Current radiopharmaceuticals最新文献

Background: Myelosuppression is common and threatening during tumor treatment. However, the effect of radiation on bone marrow activity, especially leukocyte count, has been underestimated in cervical cancer. The aim of this study was to evaluate the severity of radiotherapy- induced acute leukopenia and its relationship with intestinal toxicity.

Methods: The clinical data of 59 patients who underwent conventional radiation alone for cervical cancer were retrospectively analyzed. The patients had normal leukocyte count on admission, and the blood cell count, gross tumor volume (GTV) dose, and intestinal toxicity were evaluated.

Results: During radiotherapy (RT), 47 patients (79.7%) developed into leukopenia, with 38.3% mild and 61.7% moderate. The mean time for leukopenia was 9 days. Compared with leukopenianegative patients, leukopenia-positive ones had lower baseline leukocyte count, while neutrophil/ lymphocyte (NLR) and monocyte/lymphocyte (MLR) showed no significance. Logistic regression analysis indicated that excluding the factors for age, body mass index (BMI), TNM stage, surgery and GTV dose, baseline leukocyte count was an important independent predictor of leukopenia (OR=0.383). During RT, a significant reduction was found in leukocyte, neutrophil and lymphocyte count at week 2 while monocyte count after 2 weeks. Furthermore, NLR and MLR showed a significant and sustained upward trend. About 54.2% of patients had gastrointestinal symptoms. However, no significant relevance was noted between leukocyte count as well as NLR/MLR and intestinal toxicity, indicating leukopenia may not be the main factor causing and aggravating gastrointestinal reaction in cervical cancer.

Conclusion: Our results suggest the underrated high prevalence and severity of leukopenia in cervical cancer patients receiving RT, and those with low baseline leukocyte count are more likely for leukopenia, for whom early prevention of infection may be needed during RT.

Introduction: F18 and Ga68 radioisotopes are used in PET imaging for prostate cancer. It was aimed to calculate the prostate, testicle and bladder effective doses (ED) caused by F18 and Ga68 used in prostate cancer imaging with PET/CT via simulation with the GATE toolkit and evaluate the ED in terms of fertility.

Methods: The prostate, testicle and bladder were defined together with their geometric properties and densities in GATE simulation. F18 and Ga68 with activity of 277.5 MBq and 151.7 MBq were identified in the prostate as a source organ. The ED, uncertainties, and S values were taken as an output file in the TXT format with the DoseActors command. S values were used for validation of the simulation.

Results: The ED of the prostate, total testicle and bladder for F18 were found to be 6.627E-04 ± 1.799E-06, 12.74E-07 ± 4.11E-08 and 1.617E-05 ± 4.317E-09 (Gy/s), respectively. The ED of the prostate, total testicle, and bladder for Ga68 were found to be 9.195E-04 ± 2.660E-06, 6.54E-07 ± 2.93E-08 and 4.290E-05 ± 6.936E-09 (Gy/s), respectively.

Conclusion: It was found that Ga68 produced high prostate and bladder ED, and F18 produced high testicular ED. In terms of male fertility, Ga68 seems to be a good alternative because it produces low testicular doses. The ED of the testicle both F18 and Ga68 were below the reported spermatogonia and azoospermia dose.

Background: During the development of novel Re-188 radiopharmaceuticals, it was discovered that no calibration settings were published to calibrate Re-188 on the Capintec CRC-25PET dose calibrator.

Methods: Sodium [¹⁸⁸Re]perrhenate was eluted from an OncoBeta ¹⁸⁸W/¹⁸⁸Re generator to measure activity on a Capintec CRC-25R dose calibrator using established dose calibrator settings provided by the manufacturer. The eluent was then used to tune the calibra on settings on a Capintec CRC-25PET dose calibrator, accounting for geometry. Radionuclidic purity of the [¹⁸⁸Re]perrhenate source was verified via gamma spectroscopy.

Results: The calibrator number for Re-188 was determined to be 469 x 10 for the Capintec CRC-25PET dose calibrator, which differed from the manufacturer provided calibra on number of 496 x 10 for the Capintec CRC-25R dose calibra on model. W-188 breakthrough was characterised as < 0.01%.

