounds can be related to the lipophilicity of the labeled compounds.Várias células tumorais expressam significantemente uma alta quantidade de receptores VIP (VIPR que determinam a base para o uso clínico de VIP radiomarcado para localização de tumores in vivo. Foi estudado neste trabalho a marcação do VIP e do fragmento VIP10-28 com iodo-131 comparando a distribuição biológica dos compostos marcados em camundongos Nude e sua afinidade pelas células tumorais. Ambos os peptídeos, VIP e VIP10-28. contém dois resíduos de tirosina nas posições 10 e 22, que teoricamente são igualmente susceptíveis pela substituição eletrofílica oxidativa do radioiodo utilizando Cloramina T como agente oxidante. A pureza radioquímica da mistura de reação foi determinada por eletroforese e cromatografia líquida de alta eficiência (CLAE. O VIP e fragmento foram

  18. Early Tumor Response to Hsp90 Therapy Using HER2 PET: Comparison with 18F-FDG PET

    Smith-Jones, Peter M.; Solit, David; Afroze, Farzana; Rosen, Neal; Larson, Steven M.

    2006-01-01

    We compared 68Ga-DOTA-F(ab′)2-herceptin (DOTA is 1,4,7,10-tetraazacyclododecane-N,N′,N″,N‴-tetraacetic acid [HER2 PET]) and 18F-FDG PET for imaging of tumor response to the heat shock protein 90 (Hsp90) inhibitor 17-allylamino-17-demethoxygeldanamycin (17AAG).

  19. Quantitative evidence of thyroid stunning in 131I cancer treatment

    Background: An obvious paradox remains in the diagnosis, treatment and follow-up of differentiated thyroid cancer by 131I. The higher the activity for raising diagnostic precision, the greater is the potential reduction in therapeutic effects. This is due to a phenomenon called thyroid stunning. MATERIAL AND METHODS: 131I tracer and therapeutic parameters: uptake, effective half-life and thyroid remnants mass were compared in two different groups of patients. Pre-treatment planning of radioiodine (RI) ablation was performed in 30 patients after administration of 0,185-74 MBq. The same parameters comparison was performed in the second group of four cases. They received two or three single fractions of 600-2400 MBq 3-15 days apart (a long-term abandoned regime). RESULTS: 1. Comparative data collected by pre-treatment planning and subsequent RI administration supported the thesis that low range tracer activity (0.7-74 MBq) does not cause thyroid stunning. We have registered higher or similar uptake in thyroid bed after 1100-3700 MBq in 90% of cases. Only in 10% of cases was therapeutic uptake lower than the tracer one. In 18% of patients the higher rate of uptake was associated with additional thyroid tissue visualized on the post-treatment scan. Half-life reduction only could be interpreted in the direction of stunning, but such changes characterizes every RI treatment, if it takes more than one administration. Data elucidate why our pre-treatment planning failed in one-third of the patients. 2. We have clearly observed thyroid stunning after 600-2400 MBq 131I. In one case only, even after 1200 MBq, stunning did not take place. Individual RI kinetics appear highly unpredictable. The author advocates avoiding high activity first pre-treatment scan in advanced cases with elevated thyroglobuline. It remains an unanswered question what time is necessary for stunning to recover. (author)

  20. Efficacy analysis of 131I in treatment of hyperthyroidism with periodic paralysis

    To evaluate therapeutic effect of 131I in thyrotoxic periodic paralysis (TPP), the serum TT3, TT4, FT3 and FT4 in TPP Patients before and after treatment with 131I were detected. The results showed that the serum potassium was decreased and serum TT3, TT4, FT3 and FT4 in those patients were increased. The cure rates in 8 TPP were 75% and 100% after 6 and 12 months treatment with 131I respectively. 131I treatment was a good therapeutic effect with short course and high cure rate. 131I is the first choice for the treatment of patients with TPP. (authors)

  1. Determination of 129I in 131I-pharmaceuticals produced in THOR

    131I is one of the most important radionuclides used in nuclear medicine. The accompanying isotope 129I with insignificant activities in 131I-pharmaceuticals, produced in THOR, were determined in terms of 129I/131I ratio by neutron activation analysis. The detection limit of 129I can be lowered to order of 0.1 Bq, superior to conventional radiometric methods. The 129I/131I ratios in the 131I-pharmaceuticals, were measured to be in the range from 3.9 to 8.3

  2. Interventional therapy for human breast cancer in nude mice with 131I gelatin microspheres (131I-GMSs) following intratumoral injection

    The aim of this study was to investigate the effects of 131I gelatin microspheres (131I-GMS) on human breast cancer cells (MCF-7) in nude mice and the biodistribution of 131I-GMSs following intratumoral injections. A total of 20 tumor-bearing mice were divided into a treatment group and control group and received intratumoral injections of 2.5 mci 131I-GMSs and nonradioactive GMSs, respectively. Tumor size was measured once per week. Another 16 mice received intratumoral injections of 0.4 mci 131I-GMSs and were subjected to single photon emission computed tomography (SPECT) scans and tissue radioactivity concentration measurements on day 1, 4, 8 and 16 postinjection. The 20 tumor-bearing mice received intratumoral injections of 0.4 mci [131I] sodium iodide solution and were subjected to SPECT scans and intratumoral radioactivity measurements at 1, 6, 24, 48 and 72 h postinjection. The tumors were collected for histological examination. The average tumor volume in the 131I-GMSs group on post-treatment day 21 decreased to 86.82 ± 63.6%, while it increased to 893.37 ± 158.12% in the control group (P < 0.01 vs. the 131I-GMSs group). 131I-GMSs provided much higher intratumoral retention of radioactivity, resulting in 19.93 ± 5.24% of the injected radioactivity after 16 days, whereas the control group retained only 1.83 ± 0.46% of the injected radioactivity within the tumors at 1 h postinjection. 131I-GMSs suppressed the growth of MCF-7 in nude mice and provided sustained intratumoral radioactivity retention. The results suggest the potential of 131I-GMSs for clinical applications in radiotherapy for breast cancer

  3. Toxicity of upfront {sup 131}I-metaiodobenzylguanidine ({sup 131}I-MIBG) therapy in newly diagnosed neuroblastoma patients: a retrospective analysis

    Bleeker, Gitta; Schoot, Reineke A.; Caron, Huib N.; Kraker, Jan de; Tytgat, Godelieve A. [Emma Children' s Hospital, Academic Medical Centre (AMC), Department of Paediatric Oncology, PO Box 22700, Amsterdam (Netherlands); Hoefnagel, Cees A. [National Cancer Institute (NKI-AvL), Department of Nuclear Medicine, Amsterdam (Netherlands); Eck, Berthe L. van [Academic Medical Centre (AMC), Department of Nuclear Medicine, Amsterdam (Netherlands)

    2013-10-15

    In the treatment of patients with high-risk neuroblastoma, different doses of {sup 131}I-metaiodobenzylguanidine ({sup 131}I-MIBG) are administered at different time points during treatment. Toxicity, mainly haematological (thrombocytopenia), from {sup 131}I-MIBG therapy is known to occur in extensively chemotherapy pretreated neuroblastoma patients. Up to now, acute toxicity from {sup 131}I-MIBG as initial treatment has never been studied in a large cohort. The aim of this retrospective study was to document acute toxicity related to upfront {sup 131}I-MIBG. All neuroblastoma patients (stages 1-4 and 4S) treated upfront with {sup 131}I-MIBG at the Emma Children's Hospital, Academic Medical Centre (1992 - 2008) were included in this retrospective analysis. The acute toxicity (during therapy) and short-term toxicity (1st month following therapy) of the first two {sup 131}I-MIBG therapies were studied. Of 66 patients (34 boys, 32 girls; median age 2.2 years, range 0.1 - 9.4 years), 49 had stage 4 disease, 5 stage 4S, 6 stage 3, 1 stage 2 and 5 stage 1. The median first dose was 441 MBq/kg (range 157 - 804 MBq/kg). The median second dose was 328 MBq/kg (range 113 - 727 MBq/kg). The most frequently observed symptoms were nausea and vomiting (21 %, maximum grade II). The main toxicity was grade IV haematological, occurring only in stage 4 patients, after the first and second {sup 131}I-MIBG therapies: anaemia (5 % and 4 %, respectively), leucocytopenia (3 % and 4 %) and thrombocytopenia (2 % and 4 %). No stem cell rescue was needed. The main acute toxicity observed was haematological followed by nausea and vomiting. One patient developed posterior reversible encephalopathy syndrome during {sup 131}I-MIBG therapy, possibly related to {sup 131}I-MIBG. We consider {sup 131}I-MIBG therapy to be a safe treatment modality. (orig.)

  4. A Comparative Study of {sup 131}I-Hippuran Renogram, {sup 131}I-Hippuran Urinary Excretion Test and Intravenous Pyelogram in Obstructive Uropathy due to Cancerous Invasion

    Park, Kee Bok; Rhee, Chong Heon; Hong, Chang Gi; Park, Soo Seong; Koh, Chang Soon [Radiological Research Institue, Seoul (Korea, Republic of)

    1968-03-15

    A comparative study of {sup 131}I-hippuran renogram, {sup 131}I-hippuran excretion test and intravenous pyelogram were performed in 61 cases of gynecological cancer. The following were the results: 1) Among 40 cases of cervix cancer showing normal excretory urography 7 cases (17.5%) were found to have unilateral or bilateral delayed excretory pattern on {sup 131}I-hippuran renogram and on the contrary only 2 cases (5.7%) showed a mild caliectatic change on excretory urography among 35 cases of gynecological cancer showing normal pattern of {sup 131}I-hippuran renogram. 2) In the group showing unilateral of bilateral delayed excretory pattern of {sup 131}I-hippuran renogram there was a reduction of {sup 131}I-hippuran excretion in the first 20 minutes, but there was no significant difference of {sup 131}I-hippuran excretion in 60 minutes compared with that of normal renogram group. 3) In the group showing unilateral non-functioning pattern of {sup 131}I-hippuran renogram in one side and normal pattern in the other side there was found to be no difference in {sup 131}I-hippuran excretion amount compared with that of normal renogram group. 4) It was evident from these experimental study that {sup 131}I-hippuran renogram was considered as a good examination method for the evaluation of obstructive uropathy, and if one side kidney was intact it might compensate for the other diseased kidney so far as to renal excretory function. It was also shown that the more severe the cancerous spread in the pelvic wall the more changes on {sup 131}I-hippuran renogram.

