Current radiopharmaceuticals最新文献

The low range of alpha particles provides an opportunity to better target cancer cells theoretically leading to the introduction of interesting alpha emitter radiopharmaceuticals including ²²⁵Ac, ²¹²Pb, etc. The combination of high energy and short range of alpha emitters differentiates targeted radiotherapy from other methods and reduces unwanted cytotoxicity of the cells around the tumoral tissue. Among interesting alpha emitters candidates for targeted therapy, ²¹¹At, one of the radioisotopes with the best optimal decay properties, shows great promise for targeted radiotherapy in some animal prostate cancer xenograft studies and bone micro tumors with significant effects compared to other beta and alpha emitters and also demonstrates interesting properties for clinical applications. However, production and application of this alpha emitter in the development of actinium-based radiopharmaceuticals is hampered by many obstacles. This mini-review demonstrates ²¹¹At production methods, chemical separation, radiolabeling procedures, ²¹¹At-radiopharmaceuticals and their clinical trials, transport, logistics, and costs and future trends in the field for ultimate clinical applications. This review showed that there are limited clinical trials on ²¹¹Ac-based radiopharmaceuticals, which is due to the low accessibility of this radioisotope and other limitations. However, the development programs of major industries indicate the development of ²¹¹Ac-based radiopharmaceuticals in the future.

Introduction: The aim of this work was to prepare a selective nuclear medicine imaging probe for the Endothelin 1 receptor A in the brain.

Material and methods: Ferulic acid (an ETRA antagonist) was radiolabeled using ¹³¹I by direct electrophilic substitution method. The radiolabeled ferulic acid was formulated as polymeric micelles to allow intranasal brain delivery. Biodistribution was studied in Swiss albino mice by comparing brain uptake of ¹³¹I-ferulic acid after IN administration of ¹³¹I-ferulic acid polymeric micelles, IN administration of ¹³¹I-ferulic acid solution and IV administration of ¹³¹I-ferulic acid solution.

Results: Successful radiolabeling was achieved with an RCY of 98 % using 200 μg of ferulic acid and 60 μg of CAT as oxidizing agents at pH 6, room temperature and 30 min reaction time. ¹³¹I-ferulic acid polymeric micelles were successfully formulated with the particle size of 21.63 nm and polydispersity index of 0.168. Radioactivity uptake in the brain and brain/blood uptake ratio for I.N ¹³¹I-ferulic acid polymeric micelles were greater than the two other routes at all periods.

Conclusion: Our results provide ¹³¹I-ferulic acid polymeric micelles as a hopeful nuclear medicine tracer for ETRA brain receptor.

Diagnostic and interventional angiograms are instrumental in the multidisciplinary approach to CAD management, enabling accurate diagnosis and effective targeted treatments that significantly enhance patient care and cardiovascular outcomes. However, cath lab staff, including interventional cardiologists, is consistently exposed to ionizing radiation, which poses inherent health risks. Radiation exposure in the cath lab primarily results from the use of fluoroscopy and cineangiography during diagnostic and interventional procedures. Understanding these risks and implementing effective radiation protection measurements are imperative to ensure the well-being of healthcare professionals while delivering high-quality cardiac care. Prolonged and repeated exposure can lead to both deterministic and stochastic effects. Deterministic effects, such as skin erythema and tissue damage, are more likely to occur at high radiation doses. Interventional cardiologists and staff may experience these effects when safety measures are not rigorously followed. In fact, while ionizing radiation is essential in the practice of radiation cardiology ward, cath lab staff faces inherent risks from radiation exposure. Stochastic effects, on the other hand, are characterized by a probabilistic relationship between radiation exposure and the likelihood of harm. These effects include the increased risk of cancer, particularly for those with long-term exposure. Interventional cardiologists, due to their frequent presence in the cath lab, face a higher lifetime cumulative radiation dose, potentially elevating their cancer risk. Protective measures, including the use of lead aprons, thyroid shields, and radiation monitoring devices, play a crucial role in reducing radiation exposure for cath lab personnel. Adherence to strict dose optimization protocols, such as minimizing fluoroscopy time and maximizing distance from the radiation source, is also essential in mitigating these risks. Ongoing research and advancements in radiation safety technology are essential in further for minimizing the adverse effects of ionizing radiation in the cath lab.

Background: Radiotherapy plays a vital role in the management of high-grade gliomas. However, the radio resistance of glioma cells limits the effect of radiation and drives recurrence inside the irradiated tumor volume leading to poor outcomes for patients.

Methods: High-grade glioma cell radioresistance significantly contributes to radiotherapy failure, highlighting the importance of identifying predictive biomarkers for radioresistance. An increasing body of evidence complies with the Yes Associated Protein 1 (Yap-1) and heat shock protein 90 (Hsp90) as biomarkers for radioresistance in glioma cells. A number of studies suggest the potential of radioresistance-associated factors as biomarkers and/ or novel therapeutic targets in glioma cells. Thus, it is essential for glioblastoma patients to identify robust druggable targets involved in radioresistance, optimizing irradiation protocol, and understanding their underlying molecular mechanisms.

Results: Therefore, in the present study, we hypothesized that hypofractionated Gamma Knife radiation therapy (HF-GKRT) could target Yap-1 and Hsp90 and downregulate the mechanism of radioresistance in high-grade glioma cells.

Conclusion: For this purpose, expression levels of radioresistance markers Yap-1 and Hsp90 were evaluated after treatment with HF-GKRT, and this was compared with single fraction Gamma Knife radiation therapy (SF-GKRT) in U87MG primary human glioblastoma cell line model. This would help design a novel radiation therapy regimen for glioblastoma patients by reducing the risk of radioresistance.