Conclusion: This previously unreported calibration number can be used to determine the activity of Re- 188 labelled radiopharmaceuticals using the Capintec CRC-25PET dose calibrator model.

Background: HYNIC-Bombesin (BBN) is a potential peptide for targeted radionuclide therapy in gastrin-releasing peptide receptor (GRPr)-positive malignancies. The ¹⁸⁸Re-HYNICBBN is a promising radiopharmaceutical for use in prostate cancer therapy.

Objective: The aim of this study was to estimate the absorbed dose due to ¹⁸⁸Re-HYNIC-BBN radio-complex in human organs based on bio-distribution data of rats.

Methods: In this research, using bio-distribution data of ¹⁸⁸Re-HYNIC-BBN in rats, its radiation absorbed dose of the adult human was calculated for different organs based on the MIRD dose calculation method.

Results: A considerable equivalent dose amount of ¹⁸⁸Re-Hynic-BBN (0.093 mGy/MBq) was accumulated in the prostate. Moreover, all other tissues except for the kidneys and pancreas approximately received insignificant absorbed doses.

Conclusion: Since the acceptable absorbed dose for the complex was observed in the prostate, ¹⁸⁸Re-Hynic-Bombesin can be regarded as a new potential agent for prostate cancer therapy.

Background: In recent years, there has been a significant increase in studies investigating the potential use of plant-origin products in the treatment and diagnosis of different types of cancer.

Methods: In this study, Estragole (EST) was isolated from basil leaves via ethanolic extraction using an 80% ethanol concentration. The isolation process was performed using the High Performance Liquid Chromatography (HPLC) method. The EST isolated from the basil plant was radiolabeled with ¹³¹I using the iodogen method. Quality control studies of the radiolabeled EST (¹³¹IEST) were carried out by using Thin Layer Radio Chromatography (TLRC). Next, in vitro cell, culture studies were done to investigate the bio-affinity of plant-originated EST labeled with ¹³¹I on human medulloblastoma (DAOY) and human glioblastoma-astrocytoma (U-87 MG) cell lines. Finally, the cytotoxicity of EST was determined, and cell uptake of ¹³¹I-EST was investigated on cancer cell lines by incorporation studies.

Results: As a result of these studies, it has been shown that ¹³¹I-EST has a significant uptake on the brain cells.

Conclusion: This result is very satisfying, and it has encouraged us to do in vivo studies for the molecule in the future.

The use of the one-of-a-kind qualities possessed by substances at the nanoscale is the core concept of nanotechnology. Nanotechnology has become increasingly popular in various business sectors because it enables better construction and more advanced product design. Nanomedicine is the name given to the application of nanotechnology in the medical and healthcare fields. It has been used to fight against some of the most prevalent diseases, such as cancer and cardiovascular diseases. This current manuscript provides an overview of the recent advancements in nanotechnology in drug delivery and imaging.

Targeted Alpha Therapy (TAT) is considered an evolving therapeutic option for cancer cells, in which a carrier molecule labeling with an α-emitter radionuclide make the bond with a specific functional or molecular target. α-particles with high Linear Energy Transfer (LET) own an increased Relative Biological Effectiveness (RBE) over common β-emitting radionuclides. Normal tissue toxicity due to non-specific uptake of mother and daughter α-emitter radionuclides seems to be the main conflict in clinical applications. The present survey reviews the available preclinical and clinical studies investigating healthy tissue toxicity of the applicable α -emitters and particular strategies proposed for optimizing targeted alpha therapy success in cancer patients.

Background: During a radiological or nuclear disaster, exposure to a high dose of ionizing radiation usually results in cardiovascular diseases such as heart failure, attack, and ischemia.

Objective: The purpose of this study was to examine the mitigation effects of Spirulina in comparison to Metformin's.

Methods: 25 male Wistar rats were randomly assigned to five groups (5 rats in each): for the control group, rats did not receive any intervention. In group 2, spirulina was administered orally to rats. In group 3, rats were irradiated to the chest region with 15 Gray(Gy) x-radiation. In groups 4 and 5, rats were irradiated in the same way as group 3. Forty-eight hours after irradiation, treatment with Spirulina and Metformin began. All rats were sacrificed after ten weeks, and their heart tissues were removed for histopathological and biochemical assays.