  5. A Comparative Study of 131I-Hippuran Renogram, 131I-Hippuran Urinary Excretion Test and Intravenous Pyelogram in Obstructive Uropathy due to Cancerous Invasion

    A comparative study of 131I-hippuran renogram, 131I-hippuran excretion test and intravenous pyelogram were performed in 61 cases of gynecological cancer. The following were the results: 1) Among 40 cases of cervix cancer showing normal excretory urography 7 cases (17.5%) were found to have unilateral or bilateral delayed excretory pattern on 131I-hippuran renogram and on the contrary only 2 cases (5.7%) showed a mild caliectatic change on excretory urography among 35 cases of gynecological cancer showing normal pattern of 131I-hippuran renogram. 2) In the group showing unilateral of bilateral delayed excretory pattern of 131I-hippuran renogram there was a reduction of 131I-hippuran excretion in the first 20 minutes, but there was no significant difference of 131I-hippuran excretion in 60 minutes compared with that of normal renogram group. 3) In the group showing unilateral non-functioning pattern of 131I-hippuran renogram in one side and normal pattern in the other side there was found to be no difference in 131I-hippuran excretion amount compared with that of normal renogram group. 4) It was evident from these experimental study that 131I-hippuran renogram was considered as a good examination method for the evaluation of obstructive uropathy, and if one side kidney was intact it might compensate for the other diseased kidney so far as to renal excretory function. It was also shown that the more severe the cancerous spread in the pelvic wall the more changes on 131I-hippuran renogram.

  6. Effects of oral contraceptives on thyroid tests using 131I

    The effect of oral contraceptives on 131I uptake, the depuration rate of this isotope and the PBI was studied in 24 euthyroid female patients. The dose administered was of 2.5 mg of norestinodrel and 0.05 mg of ethynil estradiol. The data were submitted to a statistical study applying analysis of variance, comparison of the means, determination of the standard deviations and the confidence interval. It is concluded that drug does affect thyroid function and that these effects may cause certain disturbances, as arterial hypertension, thrombosis, etc., in patients under prolonged contraceptive treatment

  7. Pharmacokinetic studies of 131I-stevioside and its metabolites

    131I-STEVIOSIDE (1.10 MBq) was injected i.v in Wistar male rats, in distribution in the body and metabolism were studied. The highest concentration of radioactivity was observed in the liver and in the small intestine after 10 and 120 minutes, respectively. At 2 h after injection, the radioactivity eliminated in the bile was 52.0% of the original dose. The results of RP-HPLC analysis of the bile showed that stevioside was degraded in vivo and that steviol appeared as a major metabolite. However, in the urine; RP-HPLC analysis did not show the presence of steviol

  8. Treatments with radioactive iodine, 131 I. How, when and where?

    A great variety of approaches exists in the application of the treatments with radioactive materials, as the 131I, but it is necessary to standardize them for the patient's benefit, because their doctor doesn't always know the principle that it bases this therapy, called metabolic therapy or radioiodine therapy (RYT). In this work the experience that was acquired by more of 50 years of RYT management in the Thyroid and Nuclear Medicine Clinic in patients with thyroid pathologies is informed, so that their management fulfills its function and it was carried out inside the corresponding juridical frame and the physicochemical and endocrinological principles that should take implicit. (Author)

  9. Simulation of 131I emergency emission. processes of dose formation

    Kinetics of 131I and dose formation in tissues and organs of laboratory Wistar rats in a simulation of long entry of the isotope were studied. The function of weight of the thyroid gland changes due to accumulation of absorbed dose in the body was optimized. Maximum activity of the initial ingestion of the isotope in the body, above which the thyroid tissue loses its ability to retain iodine was substantiated. Residual thyroid tissue mass after radiation damage was estimated. Features of the processes of dose formation in other tissues and organs were described

  10. Evaluation of irradiation in patient's environment receiving 131I therapy

    This article describes measurements made in the bed station of Clinic of Nuclear Medicine in St. Elizabeth Oncological Institute in Bratislava. There are treated thyroid cancer and thyrotoxicosis with the use of 131I. The aim of the measurements was to determine the possibility of the ambulation treatment of thyrotoxicosis or the possibility of shortening of the patient;s stay in the bed station that the effective dose would not be exceeded suggestions according to the publication of EURATOM. The measurements were made also with thyroid cancer patients but owing to clinical reasons the ambulation treating in this case is not permissible. Therefore this article does not describe the results of these measurements.The effective dose rates were measured in 0.25 m; 0.5 m; 1 m and 2 m distances from the patient's thyroid so the effective dose in the patient's surroundings could be determined. To the present time the results of effective dose rates measurements for 17 patients were evaluated by described way. The age of the patients was from 41 to 82 years, the administered quantity of 131I was from 259 to 481 MBq, in fractions 37 MBq, 74 MBq, or 111 MBq. The calculated effective half-life of 131I excretion from the patients body is crucial for the length of patient's necessary staying in the bed station, were from 4.2 days to 8 days. This great extend of values is given by by the different clinical parameters of the treated patients. After the analyse of them can be said that the effective half-life increases, when the patient is elder, has greater mass of thyroid and the accumulation is higher. At the present time authors don't suggest using the ambulation treatment of thyrotoxicosis by 131I. For discharging the patient from the hospital authors suggest to think criteria according to the model of behaviour D with the effective dose limit 0.5 mSv. For the households with children up to 2 years and/or pregnant women according to the model B with effective dose limit 0

  11. The therapeutic effect of different dose 131I on hyperthyroidism

    1228 hyperthyroidism patients treated with two doses of 131I 3.7-4.4 MBq/g and 2.59-3.96 MBq/g are observed and the results are compared. The results indicate that the administered dose is larger the treating rate is higher, and hypothyroidation occurs frequently; while the dose is lower, the treating rate and hypothyroidation is also getting lower. So, there are some other factors of the indication selection, the estimation of thyroidism size, individual sensitively and the hyperthyroidism nature history and so on should be considered in the hyperthyroidism therapy for improving the therapeutic effect

  12. Effect of irradiation combined with 131I-chTNT on lewis tumor of mice

    Objective: To investigate the biodistribution and scintigraphy of Lewis carcinoma of mice with 131I-chTNT combined with or without irradiation, and to study the effects on the tumor growth of mice. Methods: When the tumor size in C57 mice bearing Lewis carcinoma in the right leg was big enough, the mice were randomly divided into different groups to receive different treatment. The biodistribution and scintigraphy of 131I-chTNT were observed at various time after tail-intravenous injection in tumor-bearing mice. The effect of treatment was assessed by tumor growth delay. Results: The uptake of 131I-chTNT in tumor tissue was significantly higher in combined group than in 131I-chTNT group (P0.05). The scintigraphy result showed higher tumor accumulation of 131I-chTNT in combined group than that in 131I-chTNT group. The absolute growth delay for irradiation group, 131I-chTNT group and the combined group was 9.1, 3.1 and 13.1 days, respectively. The nominal growth delay was 10 days, and the enhancement factor of 131I-chTNT for RT was 1.08. Conclusions: 131I-chTNT combined with irradiation can increase the uptake of 131I-chTNT in tumor without side effects. 131I-chTNT can enhance the radiotherapeutic effect for tumor-bearing mice. (authors)

  13. The hepatic excretion of 131I-rose bengal and sup(99m)Tc-IDA derivatives in Rotor's syndrome

    Bilirubin kinetics and hepatobiliary excretion of some exogenous anions (BSP, 131I-rose bengal, diethyl and parabutyl-IDA labeled with sup(99m)Tc) were studied in three patients presenting with Rotor's syndrome. Two were brothers; a noja undiced fraternal twin of one of them was also evaluated. The hepatic clearance of the radiopharmaceuticals was imparired in the affected patients but the degree of impairment was different among the tested anions, i.e., maximal for 99Tc-diethyl-IDA and minimal for 131I-rose bengal. Parabutyl-IDA was cleared better than the diethyl derivative. The metabolic derangement seems to be the level of transfer from plasma to liver and of the hepatic storage, rather than at the level of hepatocyte excretory pathways, as in the case of Dubin-Johnson syndrome. (orig.)

  14. Diagnosis of pheochromocytome by 131-I-MIBG

    The purpose of this project is to evaluate the specificity and sensitivity of 131-I-metaiodobenzylguanidine (MIBG), a newly developed radiopharmaceutical which accumulated in the neuro transmitter adrenergic sacs, in diagnosing pheochromocytomes, which originate from well-differentiated cells in the adrenergic region of the autonomous nervous system. A sizeable number of these cells appear in the adrenal medulla, the para-spinal ganglion and the para-aortic (Organ of Zuckerkandl), however, a certain number of pheochromocytomes are found in other sites including the bladder, heart and vagus nerves. Adrenergic tumors which are located outside the adrenal medulla and which secrete both norepinephrine and epinephrine are called pheochromocytomes. Scintigraphic distribution of 131-I-MIBG, an imaging agent for the adrenal medulla, was studied to determine the uptake in patients suspected of harboring pheochromocytomes. Normal distribution of the radiotracer includes: the salivary glands, liver, spleen, gall-bladder, kidneys and heart. Accumulations in the thyroids are detected only in cases of inadequate thyroid blocking. Injected were 0.5 mCi/1.7 m2 and scans taken 24, 48 and 72 hours afterward. The five patients investigated showed high levels of epinephrine and norepinephrine and revealed abnormal accumulations of radioactive material. These data were surgically verified. (author)

  15. Effect of 131I on the anemia of hyperthyroidism

    Perlman, J.A.; Sternthal, P.M.

    1983-01-01

    Data from the National Thyrotoxicosis Therapy Follow-Up Study (NTTFS) are presented here to document the existence of anemia in hyperthyroidism, a mild and reversible anemia that is simultaneously ameliorated with reversal of the hyperthyroid state. Among 20,600 women entered into the NTTF study with no previous history of hematological disorders, the prevalence of anemia was found to range from 10-15%, appearing to be higher in those selected for treatment with 131I when compared to those selected for surgery. An attempt is made to verify the recent hypothesis that thyroid hormone levels in the supraphysiologic range may suppress erythrogenesis. Two statistically significant regression models are consistent with a hypothesis of thyrotoxic bone marrow suppression. However, both associations are weak enough to suggest that some other physiologic improvement underlies the amelioration of anemia when hyperthyroidism is reversed. The degree of improvement in hematological status is similar for women in both treatment groups. Among 4464 women for whom serial hematological tests are obtained, over 3/4 of anemic patients are no longer anemic after an average 6.2 yr of follow-up. Clinicians are reassured that radioactive iodine exposure causes no further insult to the bone marrow, no matter what the cumulative dosage. The highly fractionated low dose bone marrow exposures to radiation account for the minimal hematological risks of 131I treatment.

  16. Use of gamma probe in 131I thyroid uptake studies

    Evaluation of thyroid uptake by administration of radioactive iodine is a well-defined procedure to assess patient thyroid function. In general, nuclear medicine institutions use gamma cameras coupled to pinhole collimators to perform uptake studies. With the growing use of intraoperative gamma probes in the radioguided surgical techniques, several institutions are purchasing this new and portable equipment, which can technically be also employed to assess patient's thyroid function, permitting further other applications of gamma cameras. The aim of the study was to compare thyroid uptake trails carried out with both gamma camera and intraoperative gamma probe, in order to evaluate the possible use of gamma probe for this purpose. At first a preliminary study of feasibility was carried out using a neck phantom to verify equipment efficiency with known activities of 131 I. Henceforth, work data from 12 patients undergone studies of thyroid uptakes were evaluated, 24 hours after oral administration of 370 kBq of 131 I. The maximum difference observed between the values obtained with both equipment was 60%, which demonstrated the feasibility of the proposed protocol and made clear that gamma probe can be useful for thyroid uptake studies. (author)

  17. Effect of 131I on the anemia of hyperthyroidism

    Data from the National Thyrotoxicosis Therapy Follow-Up Study (NTTFS) are presented here to document the existence of anemia in hyperthyroidism, a mild and reversible anemia that is simultaneously ameliorated with reversal of the hyperthyroid state. Among 20,600 women entered into the NTTF study with no previous history of hematological disorders, the prevalence of anemia was found to range from 10-15%, appearing to be higher in those selected for treatment with 131I when compared to those selected for surgery. An attempt is made to verify the recent hypothesis that thyroid hormone levels in the supraphysiologic range may suppress erythrogenesis. Two statistically significant regression models are consistent with a hypothesis of thyrotoxic bone marrow suppression. However, both associations are weak enough to suggest that some other physiologic improvement underlies the amelioration of anemia when hyperthyroidism is reversed. The degree of improvement in hematological status is similar for women in both treatment groups. Among 4464 women for whom serial hematological tests are obtained, over 3/4 of anemic patients are no longer anemic after an average 6.2 yr of follow-up. Clinicians are reassured that radioactive iodine exposure causes no further insult to the bone marrow, no matter what the cumulative dosage. The highly fractionated low dose bone marrow exposures to radiation account for the minimal hematological risks of 131I treatment

  18. Radiosynthesis of [131I]IAZGP via nucleophilic substitution and its biological evaluation as a hypoxia marker - is specific activity a factor influencing hypoxia-mapping ability of a hypoxia marker?

    Introduction: The hypoxia marker IAZGP, 1-(6-deoxy-6-iodo-β-D-galactopyranosyl)-2-nitroimidazole, has been labeled with 123I/124I/125I/131I via iodine-radioiodine exchange, which gives the radiotracer in a specific activity of 10-90 MBq/μmol. We synthesized the same radiotracer possessing several hundred to thousand times higher specific activity (high-SA IAZGP) via nucleophilic substitution and compared its biological behavior with that of conventionally produced IAZGP (low-SA IAZGP) to determine if specific activity is a factor influencing cell uptake kinetics, biodistribution and intratumor microregional localization of the radiotracer. Methods: High-SA [131I]IAZGP was prepared by substitution of the tosyl functionality with [131I]iodide. In vitro uptake of high- and low-SA [131I]IAZGP by HCT8 and HT29 cells was assessed in normoxic and hypoxic conditions. Biodistribution and intratumor localization of high- and low-SA [131I]IAZGP were determined by injection into HT29 tumor-bearing mice. Results: The nucleophilic substitution reaction proceeded efficiently in acetonitrile at 150oC, giving the final product in an average yield of 42% and an average specific activity of 30 GBq/μmol. In vitro, high-SA [131I]IAZGP was incorporated into the tumor cells with similar kinetics and oxygen dependence to low-SA [131I]IAZGP. In HT29 tumor-bearing mice, biodistributions of high- and low-SA [131I]IAZGP were equivalent. Ex vivo autoradiography revealed heterogeneous intratumor localization of high-SA [131I]IAZGP corresponding closely to distributions of other exogenous and endogenous hypoxia markers. Comparable microregional distribution patterns were observed with low-SA [131I]IAZGP. Conclusions: Radiolabeled IAZGP produced via nucleophilic substitution is validated as an exogenous hypoxia marker. Specific activity does not appear to influence the in vivo hypoxia-mapping ability of the radiotracer.

  19. Influence of the chain length on the biological behaviour of /sup 131/I fatty acids

    Riche, F.; Mathieu, J.P.; Comet, M.; Vidal, M.; Pernin, C.; Marti-Batlle, D.; Busquet, G. (Universite de Grenoble, 38 (France)); Bardy, A. (C.E.A.-ORIS, 91 - Gif-sur-Yvette (France))

    1983-01-01

    Saturated and acetylenic fatty acids labeled with /sup 131/I in ..omega.. position, differing by their chain length (C8 to C20) and the number odd or even of their carbon atoms are injected in mice. The evolution of the activity in myocardium, blood, liver and kidney is measured until 10 minutes after injection. The myocardial activity increases with chain length from C8 to C16 then decreases for C18 and C20. The odd or even number of carbon atoms does not influence myocardial activity but in the liver, activity is inferior with the odd fatty acids. The presence of a triple bond accelerates the output of activity from the myocardium and these fatty acids are not well suited for the study of myocardial metabolism.

  20. Influence of the chain length on the biological behaviour of 131I fatty acids

    Saturated and acetylenic fatty acids labeled with 131I in ω position, differing by their chain length (C8 to C20) and the number odd or even of their carbon atoms are injected in mice. The evolution of the activity in myocardium, blood, liver and kidney is measured until 10 minutes after injection. The myocardial activity increases with chain length from C8 to C16 then decreases for C18 and C20. The odd or even number of carbon atoms does not influence myocardial activity but in the liver, activity is inferior with the odd fatty acids. The presence of a triple bond accelerates the output of activity from the myocardium and these fatty acids are not well suited for the study of myocardial metabolism

  1. Preparation of the radiopharmaceutical 131I-Anti-CD20 for the treatment of lymphomas

    At the present time they are considered to the lymphomas like a problem of first magnitude since has happened it is necessary to be the fifth cancer cause in the world. Different treatments focused to the lymphoma like the chemotherapy and the radiotherapy, have been employees to counteract the No-Hodgkin lymphoma, without these they don't exclude the healthy tissue of the toxicity. It is for it that is taking a new direction with the employment of the directed radioimmunotherapy since this it allows to kill wicked cells selectively with radiation dose joined to the apoptosis and cytotoxicity induced by the own one bio molecule. The radioimmunotherapy with radiolabelled antibodies directed to the surface antigen CD20 represents a new modality for the treatment of No-Hodgkin lymphoma and potentially other illnesses. In this work the parameters of optimization are presented for the preparation, control of quality and evaluation of the stability in vitro and in vivo of the monoclonal antibody anti-CD20 labelled with 131 I for the treatment of No-Hodgkin lymphoma. The anti-CD20 labelled by the chloramine-T method with high radiochemical purity (>98%), it is stable in solution for but of a half life of the radionuclide (8.04 days) The 131 I-anti-CD20 doesn't present dehalogenation in vitro (human serum) during 24 h of incubation at 37 C. According to the tests carried out to establish the immunoreactivity, a percentage of union to cells was obtained (B lymphocytes) bigger to 30%. The biodistribution in mice balb/c one hour after their administration, it shows that there is not high reception in mucous neither kidneys, what indicates that the complex is stable in vivo. In conclusion, the radiopharmaceutical 131 I-anti-CD20 was obtained in sterile injectable solution and free of pyrogens with a radiochemical purity bigger to 98% and a specific activity of 296 MBq. The radiolabelled molecule maintains its biological recognition for the receiving CD20 highly expressed in

  2. Comparison of some physicochemical and pharmacokinetical parameters of 99mTc-PAH, 99mTc-MAG3 and 131I-OIH

    Some physicochemical characteristics as well as pharmacokinetic behavior of 99mTc-PAH, as a novel renal agent, 99mTc-MAG3 and 131I-OIH were compared. 99mTc-PAH was prepared from lyophilized kit by adding 99mTcO4-. Labeled complex was stabile and high radiochemical purity radiopharmaceutical, with a low percentage of protein bound to human albumin and hydrophilic character. In spite of its smaller renal uptake, 99mTc-PAH gave satisfactory renal images, 99mTc-PAH showed faster urinary elimination than 99mTc-MAG3 and similar to those one for 131I-OIH. The comparison of pharmacokinetic parameters of 99mTc-PAH, 99mTc-MAG3 and 131I-OIH indicated the favorable characteristics of 99mTc-PAH. (author)

  3. Recurrent malignant pheochromocytoma with unusual omental metastasis: 68Ga-DOTANOC PET/CT and 131I-MIBG SPECT/CT scintigraphy findings

    Pheochromocytomas are rare catecholamine-secreting tumors derived from the sympathetic nervous system. The most common sites of metastasis for pheochromocytoma or extra-adrenal paraganglioma are lymph nodes, bones, lungs, and liver. Patients with known or suspected malignancy should undergo staging with computed tomography (CT) or magnetic resonance imaging as well as functional imaging (e.g. with 123I/131I-MIBG (131I-metaiodobenzylguanidine) and 68Ga-DOTANOC (68Ga-labeled [1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid]-1-NaI3-octreotide) positron emission tomography (PET)/CT) to determine the extent and location of disease. We present a case of recurrent malignant pheochromocytoma with unusual site of metastasis in omentum, which was positive on 68Ga-DOTANOC PET/CT and 131I-MIBG single-photon emission computed tomography (SPECT/)/CT scintigraphy

  4. Biodistribution and SPECT imaging of 125/131I-crotoxin on mice bearing Ehrlich solid tumour

    The search of specific radiopharmaceuticals to be used in breast tumour diagnosis is relevant to complement the techniques applied in conventional medicine. Crotalus durissus terrificus venom (CV) and its main polypeptide, Crotoxin (Crtx), are natural source of several bioactive substances with therapeutical potential. The aim of this work was to evaluate the binding of Crtx with tumour targets in vivo, as well as, evaluate its applicability for breast tumours diagnosis. Crtx was labelled with 125/131I using lactoperoxidase method and radiochemical analysis was performed by chromatography. 125I-Crtx was used for biodistribution and pharmacokinetics studies on swiss mice bearing Ehrlich solid tumour, while 131I-Crtx was used for single photon emission computed tomography (SPECT) imaging. Crtx presented specific binding sites on Ehrlich tumour cells and had a rapid blood clearance (T1/2= 201.1 min.). Intratumoral administration increased significantly the activity delivered into the tumour site (128-fold higher) and reduced the kidney burden (7.2-fold lower). 131I-Crxt demonstrated to interact with tumour cells for until 72 hours allowing good quality images of tumour. Our results indicate the biotechnological potential of Crtx as template for radiopharmaceutical design for cancer diagnosis. (author)

  5. Liquid discharges from patients undergoing {sup 131}I treatments

    Barquero, R. [Servicio de Radiofisica y Proteccion Radiologica, Hospital Universitario Rio Hortega, E-47010 Valladolid (Spain)], E-mail: rbarquero@hurh.sacyl.es; Basurto, F. [Departamento de Fisica Teorica, Atomica y Optica, Universidad de Valladolid, E-47010 Valladolid (Spain); Nunez, C. [Servicio de Radiofisica y Proteccion Radiologica, Fundacion Jimenez Diaz, FJD, E-82001 Madrid (Spain); Esteban, R. [Servicio de Radiologia, Hospital Clinico Universitario, E-47005 Valladolid (Spain)

    2008-10-15

    This work discusses the production and management of liquid radioactive wastes as excretas from patients undergoing therapy procedures with {sup 131}I radiopharmaceuticals in Spain. The activity in the sewage has been estimated with and without waste radioactive decay tanks. Two common therapy procedures have been considered, the thyroid cancer (4.14 GBq administered per treatment), and the hyperthyroidism (414 MBq administered per treatment). The calculations were based on measurements of external exposure around the 244 hyperthyroidism patients and 23 thyroid cancer patients. The estimated direct activity discharged to the sewage for two thyroid carcinomas and three hyperthyroidisms was 14.57 GBq and 1.27 GBq, respectively, per week; the annual doses received by the most exposed individual (sewage worker) were 164 {mu}Sv and 13 {mu}Sv, respectively. General equations to calculate the activity as a function of the number of patient treated each week were also obtained.