Results: Results showed an elevation in Malondialdehyde (MDA) and decreasing superoxide dismutase (SOD) activity. Moreover, pathological changes of radiation were irregularities in the arrangement of myofibrils, proliferation, migration of mononuclear cells, vacuolation of the cytoplasm, and congestion. Administration of spirulina enhanced the SOD activity while did not affect MDA level and pathological change in heart tissue. Despite spirulina, metformin had a considerable effect on pathological lesions and decreased the level of MDA.

Conclusion: Reactive oxygen species (ROS) may be involved in the late effects of radiationinduced heart injury, and scavenging these particles may contribute to reduced radiation side effects. Based on these results, Spirulina had no effect on radiation-induced cardiac damage, while metformin did. Higher Spirulina doses given over a longer period of time will likely have a greater heart-mitigate effect.

Background: Glioblastoma is the most common primary malignant tumor of the central nervous system. The patient's median survival rate is 13.5 months, so it is necessary to explore new therapeutic approaches.

Objective: Extremely low-frequency electromagnetic field (EMF) has been explored as a noninvasive cancer treatment. This study applied the EMF with previous conventional chemoradiotherapy for glioblastoma.

Methods: In this study, we evaluated the cytotoxic effects of EMF (50 Hz, 100 G), temozolomide (TMZ), and radiation (Rad) on gene expression of T98 glioma cell lines in monolayer and spheroid cell cultures.

Results: Treatment with Rad and EMF significantly increased apoptosis-related gene expression compared to the control group in monolayers and spheroids (p<0.001). The expression of apoptotic-related genes in monolayers was higher than the similar spheroid groups (p<0.001). We found that treatment with TMZ and EMF could increase the gene expression of the autophagy cascade markers compared to the control group (p<0.001). Autophagy-related gene expression in spheroids was higher than in the similar monolayer group (p<0.001). We demonstrated that coadministration of EMF, TMZ, and Rad significantly reduced cell cycle and drug resistance gene expression in monolayers and spheroids (p<0.001) compared to the control group.

Conclusion: The combinational use of TMZ, Rad and, EMF showed the highest antitumor activity by inducing apoptosis and autophagy signaling pathways and inhibiting cell cycle and drug resistance gene expression. Furthermore, EMF increased TMZ or radiation efficiency.

Background: Radiopharmaceuticals labeled with [⁶⁸Ga] from positron emission tomography (PET) radionuclides are utilized in nuclear medicine for non-invasive in vivo molecular imaging. Buffer solutions for radiolabeling play an important role as choosing the right buffer for the reaction helps to obtain high yield radiopharmaceuticals. Zwitterionic organic buffer 4-(2- hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES), sodium acetate (CH₃COONa), sodium bicarbonate (NaHCO₃) buffers are widely used for labeling of peptides with [⁶⁸Ga]Cl₃. They can be used for peptide labelings with the acidic [⁶⁸Ga]Cl₃ precursor of triethanolammonium (TEA) buffer. The cost and toxicity of TAE buffer are relatively low.

Method: For [⁶⁸Ga]GaPSMA-HBED-CC and [⁶⁸Ga]GaDOTA-TATE labeling, the effectiveness of TEA buffer without chemical impurities in radiolabeling reactions and QC parameters in successful labeling was investigated.

Results: The method used to label [⁶⁸Ga]Cl₃ with PSMA-HBED-CC peptide in the presence of TEA buffer was successful when applied at room temperature. High purity radiosynthesis suitable for clinical use was performed to obtain DOTA-TATE peptide with the addition of 363K temperature and radical scavenger. Quality control tests with R-HPLC have shown that this method is suitable for clinical use.

Conclusion: We present an alternative procedure for labeling PSMA-HBED-CC and DOTATATE peptides with [⁶⁸GaCl₃] to obtain high radioactive doses of final radiopharmaceutical products used in nuclear medicine clinical applications. We have provided a quality-controlled final product that can be used in clinical diagnostic procedures. With the use of an alternative buffer, these methods could be adapted to semi-automatic or automated modules routinely used in nuclear medicine laboratories to label [⁶⁸Ga]-based radiopharmaceuticals.