  6. Scintiscanning of the adrenal glands with 19-iodocholesterol 131I

    The experiment reported here, though still restricted nevertheless shows up the advantages and limits of a new suprarenal exploration method using 19-iodocholesterol 131I. It is first specified that the suprarenal uptake of radiocholesterol is unsuitable as a functional exploration test. On the other hand extremely valuable morphological information can be obtained by suprarenal scintigraphy especially in the case of Cushing's syndrome and Conn's syndrome, although the method seems less promising in pheochromocytomes. With regard to dosimetric problems, in view of the relative radioresistance of the suprarenals and the liver the dose received by these organs is considered acceptable, but the irradiation of the gonads causes some concern and the doctor must decide as a function of each case

  7. Differential expression profiling of circulation microRNAs in PTC patients with non-131I and 131I-avid lungs metastases: a pilot study

    Introduction: Loss of the ability to concentrate 131I is one of the important causes of radioiodine-refractory disease in papillary thyroid carcinoma (PTC). Recent advantages of serum microRNAs (miRNAs) open a new realm of possibilities for noninvasive diagnosis and prognosis of many cancers. The aim of the current study was to identify differential expression profiling of circulation miRNAs in PTC patients with non-131I and 131I-avid lungs metastases. Methods: The expressions of miRNAs were examined using miRNA microarray chip. The most significantly changed miRNAs from microarray were verified by using qRT-PCR. The potential miRNAs regulating target genes and their preliminary biological functions were forecasted by Bioinformatic analysis. Results: Compared to 131I-avid lung metastases, 13 kinds of significantly differential serum miRNAs including 5 upregulated miRNAs (miR-1249, miR-106a, miR-503, miR-34c-5p, miR-1281) and 8 downregulated miRNAs (miR-1915, miR-2861, miR-3196, miR-500, miR-572, miR-33b, miR-554, miR-18a) in PTC patients with non-131 I-avid lung metastases were identified. Bioinformatic analysis demonstrated that miR-106a was the core miRNA regulating 193 genes in the network. The results of validation confirmed the up-regulation of miR-106a in non-131I-avid lungs metastatic PTC patients. Conclusion: Differentially expressed serum miRNA profiles between PTC patients with non-131I and 131I-avid lungs metastases were analyzed. These findings in our present study could represent new clues for the diagnostic and therapeutic strategy in PTC patients with non-131I-avid metastatic disease

  8. A study on sheep-tissue contamination of 131I after the accident at Chernobyl

    The change of 131I content in sheep-tissue in Xinjiang after the accident at Chernobyl USSR was studied with a radiochemical method. The results showed that 131I level was increased from 7th May in sheep-tissue and reached its maximum on 20th May in thyroid. The effective half-life of 131I in thyroid, blood, muscle and contents in stomach were 7.2d, 6.7d, 6.7d and 5.1d respectively. The specific activities of 131I in grass, thyroid, blood, muscle and contents in stomach showed linear correlations. The 131I content in thyroid for the folded sheep was only 1.7 percent of that for the grazed sheep during the polluting period. The effective dose equivalence for adult to the 1'31I release from Chernobyl was 14.0 μSv in Urumqi and 3.8 μSv in Xinjiang

  9. Treatment of brain metastases from differentiated thyroid cancer with 131I

    Objective: To study the clinical value of treatment of brain metastases from differentiated thyroid cancer (DTC) with 131I. Methods: Eight cases of brain metastases from DTC were followed-up after 131I therapy (2 males, 6 females). The results of 131I therapy were evaluated with clinical presentation, imaging scan and survival analysis. Results: 1) All cases had been survival for 2-35 years within follow-up. 2)A space-occupying lesion in right cerebellum was shrunk after taking 131I 20.65 GBq and disappeared after 23.61 GBq, demonstrated by CT. 3)The times of treatment and total dose of 131I used for each case were clearly decreased with total thyroidectomy than with semithyroidectomy (P131I may improve clinical symptoms and life quality, reduce lesion size, and prolong survival

  10. Gene expression signature in mouse thyroid tissue after 131I and 211At exposure

    Rudqvist, Nils; Spetz, Johan; Schüler, Emil; Langen, Britta; Parris, Toshima Z.; Helou, Khalil; Forssell-Aronsson, Eva

    2015-01-01

    Background 131I and 211At are used in nuclear medicine and accumulate in the thyroid gland and may impact normal thyroid function. The aim of this study was to determine transcriptional profile variations, assess the impact on cellular activity, and identify genes with biomarker properties in thyroid tissue after 131I and 211At administration in mice. Methods To further investigate thyroid tissue transcriptional responses to 131I and 211At administration, we generated a new transcriptional da...

  11. Transient cytotoxicity of 131I beta radiation in hyperthyroid patients treated with radioactive iodine

    Sundaram, P. Shanmuga; Padma, S.; Sudha, S.; Sasikala, K.

    2011-01-01

    Background & objectives: Radioiodine (131I) or radioactive iodine in low doses is used worldwide as the first line of management in the treatment of hyperthyroidism. Information is available on the extent and severity of cell damage after a high dose radioiodine (131I) therapy for thyroid cancer, but information is scanty on its cellular effects, its extent and severity of cell damage after a low dose 131I therapy. The present investigation was aimed to study the cytotoxic effects of a low do...

  12. Determination of the flight range of Acanthoscelides obtectus (Say, 1813) (Coleoptera Bruchidae) using 131I as radioactive tracer

    With the objective of determining the flight range (activity) of the bean weevil (A. obtectus) 800 adult insects were labelled with sodium iodide (Na 131I) at 0.468 mCi/ml. In order to label the weevil they were kept on Petri dishes with filter paper embedded in 3.2 ml sodium iodide (Na 131I) radioactive solution. The labelled insects (over 800,000 c.p.m./800 insects at 5 cm distance) were released in the middle of a bean plantation cv. Rosinha G-2 at physiological maturation stage. The labelled insects were located using a 'Victoreen' monochannel gamma spectrometer with NaI(Tl) cristal, the countings in the field being repeated 8 times. The first two countings (2 and 3 hours after release) showed that the insects had flow in different directions, reaching about 20 m from the releasing point. the 3rd and 4th countings (6 and 7 hours after release) indicate that they reached around 30 m. According to the 5th, 6th and 7th countings (8, 50 and 54 hours after release) the dispersion of the insects continued, maintaining a radius of 30 m. At the last counting (120 hours after release) a greater uniformity in the dispersion rate was observed, probably because the insects adapted themselves to the local environmental conditions. It was also noted that during the day the insects were located under small soil agregates or crop residues, close to the nutrients but never on the foliage. (Author)

  13. The influence of tapazole on iodine metabolism in patients with Graves' disease after 131I radiotherapy

    Objective: To study the influence of tapazole on 131I metabolism in patients with Graves' disease (GD) after 131I radiotherapy. Methods: One hundred and fifty-eight GD patients of first 131I radiotherapy were assigned to three groups. Group 0 did not receive tapazole, and group I, II received tapazole of different doses at 24 h after 131I radiotherapy. The radioactive counts of patients' thyroid and urine were measured dynamically after 131I radiotherapy and the 131I metabolism state was estimated. Results: All three groups after 131I radio-therapy showed a continuous decreasing tendency in radioactive counts of the thyroid, but no significant difference (P>0.05) was observed between them. Three groups' radioactive counts of urine were highest at 24 h, and decreased at 24-48 h after 131I radiotherapy; after 48 h (received tapazole for 24 h ) group I, II showed an obvious increasing tendency again, and they were significantly different from group 0 (P131I radiotherapy, but be given accordingly to the state of illness at a suitable time

  14. 131I effective half-life in patients with larger goiter

    The 131I effective half-life is crucial for the determination of the potential absorbed dose to medical staff, volunteers, and public individuals in general. The purpose of this paper is to determine the 131I effective decay rate from patients submitted to iodine therapy for goiter disease. Results show a large variation of the 131I effective half-life among the sampled population, which ranged from 24 h to 128 h with 65 h of average value. This average value is is more than five times the 131I effective half-life already reported for patients with thyroid cancer. (author)

  15. Observation of curative effect of 131I in treatment of hyperthyroidism

    Objective: To explore the curative effect of 131I in the treatment of hyperthyroidism. Method: 126 patients with hyperthyroidism were treated with 131I and the curative effect was analyzed. Result: The results showed that among 126 cases of hyperthyroidism treated with 131I, 117 cases had recovered and the cure rate was 92.9%. 9 cases were found hypothyroidism in one-year follow-up and the occurrence rate was 7.1%. Conclusion: The treatment of hyperthyroidism with 131I is safe and effective method. (authors)

  16. Application of an imaging plate system to in vivo thyroid 131I monitoring

    An imaging plate (IP) system was applied to in vivo thyroid radioactive iodine 131 (131I) monitoring. Thyroid contamination by 131I occurs when medical staffs and patient's families take in 131I used as treatment agent for thyroid cancer and hyperthyroidism in nuclear medicine, inhabitants take in 131I released into environment by an accident of nuclear facilities, or worker take in 131I used by experiment of research. The IP system is a two-dimensional integrating radiation detector which is a plate thinly coated plastic sheet with a kind of phosphore. The IP was exposed to a neck-thyroid phantom loaded 131I aqueous solution. The IP system displayed a thyroid image that reflects a unique shape characteristic of the thyroid gland. A 131I thyroid imaging allows visual confirmation of thyroid contamination by 131I. The counting efficiency was approximately constant when neck diameter, thyroid volume and prethyroid tissue thickness varied within the normal adult. The detection limit of 450Bq was about 1/65 of the screening level of 30kBq. The IP system is applicable for thyroid 131I monitoring

  17. A new and simple method for separation of 131I from tellurium oxide using an activated charcoal column

    A simple method for separation of 131I from irradiated TeO2 is described. Initially Te was separated from the 131I by precipitation technique. 131I solution containing traces of Te was adsorbed on an activated charcoal. After sufficient washings with HCl and water, 131I was desorbed from charcoal with NaOH. The recovery of Te was 99%. Retention of 131I on charcoal was 100% and elution efficiency was 75-80%. (author)

  18. Metabolic therapy of thyroid by {sup 131}I and radiation protection; Therapie metabolique thyroidienne par {sup 131}I et radioprotection

    Mathieu, I.; Caussin, J.; Smeesters, P.; Wambersie, A.; Beckers, C. [Centre de Medecine Nucleaire, Universite Catholique de Louvain, B-1200 Brussels (Belgium)

    1997-12-31

    The recommendations of International Commission on Radiological Protection (ICRP 60) to be applied in the European Union from the year 2000 imply a limit of the annual dose of 1 mSv for public as well as the compliance with the dose constraints. In order to verify the possibility of observing these new standards without losing the very favourable cost-profit of the {sup 131}I therapy in thyroiditis, 73 members of patient families treated by radioiodine were surveyed by direct dosimetry. A number of 22 patients afflicted with thyroid cancer received doses of 3700 to 7400 MBq and 18 hyperthyroid patients received 200 to 600 MBq. Dosemeters mounted around the neck were carried for 2-3 weeks by 35 spouses and 38 children 4 months to 25 years old. The residual thyroid radioactivity and the T{sub 1/2} of {sup 131}I were measured by gamma chambers in every patients. In the group of patients with thyroid cancers the effective T{sub 1/2} is 2.2 days. The doses measured in families are lower than 1 mSv in any spouses and lower than 0.3 mSv in all the children except one. In hyperthyroid patients the effective T{sub 1/2} is 6.2 days. The average dose received is 1.04 mSv (0.05-5.2) for spouses and 0.13 mSv (0.04-3.1) for children. These direct dosimetry data are reliable and allow to propose reasonable and efficient restrictions which will not compromise neither the efficiency of treatment or the environment safety

  19. The experimental study on anti-tumor effect of 131I-Tyr-octreotide in nude mice bearing human non-small cell lung cancer

    Objective: Radionuclide-labeled low molecular weight polypeptide is recently advocated for the diagnosis and treatment of malignant tumor. The purpose of this study was to evaluate the anti-tumor effect of 131I-Tyr-octreotide in nude mice bearing human non-small cell lung cancer (NSCLC). Methods: 131I-Tyr-octreotide was prepared by Ch-T method. The radiochemical purity was measured and biodistribution was evaluated. The nude mice models bearing human NSCLC were studied and divided into four groups: group A injected 131I-Tyr-octreotide through tail vein, group B injected normal saline, group C injected 131I-Tyr-octreotide through stroma and group D injected 131I through stroma. The radioactivity ratio of tumor to normal tis- sue (T/NT) was calculated over region of interest (ROI). The tumor cell cycle and cell apoptosis were analyzed by flow cytometry (FCM), terminal deoxynucleotidyl transferase mediated dUTP-biotion nick end labeling (TUNEL) and histopathological analysis. Statistical analysis was performed with SPSS 11.0, and the comparison for difference between groups performed with one-way ANOVA analysis. Results: The labeled radiochemical purity was (95.23 ± 1.67)% and specific activity of 3.5 x l06 Bq/μg. The biodistribution showed high uptake in kidney, and low uptake in liver and spleen. The radioactive uptake in group C was higher than the other groups, and the retention time was longer. The T/NT was 52.74 ± 0.13 after 24 h, which was much higher than that of the other groups (group D: 8.90 ± 0.23, group A: 6.42 ± 0.02, q=628.81 and 664.33, all P1 phase was blocked most remarkably in group C than the other groups [group C: (83.17 ± 6.86)%, group A: (57.02 ± 18.81)%, group D: (49.29 ± 7.80)%, group B: (45.88 ± 5.13)%, q=5.29, 6.86, 7.55, 1.56, 2.26, 0.69, all P131I-Tyr-octreotide was easily labeled by Ch-T. 131I-Tyr-octreotide could induce tumor cell apoptosis and inhibit the tumor cell of NSCLC. It might be a potential target-directed agent in

  20. Graves hyperthyroidism 131I treatment the clinical curative effect of observation

    Objective: to study the clinical treatment of 131I Graves hyperthyroidism curative effect. Methods: the clinical data of Graves hyperthyroidism patients were retrospectively analyzed. Results: 258 cases of patients with hyperthyroidism Graves. 131I treatment 1∼2 times after healed 200 cases, improvement of 38 patients, a low, 10 cases were invalid 10 cases failure; the total effective 96.12%. 1 year after treatment 131I thyroid quality by before treatment 43.6 + 20.9 grams shrinks to 1.98 + 18.5 grams (p131I before treatment with prominent eyes 68 cases (26.4%) 131I after treatment, the prominent eyes healed 24 cases (34.8%), improvement 30 patients (43.5%), invalid in 12 cases (17.4%), aggravating in 2 cases (2.9%), efficient for 79.7%. Concurrent hyperthyroidism 131I before treatment in patients with 31 patients (heart), after the treatment of 131I 12.0% in 25 patients recovered, 6 patients get better, efficient 100%. After the treatment of 131I temporary armor low in 25 patients (9.7%) , permanent armour low 27 cases (10.5%). After the treatment of 131I 15 cases have been reduced to a sex WBC (5.8%), 8 cases of liver function mild damage (3.1%), 13 cases itchy skin (1 case), cholesterol by 5.0% compared appear suspected hyperthyroidism crises (0.4%). 258 patients with thyroid type micronodular 41 cases, treatment cured after 131I in 25 patients (61.0%), improvement in 16 (39.0%), laseris 100%, Diffuse 217 example, cure 175 cases (80.6%), improvement 22 patients (10%), a low 10 (4.6%), invalid 10 (4.6%), laseris 95.4 percent. Conclusion: 131I treatment Graves hyperthyroidism is simple, safe, effective, and can be used as the preferred treatment method outperforms that of anti-thyroid drugs. (authors)

  1. Comparison of 131I whole-body imaging, 131I SPECT/CT, and 18F-FDG PET/CT in the detection of metastatic thyroid cancer

    The aim of this study was to compare 131I whole-body scintigraphy (WBS), WBS with 131I single photon emission computed tomography/computed tomography (SPECT/CT), and 18F-fluorodeoxyglucose (FDG) positron emission tomography (PET)/CT in the detection of distant metastases of differentiated thyroid cancer (DTC). A total of 140 patients with 258 foci of suspected distant metastases were evaluated. 131I WBS, 131I SPECT/CT, and 18F-FDG PET/CT images were interpreted separately. The final diagnosis was obtained from histopathologic study, serum thyroglobulin level, other imaging modalities, and/or clinical follow-up. Of the 140 patients with 258 foci, 46 patients with 166 foci were diagnosed as positive for distant metastasis. The sensitivity, specificity, and diagnostic accuracy of each imaging modality were 65, 55, and 59%, respectively, for 131I WBS; 65, 95, and 85% for 131I SPECT/CT, respectively; and 61, 98, and 86%, respectively, for 18F-FDG PET/CT in patient-based analyses. Lesion-based analyses demonstrated that both SPECT/CT and PET/CT were superior to WBS (p18F-FDG PET/CT presented the highest diagnostic performance in patients who underwent multiple challenges of radioiodine therapy. (orig.)

  2. Individualised 131I-mIBG therapy in the management of refractory and relapsed neuroblastoma

    Full text of publication follows. Introduction: 131I labeled mIBG is used as targeted radionuclide therapy for relapsed and refractory neuroblastoma. An individualized form of 131I-mIBG-therapy using whole body dosimetry has been developed at our institution. We report toxicity and outcome data. Methods: a retrospective review of children treated at the Royal Marsden Hospital (RMH) from 1994-2012. The overall aim was initially to deliver a whole body dose (WBD) of 2 Gy based on a tracer study, or in later years a total 4 Gy WBD in two fractions, with cell support, was delivered by a first therapeutic activity of 444 mBq/KXg and a subsequent therapy adjusted according to the measured WBD. Toxicity and outcome data were collated by clinical note review. Institutional review board approval was obtained. Results: 45 treatments were given to 26 patients (16 male, 10 female). Median age at first mIBG: 72 months (range 17-241), median 2 treatments per patient. Indication: primary refractory disease (12), relapse (8), other (6). Administered mean mIBG activity 10951 mBq (range 3539-32871). Mean mIBG whole body dose 1.8 Gy, (range: 1-3.5). Recorded toxicities: grade 3-4 neutropenia in 20/24 treatments, grade 3-4 thrombocytopenia in 20/26 treatments. Acute toxicity occurred following 21/45 treatments, including 9 cases of febrile neutropenia and 1 hypertensive crisis. The only long-term toxicity was prolonged thrombocytopenia in a patient where there was no hematopoietic stem cell rescue. There were no toxic deaths related to mIBG therapy. Response rates as reported on first post-treatment mIBG scan were complete response (4.5%), partial response (52%), stable disease (30%), progression (9%) and mixed response (4.5%). Median time to progression was 3 months (range 6 weeks to 11 months). 6 patients were alive with disease at last follow up (mean 11 months) and 3 are alive and disease-free at last follow up (4 months, 20 months and 10 years). Conclusions: in children with

  3. Pharmacokinetic studies of 131 I-stevioside and his metabolites

    Stevia rebaudiana is a shrub widely in Paraguay and Brazil, belonging to the compositae family. The leaves of this plant contain large amounts of stevioside. Since the use of stevioside as sugar substitute continues to increase, the purpose of this study is to investigate the biological distribution, excretion and the possibility of stevioside to be degraded to steviol 'in vitro'. 131-I-stevioside (1,10 MBq) was i.v. injected in Wistar male rats its distribution in the body and metabolism were studied. The highest concentration of radioactivity was observed in the liver and the small intestine after 10 and 120 minutes respectively. RP-HPLC analysis of the bile showed that steviol appeared as a major metabolite, representing 47,3% of the radioactivity while stevioside represented 37,3% and the remaining 15,4% was due to an unidentified metabolite. The results showed that stevioside was partially degraded 'in vivo' to steviol and other metabolite, and that part of the radioactivity was absorbed from the small intestine. (author)

  4. Biokinetics and dosimetry of 131I-metaiodobenzylguanidine (MIBG)

    In connection with clinical 131I-MIBG studies of patients with suspected sporadic pheochromocytoma or multiple endocrine neoplasia (MEN II), quantitative biokinetic data have been collected in order to improve the present estimates of absorbed dose to various organs and tissues as well as of the effective dose equivalent and its variation from patient to patient. The authors find considerably higher liver uptake than earlier published, but their estimates of the uptake in the thyroid and in the normal adrenal medulla show lower values than earlier reported. This results in the following absorbed dose per activity unit administered (mGy/MGq) (mean and typical range): Liver: 0.83 (0.50 - 1.2); Spleen: 0.61 (0.17 - 1.3); Salivary glands: 0.22 (0.082 - 0.41); Thyroid (blocked): 0.1; Total body: 0.082 (0.055 -0.12). The effective dose equivalent was estimated to be 0.20 (0.1 -0.3) mSv/MBq when the thyroid is adequately blocked. 16 references, 4 figures, 2 tables

  5. 131I-iodocholesterol (NP-59) scintigraphy in adrenocortical diseases

    The diagnostic usefulness of adrenal imaging with 131I-iodocholesterol (NP-59) is now well established. In order to correlate histopathology with the adrenal scan the authors examine and report their experience in 37 patients with surgically proven adrenal lesions or pituitary adenomas. This series included 24 patients with Cushing's syndrome: 14 caused by benign adrenal adenoma and 10 due to bilateral pituitary-ACTH-dependent adrenocortical hyperplasia. Ten patients with primary aldosteronism were submitted to surgery which confirmed the presence of aldosterone-producing adrenal adenomas. Two women with hyperandrogenism (due to virilizing ovarian tumors) had normal adrenals but the ovarian stromal luteoma markedly concentrated the iodocholesterol while the arrhenoblastoma did not. A patient with adrenal hematoma is also included in this report. The overall histopathological correlation with the radiocholesterol scintiscan yields an accuracy in our series of 97 percent (36/37). The false-negative adrenal scan (also missed by other non-invasive techniques) occurred in a patient with an aldosterone-producing adrenal adenoma measuring 1.0 x 1.5 cm

  6. Regulation examinations to determine the success of 131I therapy

    97 patients with diffuse or nodular struma and 42 patients with autonomous adenoma were re-examined who had been treated with 131I for hyperthyroidism between 1970 and 1975. Besides in-vitro determinations of T4, NTR, T3, and TSH, the TcTU was determined 20 min. p.i. in all patients. The TRH test and in most patients also the suppression test with 14 x 200 μg T4 were carried out as regulation tests. In the group of treated hyperthyroid strumae, a clinically hyperthyroid picture was correlated with the in vitro values in 3 patients. 47 other patients had increased T3 values but no hyperthyroid symptoms. 8 patients were hypothyroid, and 17 patients had latent hypothyroidism. The TRH test was positive in 49 cases and negative in 48 cases. The suppression test showed a residual autonomy in 63% of the patients. 10 patients with positve TRH test results had negative suppression test results. (orig./AJ)

  7. The curative effect of 131I therapy on Re-hyperthyroidism treated with ATD

    68 cases of re-hyperthyroidism patients treated with ATD are treated with 131I, and the results are analyzed carefully. It indicates that the re-hyperthyroidism patients with 131I treating could receive good effect. It is necessary to monitor the thyroid hormone level and to be supplemented with ATD or thyroxine agent when the thyroid function is abnormal

  8. Diagnostic and therapeutic use of 131I-metaiodobenzylguanidine in children with neuroblastoma

    A total of 68 scintigraphies with 131I-metaiodobenzylguanidine (131I-MIBG) were performed in 35 children affected by neuriblastoma, and the results were compared with those obtained by other diagnostic procedures. In 46 studies, the results of 131I-MIBG scintigraphy were in accordance with biochemical and instrumental data (31 true positives, 15 true negative results). Whereas, in 22 instances the results of 131I-MIBG scintigraphy did not agree with those of other diagnostic procedures. In 13 studies 131I-MIBG was negative and other data positive (false negatives). In 9 studies 131I-MIBG was positive and other data negative. Further investigation, including surgical exploration in 5 cases, revealed no false positives. These individual cases are discussed. 131I-MIBG can thus play an important, albeit not exclusive, role in diagnosis, staging and follow-up of neuroblastoma. Disappointing results were on the other hand obtained in seven patients with advanced disease in whom therapeutic attempts were carried out with 131I-MIBG

  9. Transfer of 131I to sheep milk from vegetation contaminated by Chernobyl fallout

    The transfer of 131I to sheep milk was measured in a controlled feeding experiment using herbage recently contaminated by fallout from the Chernobyl accident. The transfer coefficient (Fm) of 131I from the Chernobyl-contaminated herbage was 0.29±0.017 day litre-1. The daily proportion of 131I intake which was secreted in milk was 56±0.035%. This is an order of magnitude higher than for cattle and agrees with the higher transfer of stable iodine from plasma to milk which occurs in sheep and goats. At the same time the biological half-life of 131I was measured in ewes which had been grazing outside during deposition of the Chernobyl fallout and were then housed and fed an 131I-free diet. The loss of 131I in sheep milk was described using a double exponential relationship. The calculated biological half-life for the first component in the milk was 1 day, accounting for 97.4% of the reduction in the concentration of 131I activity in the milk. The 131I-free diet had a comparatively high stable iodine content since it was saltmarsh vegetation, however, the calculated half-life was similar to previously estimated values for goats. (Author)

  10. Randomized trial of lithium carbonate in augmentation of 131I absorbed by thyroid remnant

    Objective: To evaluate the value of lithium carbonate in the ablation of thyroid remnant with 131I. Methods: Thirty consecutive DTC patients with thyroid remnants were assigned to two groups, the first is lithium carbonate group received lithium carbonate 250 mg quater in die (Qid) for a week, the second was control group received Vit B4 10 mg ter in die (Tid) for a week. Responses to treatment were evaluated with the parameters as the increase of thyroid 131I uptake rate at 24 h, the prolongation of Teff and the augmentation of absorbed dose of 131I. Data analysis was performed with SPSS statistic software. Results: Compared with the uptake before the lithium carbonate treatment, 24 h 131I uptake rate of the thyroid remnant was increased about (1.32±0.26) fold, Teff was about (1.15±0.18) fold, absorbed dose was about (1.52±0.50) fold in the lithium carbonate group; compared with control group, 24 h 131I uptake rate in the lithium carbonate group was significantly increased, Teff was significantly prolonged, absorbed 131I dose was significantly augmented. Conclusion: Lithium carbonate effectively increased 24 h 131I uptake rate, prolonged Teff and augmented absorbed 131I dose of thyroid remnant

  11. Study of the effect of 131I treatment of graves disease on the number of peripheral blood leucocyte

    Objective: To study the effect of 131I treatment of Graves disease on the number of peripheral blood leucocytes. Methods: The Graves disease patients were divided into groups according to the 131I dosage taken, peripheral blood leucocytes were measured before and after the taking of 131I. Results: On the 4th day after taking 131I, the absolute value of leucocyte, neutrophil, Lymphocyte were decreased, the number of neutrophil was significantly decreased (P 131I(P 131I. Conclusion: 131I treatment of Graves disease can reduce the number of leucocytes, especially neutrophil, in a short time (about one week), it is related with the dosage of 131I. After a week, they can nearly return to the primary level. Some medicine which can increase the number of leucocytes should be used when the patient taking 131I

  12. Analysis of factors for early hypothyroidism after 131I treatment of hyperthyroidism

    To explore the factors for the early hypothyroidism following 131I treatment of hyperthyroidism, clinic data of 120 hyperthyroidism patients including 8 independent and 1 dependent variables after one year 131I treatment were analyzed by logistic regression analysis method. The results showed that the average 131I dosage given to one gram thyroid tissue was correlated positively with early hypothyroidism occurrence, and the weight of thyroid was negatively correlated to early hypothyroidism occurrence. The positive and negative prediction accuracy of the early hypothyroidism were 53.3% and 96.1% respectively, and the total prediction accuracy was 46.7%. The results suggest that the 131I dosage and the weight of thyroid are key factors for early hypothyroidism; the appropriate adjustment of 131I dosage based on the thyroid mass could prevent the early hypothyroidism occurrence in certain degree. (authors)

  13. Biochemistry of derivatives of amino acid with (/sup 103/Ru)ruthenocene. Comparison with /sup 131/I-hippuran

    Wenzel, M.; Park, I.-H.

    1986-01-01

    The potential radiopharmaceuticals: ruthenocenoyl alanine, ruthenocenoyl methionine, 1'methyl-ruthenocenoyl glycine and its esters were labelled with /sup 103/Ru starting from the analogous ferrocene compounds. In a series of tests in mice and rats these substances were compared with hippuran and ruppuran (=ruthernocenoyl glycine, a ruthenocene-amino acid analogue of hippuran). The organ distribution of these compounds was measured at various times after injection. Kidney concentrations of 1'-methyl-ruthenocenoyl glycine and its esters were found to be extremely high, followed by a rapid excretion. In contrast with these compounds, ruthenocenoyl methionine indicated a significantly greater affinity for liver than for kidney, but not for pancreas. Ruthenocenoyl alanine exhibits a high affinity for tumor cells. The advantages of /sup 97/Ru labelled radiopharmaceuticals compared with sup(99m)Tc or /sup 123/I//sup 131/I labelled compounds are discussed.

  14. Evaluation of 131I treatment efficacy and prognostication for bone metastases from differentiated thyroid cancer

    Objective: To evaluate the efficacy of 131I treatment for bone metastases from DTC and analyze the survival rates after 131I treatment and prognostic factors. Methods: One hundred and six DTC patients with bone metastases treated by 131I during January 1991 and January 2009 were retrospectively analyzed. Treatment efficacy was assessed based on serum Tg change, bone pain palliation and changes on medical imaging. Univariate analysis was performed for defining the factors affecting 131I treatment efficacy. Survival curves were estimated using the life table method. Survival analysis was performed using Kaplan-Meier method. Results: Serum Tg decreased dramatically in 37/106 (34.9%) patients treated with 131I. Thirty-nine of 61 patients (63.9%) with bone pain had pain relief. Age, tumor subtype and presence of non-osseous distant metastases were significant factors affecting 131I treatment efficacy based on serum Tg change (χ2=6.443, 11.455, 6.756, all P2=0, 0, 0.060, all P>0.05). There were no imaging changes of bone metastases in 77.4% of patients after 131I treatment. The overall 5-year and 10-year survival rates from initial diagnosis of bone metastases was 86.47% and 57.90%, respectively. Univariate analysis showed that number of metastases, presence of non-osseous distant metastases and pre-131I treatment surgery were significant factors for survival (Log-rank values were 4.05, 5.98, 4.22, all P131I treatment for bone metastases from DTC is effective for lowering serum Tg and palliation of bone pain. Single metastasis, absence of non-osseous distant metastases and pre-131I therapy surgery are favorable predictors of prognosis. (authors)

  15. Health effects of therapeutic use of 131I in hyperthyroidism

    Since 1942, therapy with radioiodine (Na131I) has gained a major role in the treatment of benign thyroid disorders, notably hyperthyroidism caused by Graves' disease or toxic multi nodular goiter. The very large series of patients treated so far offer the opportunity for an assessment of both benign and malignant side effects. Hyperthyroidism is sometimes observed after radioiodine therapy due to radiation induced thyroid hormone or by an immunological mechanism. Despite the numerous attempts to design dosage schedules aiming at euthyroidism, hypothyroidism occurs in the majority of patients throughout life. Transient hypothyroidism may be observed within the first year after therapy and is caused by an immunological mechanism. Radioiodine therapy in Graves' disease may induce or worsen ophthalmopathy, which can be prevented by steroids effectively. Hypoparathyroidism and hyperparathyroidism have been reported after radioiodine therapy but probably do not exceed the normal incidence. Sialitis is commonly observed but mostly in patients treated with radioiodine for thyroid cancer. There are no indications for induction of genetic abnormalities after radioiodine therapy although no definite conclusion can be reached. Much attention has been paid to malignant disease. In very large series, no effects of radioiodine therapy on survival have been observed. Some studies report an increased relative risk for certain types of cancer (notably thyroid cancer, stomach cancer, bladder and kidney cancer or hematological malignancies). However, these observations were not confirmed by other large studies, so that no definite conclusion with respect to risk for certain types of malignant disease can be drawn. However, radioiodine therapy for benign thyroid disorders has generally considered safe and without major side effects, hypothyroidism being the most frequent one

  16. Cytotoxic effects of m-[131I]- and m-[125I]iodobenzylguanidine on the human neuroblastoma cell lines SK-N-SH and SK-N-LO

    As we have reported recently, the human neuroblastoma cell line SK-N-SH is able to take up and store m-iodobenzylguanidine (mIBG). This is in contrast to several other neuroblastoma cell lines, among which are SK-N-LO cells. Both cell lines were used in cell killing experiments with unlabeled and radioactive-labeled mIBG. Using 1-200 microCi m-[131I]IBG (1 h incubation time), only SK-N-SH cells could to a large extent be destroyed in a dose-dependent manner. This effect is completely caused by the radioactive labeling of the molecule, because unlabeled mIBG proved not to be toxic in the concentration range used in experiments with radiolabeled mIBG (30 nM-3 microM). The killing effect was strongly reduced when m-[131I]IBG with low specific activity (0.2-0.3 mCi/mg) was used instead of 20-30 mCi/mg. Similar effects in both cell lines were obtained using m-[131I]-and m-[125I]IBG. SK-N-SH cells that survived a first treatment with m-[131I]IBG were less sensitive to a second treatment. SK-N-LO cells were more sensitive against m-[131I]- and m-[125I]IBG than SK-N-SH cells if both cell lines are exposed to these radioactive compounds over a long period of time (24 h). The reason that only SK-N-SH cells could be destroyed in short-term incubation experiments is that mIBG is stored for approximately 7 days in these cells only. SK-N-LO cells could only be destroyed to a significant degree if m-[131I]IBG was permanently present in the test system. Bone marrow stem cells (CFU-c) also proved to be sensitive against m-[131I]IBG, although the effects were less pronounced than on SK-N-SH cells

  17. Investigations on 131I-hippurate-clearance in ostructive-uropathy extraction of para-aminohippuric acid and 131I-hippurate in the acutely obstructed canine kidney

    The results of more recent clinical and experimental investigations have thrown doubt on the usefulness of determining the individual 131I-hippurate clearance for evaluation of the function of acutely obstructed kidneys. In the clearance studies carried out in the conventional way it was difficult to determine quantitatively the urine produced during urinary obstruction. The renal extraction of p-aminohippuric acid and 131I-hippurate was determined in simultaneous measurement in six dogs before and after acute urinary obstruction with a constant plasma level of the test substances. The results obtained with this very elaborate method which is, however, independent of urine collection show that an acute urinary obstruction leads to a decrease of renal extraction both of PAH and of 131I-hippurate. The results of the extraction investigations hence confirm the results of the clearance studies mentioned. In addition, they show that the 'increase' of renal performance immediately after an experimentally induced urinary obstruction repeatedly found with catheterless determination of 131I-hippurate-clearance cannot be explained by a different kinetic behavior of PAH and 131I-hippurate in the acutely obstructed kidney. (orig./MG)

  18. Benign oral pathology as a cause of false positive 131I uptake in thyroid carcinoma

    Full text: We present three thyroidectomised patients with a history of thyroid carcinoma who had non-metastatic 131I uptake due to benign oral pathology. A salivary gland study suggested impaired function but no obstruction was demonstrated on a sialogram. The symptoms resolved on antibiotic therapy and a subsequent 131I study was normal. A subsequent thallium study demonstrated physiological tracer distribution. A 35-year-old female with papillary cell carcinoma of the thyroid demonstrated a focus of uptake on the right hemi-mandible following both a diagnostic and a therapeutic dose of 131I. This area was tender and an OPG confirmed an area of liquefaction at this site. A 53-year-old female with medullary cell carcinoma of the thyroid demonstrated a focus of uptake in the right side of the maxilla following a diagnostic administration of 131I. An OPG confirmed an area of liquefaction around the apex of the right upper centre. These three cases illustrate salivary gland and dental inflammation as causes of false positive 131I uptake. It is important to differentiate non-metastatic 131I uptake from that due to functioning metastatic thyroid carcinoma in order to avoid inappropriate treatment with large additional doses of 131I. As in these patients, clinical assessment and the use of anatomical imaging or other isotopes such as thallium or technetium can be helpful in ruling out a mistaken diagnosis of metastasis

  19. {sup 131}I treatment for thyroid cancer and risk of developing primary hyperparathyroidism: a cohort study

    Lin, Chien-Mu [Taipei Medical University - Shuang Ho Hospital, Department of Nuclear Medicine, Taipei (China); Taipei Medical University, Department of Radiology, College of Medicine, Taipei (China); Doyle, Pat [London School of Hygiene and Tropical Medicine, Faculty of Epidemiology and Population Health, London (United Kingdom); Tsan, Yu-Tse [National Taiwan University College of Public Health, Institute of Occupational Medicine and Industrial Hygiene, Taipei (China); Taichung Veterans General Hospital, Department of Emergency Medicine, Taichung (China); Chung Shan Medical University, School of Medicine, Taichung (China); Lee, Chang-Hsing [Ton Yen General Hospital, Department of Occupational Medicine, Hsinchu County (China); Wang, Jung-Der [National Taiwan University College of Public Health, Institute of Occupational Medicine and Industrial Hygiene, Taipei (China); National Cheng Kung University College of Medicine, Department of Public Health, Tainan (China); Chen, Pau-Chung [National Taiwan University College of Public Health, Institute of Occupational Medicine and Industrial Hygiene, Taipei (China); National Taiwan University College of Public Health, Department of Public Health, Taipei (China); National Taiwan University College of Medicine and Hospital, Department of Environmental and Occupational Medicine, Taipei (China); Collaboration: Health Data Analysis in Taiwan (hDATa) Research Group

    2014-02-15

    To evaluate the association between {sup 131}I therapy for thyroid cancer and risk of developing primary hyperparathyroidism. This was a nationwide population-based cohort study of patients with thyroid cancer diagnosed during the period 1997-2008. The data were obtained from the Taiwan National Health Insurance Research dataset. The cumulative {sup 131}I dose in each patient was calculated. Hazard ratios (HRs) were calculated using a proportional hazards model to estimate the effect of {sup 131}I therapy on the risk of developing primary hyperparathyroidism in the cohort. A total of 8,946 patients with thyroid cancer were eligible for the final analysis. Among these patients, 8 developed primary hyperparathyroidism during the follow-up period that represented 38,248 person-years giving an incidence rate of 20.9 per 10{sup 5} person-years. {sup 131}I was used in the treatment of 6,153 patients (68.8 %) with a median cumulative dose of 3.7 GBq. The adjusted HRs were 0.21 (95% CI 0.02-1.86) and 0.46 (95% CI 0.10-2.10) for those receiving a cumulative {sup 131}I dose of 0.1-3.6 GBq and ≥3.7 GBq, respectively, compared to no therapy. The risk of developing primary hyperparathyroidism did not increase with increasing {sup 131}I dose (test for trend p = 0.51). No interaction was found between {sup 131}I dose and age (p = 0.94) or {sup 131}I dose and sex (p = 0.99). {sup 131}I treatment for thyroid cancer did not increase risk of primary hyperparathyroidism during a 10-year follow-up in this study population. Further research with a longer follow-up period is needed to assess late adverse effects beyond 10 years. (orig.)

  20. 131I treatment for thyroid cancer and risk of developing primary hyperparathyroidism: a cohort study

    To evaluate the association between 131I therapy for thyroid cancer and risk of developing primary hyperparathyroidism. This was a nationwide population-based cohort study of patients with thyroid cancer diagnosed during the period 1997-2008. The data were obtained from the Taiwan National Health Insurance Research dataset. The cumulative 131I dose in each patient was calculated. Hazard ratios (HRs) were calculated using a proportional hazards model to estimate the effect of 131I therapy on the risk of developing primary hyperparathyroidism in the cohort. A total of 8,946 patients with thyroid cancer were eligible for the final analysis. Among these patients, 8 developed primary hyperparathyroidism during the follow-up period that represented 38,248 person-years giving an incidence rate of 20.9 per 105 person-years. 131I was used in the treatment of 6,153 patients (68.8 %) with a median cumulative dose of 3.7 GBq. The adjusted HRs were 0.21 (95% CI 0.02-1.86) and 0.46 (95% CI 0.10-2.10) for those receiving a cumulative 131I dose of 0.1-3.6 GBq and ≥3.7 GBq, respectively, compared to no therapy. The risk of developing primary hyperparathyroidism did not increase with increasing 131I dose (test for trend p = 0.51). No interaction was found between 131I dose and age (p = 0.94) or 131I dose and sex (p = 0.99). 131I treatment for thyroid cancer did not increase risk of primary hyperparathyroidism during a 10-year follow-up in this study population. Further research with a longer follow-up period is needed to assess late adverse effects beyond 10 years. (orig.)

  1. Predictive value of tracer studies for /sup 131/I treatment in hyperthyroid cats

    Broome, M.R.; Turrel, J.M.; Hays, M.T.

    1988-02-01

    In 76 cats with hyperthyroidism, peak thyroidal radioiodine (/sup 131/I) uptakes and effective half-lives were determined after administration of tracer and therapeutic activities of /sup 131/I. In 6 additional hyperthyroid cats, only peak thyroidal uptakes after administration of tracer and therapeutic activities of /sup 131/I were determined. Good correlation was found between peak thyroidal uptakes of tracer and therapeutic /sup 131/I; however, only fair correlation was observed between effective half-lives. In 79% of the cats, the effective half-life for therapeutic /sup 131/I was longer than that for tracer /sup 131/I. After administration of therapeutic activity of /sup 131/I, monoexponential and biphasic decay curves were observed in 51 and 16 cats, respectively. Using therapeutic kinetic data, radiation doses to the thyroid gland were calculated retrospectively on the basis of 2 methods for determining the activity of /sup 131/I administered: (1) actual administration of tracer-compensated activity and (2) hypothetic administration of uniform activity (3 mCi). Because of the good predictive ability of tracer kinetic data for the therapeutic kinetic data, the tracer-compensated radiation doses came significantly (P = 0.008) closer to the therapeutic goal than did the uniform-activity doses. In addition, the use of tracer kinetic information reduced the extent of the tendency for consistently high uniform-activity doses. A manual method for acquiring tracer kinetic data was developed and was an acceptable alternative to computerized techniques. Adoption of this method gives individuals and institutions with limited finances the opportunity to characterize the iodine kinetics in cats before proceeding with administration of therapeutic activities of /sup 131/I.

  2. Integral assessment of oxidative metabolism during long-term domestic revenue 131I in rats

    Peroxy processes in the blood of male rats of the Wistar chemiluminescence method with prolonged oral intake of 131I were investigated. It has been shown that long-term oral intake of 131I (29.3 kBq/day per animal for 14 days) causes changes in the indices of the chemiluminescent reaction (aggregate chemiluminescence, luminescence maximum and the final intensity of luminescence, time to reach maximum values). However, absolute value of these indicators are not significantly dependent on the administration of the active isotope. The features of the current processes of peroxidation in the blood of laboratory rats after prolonged administration of 131I we discuss

  3. Evaluation of novel tropane analogues in comparison with the binding characteristics of [18F]FP-CIT and [131I]β-CIT

    This study evaluated novel potential dopamine transporter (DAT) inhibitors as ligands for positron emission tomography. Five new tropane analogs were synthesized and compared with the known ligand 2β-carbomethoxy-3β-(4-iodophenyl)tropane (β-CIT) and the recently characterized ligands N-(3-iodoprop-2E-enyl)-2β-carbomethoxy-3β-(4-methylphenyl)-nortropane (PE2I) and 2β-carbofluoroethoxy-3β-(4-methylphenyl)tropane (FETT). Evaluation with autoradiography measured the ability to antagonize the binding of [131I]iodine-labeled β-CIT and [18F]fluorine-labeled N-(3-fluoropropyl)-2β-carbomethoxy-3β-(4-iodo-phenyl) nortropane in rat and pig brains. The standards for comparison (PE2I and FETT) competed strongly in all regions investigated (striatum, cortex, superior colliculus and cerebellum). Of the new compounds, 2α-amido-fluoroethyl-3β-(4-iodophenyl)tropane () and 2β-amido-fluoroethyl-3β-(4-iodophenyl)tropane () competed strongly with [131I]β-CIT in DAT-rich striatum, but also in other brain regions suggesting poor DAT selectivity. Because [131I]β-CIT binds unselectively both to DAT and serotonin transporters, no definite conclusion about the selectivity of the new compounds is possible. However, preclinical studies using the compounds and labeled with fluorine-18 or iodine-131 are encouraged.

  4. National comparison of activity measurements of 131I, 60Co, and 133Ba in Indonesia

    National comparisons of radioactivity measurements of 131I and 60Co (in 2010) and of 133Ba (in 2011) were carried out within the framework of the National Radiation Metrology Laboratory Program of Indonesia, coordinated by PTKMR-BATAN. Eleven laboratories took part in the comparison, and all measurements were made using gamma spectrometry, on point sources with an activity between 2000 Bq and 6000 Bq. Several laboratories reported values which were more than 10% different from the reference value for 131I and 133Ba. Possible reasons for these differences are discussed. This program will be continued with other radionuclides to maintain and control quality assurance for the local laboratories. - Highlights: • PTKMR-BATAN coordinated national comparison of 131I, 60Co and 133Ba. • Eleven laboratories took part in the comparison. • All measurements were done using gamma spectrometry methods. • For 131I and 133Ba, 3 laboratories have more than 10% difference from reference laboratory value

  5. The early development of hypothyroidism after 131I treatment for hyperthyroid Graves' disease

    827 patients with Graves' hyperthyroidism following 131I treatment were followed up at 3 monthly intervals for 12∼36 months from 1985 to 1991. Physical examination and serum total T3, T4, TSH measurements were made at each visit. According to the authors data, 90% early hypothyroidism occurred within 2∼3 months after 131I treatment, thereby, careful follow-up study is very important during this period. T4 was much more sensitive than T3 in diagnosing early hypothyroidism, while the TSH level shows thyroid reservation function, and is less sensitive than T4 in diagnosing 131I induced hypothyroidism. The study confirmed the view that the early incidence of post 131I therapy hypothyroidism was strongly dose dependent

  6. The change of serum TRAb after 131I radiotherapy in patients of Graves' hyperthyroidism

    Objective: The clinical value of thyrotrophin receptor antibody (TRAb) in patients with Graves' hyperthyroidism was investigated during 131I radiotherapy. Methods: A total of 130 patients with Graves' hyperthyroidism and 50 normal controls were included in the study. Serum concentration of TRAb was measured by radioreceptor assay (RRA) before and at 3, 6, 12 and 24 months after 131I radiotherapy. Results: Abnormally higher TRAb level [(92.93±68.99)U/L] was noted in patients before treatment(P131I radiotherapy, the TRAb [(12.99±5.52) U/L] was back to normal with no difference to that of controls (P>0.05). Conclusion: Serum concentration of TRAb was of clinical significance in the diagnosis of Graves' hyperthyroidism and in the monitoring of 131I radiotherapy. (authors)

  7. Current trend of research on 131I therapy for thyroid diseases

    At present time, there are two current trends of research on 131I therapy for thyroid diseases. The first is extension of the application on the field of thyroid diseases. Formerly, the authors use the 131I only on the hyperthyroidism of Graves' disease, plummer's disease or toxic nodular goiter as well as thyroid cancer, but now, also for some thyroid diseases with normal thyroid function, such as nontoxic multi-nodular goiter, simple diffuse goiter even the thyroid cyst. It seems quite rational to use the 131I more widely, because it is really safe, easy and cheaper than others. The second trend is using 131I combined together with other drugs in order to reduce the occurrence of hypothyroidism and enhance the therapeutic effect. Authors call it as combined therapy. Drugs recommended for such therapy are antithyroid drugs, β-adrenergic receptor blocking agents, thyroid hormone, gtucocorticoid as well as Chinese herb drugs and so on

  8. 131I therapy of teen-age hyperthyroidism: the primary results in 46 patients

    Objective: To explore various conditions of teen-age hyperthyroidism with 131I therapy. Methods: 46 patients were administrated with 131I, the changes of T3 and T4 level of serum were tested by radioimmunoassay. The improvement of clinical symptoms has been observed in 46 cases with teen-age hyperthyroidism by 131I before and after treatment. Results: 39 of 46 (84%) has been proved complete responses (CR), partial responses (PR) 7 cases. 3 months later; we found that 39 patients have hypothyroidism symptoms, T3 and T4 level of serum decreased. There are significance increases of TSH 23 percent patients. Conclusion: It has been proved that treatment of teen-age hyperthyroidism by 131I is effective and safe

  9. Local delivery of 131I-MIBG to treat peritoneal neuroblastoma

    Internal radiotherapy involving systemic administration of iodine-131 metaiodobenzylguanidine (131I-MIBG) in neural crest tumours such as neuroblastoma has shown considerable success. Although peritoneal seeding of neuroblastoma occurs less often than metastases to organs such as the liver, no effective treatments exist in this clinical setting. Previous reports have demonstrated the effectiveness of peritoneal application of chemotherapeutic drugs or radiolabelled monoclonal antibodies in several kinds of carcinomas. Local delivery of 131I-MIBG should produce more favourable dosimetry in comparison with its systemic administration in the treatment of peritoneal neuroblastoma. In the current investigation, a peritoneal model of neuroblastoma was established in Balb/c nu/nu mice by i.p. injection of SK-N-SH neuroblastoma cells. Two weeks after cell inoculation, comparative biodistribution studies were performed following i.v. or i.p. administration of 131I-MIBG. Mice were treated with 55.5 MBq of 131I-MIBG administered either i.v. or i.p. at 2 weeks. Intraperitoneal injection of 131I-MIBG produced significantly higher tumour accumulation than did i.v. injection (P131I-MIBG failed to improve the survival of mice; mean survival of untreated mice and mice treated with i.v. administration of 131I-MIBG was 59.3±3.9 days and 60.6±2.8 days, respectively. On the other hand, radiotherapy delivered via i.p. administration of 131I-MIBG prolonged survival of mice to 94.7±17.5 days (P131I-MIBG therapy). Radiation doses absorbed by tumours at 55.5 MBq of 131I-MIBG were estimated to be 4,140 cGy with i.p. injection and 450 cGy with i.v. injection. These results indicate the benefits of locoregional delivery of 131I-MIBG in the treatment of peritoneal neuroblastoma. (orig.)

  10. Behavior of medically-derived 131I in the tidal Potomac River

    Iodine-131 (t1/2 = 8.04 d) is administered to patients for treatment of thyroid disorders, excreted by patients and discharged to surface waters via sewage effluent. Radionuclides generally behave like their stable analogs; therefore, medically-derived 131I is useful as a transport-reaction tracer of anthropogenic inputs and the aquatic biogeochemistry of iodine. Iodine-131 was measured in Potomac River water and sediments in the vicinity of the Blue Plains Water Pollution Control Plant (WPCP), Washington, DC, USA. Concentrations measured in sewage effluent from Blue Plains WPCP and in the Potomac River suggest a relatively continuous source of this radionuclide. The range of 131I concentrations detected in surface water was 0.076 ± 0.006 to 6.07 ± 0.07 Bq L−1. Iodine-131 concentrations in sediments ranged from 1.3 ± 0.8 to 117 ± 2 Bq kg−1 dry weight. Partitioning in the sewage effluent from Blue Plains and in surface waters indicated that 131I is associated with colloidal and particulate organic material. The behavior of medically-derived 131I in the Potomac River is consistent with the nutrient-like behavior of natural iodine in aquatic environments. After discharge to the river via sewage effluent, it is incorporated into biogenic particulate material and deposited in sediments. Solid phase sediment profiles of 131I indicated rapid mixing or sedimentation of particulate debris and diagenetic remineralization and recycling on short time scales. - Highlights: ► Medically-derived 131I was measured in sewage effluent, river water, and sediments. ► Sediment 210Pb and 7Be profiles help characterize the sedimentary environment. ► 131I flux to sediments in study area is ∼ 1% of that discharged in sewage effluent. ► 131I distributions constrain reaction-transport processes to weekly time scales. ► Collectively these data are used to better understand iodine biogeochemistry