Objective: This study aimed to construct a nomogram based on clinical and ultrasound (US) features to predict breast malignancy in males.

Methods: The medical records between August, 2021 and February, 2023 were retrospectively collected from the database. Patients included in this study were randomly divided into training and validation sets in a 7:3 ratio. The models for predicting the risk of malignancy in male patients with breast lesions were virtualized by the nomograms.

Results: Among the 71 enrolled patients, 50 were grouped into the training set, while 21 were grouped into the validation set. After the multivariate analysis was done, pain, BI-RADS category, and elastography score were identified as the predictors for malignancy risk and were selected to generate the nomogram. The C-index was 0.931 for the model. Concordance between predictions and observations was detected by calibration curves and was found to be good in this study. The model achieved a net benefit across all threshold probabilities, which was shown by the decision curve analysis (DCA) curve.

Conclusion: We successfully constructed a nomogram to evaluate the risk of breast malignancy in males using clinical and US features, including pain, BI-RADS category, and elastography score, which yielded good predictive performance.

Crocetin is a kind of apocarotenoid carboxylic acid extracted from saffron (Crocus sativus L.), which is effective in upregulating tissue oxygenation. However, crocetin is difficult to solubilize. It was shown that the trans isomer of crocetin is effective in improving oxygen diffusivity, while its cis isomer appears not to be. Hence, the isolated trans isomer of crocetin or trans-sodium crocetinate (TSC) can be used instead of crocetin. It is shown that TSC can upregulate hypoxic tissue oxygenation and be effective in treating some hypoxia-related diseases. Moreover, experimental and clinical studies have reported no adverse effects following TSC treatment, even at high doses. The current study will discuss the potential role of TSC in hemorrhagic shock, ischemia, brain tumor radiotherapy, and others.

Radiotherapy (RT) failure has historically been mostly attributed to radioresistance. Ferroptosis is a type of controlled cell death that depends on iron and is caused by polyunsaturated fatty acid peroxidative damage. Utilizing a ferroptosis inducer may be a successful tactic for preventing tumor growth and radiotherapy-induced cell death. A regulated form of cell death known as ferroptosis is caused by the peroxidation of phospholipids containing polyunsaturated fatty acids in an iron-dependent manner (PUFA-PLs). The ferroptosis pathway has a number of important regulators. By regulating the formation of PUFA-PLs, the important lipid metabolism enzyme ACSL4 promotes ferroptosis, whereas SLC7A11 and (glutathione peroxidase 4) GPX4 prevent ferroptosis. In addition to introducing the ferroptosis inducer chemicals that have recently been demonstrated to have a radiosensitizer effect, this review highlights the function and methods by which ferroptosis contributes to RT-induced cell death and tumor suppression in vitro and in vivo.

Ovarian disease constitutes various types of endocrine disorders, such as polycystic ovarian syndrome (PCOS), ovarian cancer, premature ovarian failure, ovarian endometriosis, and ovarian cysts. The prevalence of ovarian-related diseases is highly vulnerable in the world. The utility of various drug delivery systems for ovarian diseases has resulted in varied success. Moreover, most of them lead to severe adverse effects and are incapable of ameliorating the signs and symptoms of the condition. Intrauterine devices (IUDs) have positioned themselves as a mechanism to deliver the drug for various ovarian-related diseases. Thereby avoiding various stability-related issues arising due to various physiological barriers of the female reproductive tract. However, the use of intrauterine devices for drug delivery to the ovaries has not been fully explored. This is attributed to the fact that they cause cysts in the ovaries and skepticism among patients and physicians. Photo-sensitive devices are an appealing approach for managing disorders affecting the ovaries. Photo-sensitive in situ forming intrauterine implants (IUIs) have several advantages, including simplicity in application, reduced invasiveness, as well as improved site-specific drug release control. Polymeric nanoparticles (PNPs) loaded with a drug may be a suitable choice to provide sustained release, alter the pharmacokinetics, and reduce the dose and dosing frequency. The current manuscript hypothesizes the utility of a PNP-loaded biodegradable photo-responsive intrauterine implantable device as an alternate novel strategy for ameliorating ovarian-related diseases.

Aim: This study investigated the protective effects of three antioxidants on radiationinduced lung injury.

Background: Oxidative stress is one of the key outcomes of radiotherapy in normal tissues. It can induce severe injuries in lung tissue, which may lead to pneumonitis and fibrosis. Recently, interest in natural chemicals as possible radioprotectors has increased due to their reduced toxicity, cheaper price, and other advantages.

Objective: The present study was undertaken to evaluate the radioprotective effect of Alpha-lipoic Acid (LA), Resveratrol (RVT), and Apigenin (APG) against histopathological changes and oxidative damage and survival induced by ionizing radiation (IR) in the lung tissues of rats.

Methods: First, the lung tissue of 50 mature male Wistar rats underwent an 18 Gy gamma irradiation. Next, the rats were sacrificed and transverse sections were obtained from the lung tissues and stained with hematoxylin and eosin (H and E) and Mason trichrome (MTC) for histopathological evaluation. Then, the activity of Glutathione peroxidase (GPx), Superoxide Dismutase (SOD), and Malondialdehyde (MDA) was measured by an ELISA reader at 340, 405, and 550 nm.

Results: Based on the results of this study, IR led to a remarkable increase in morphological changes in the lung. However, APG, RVT, and LA could ameliorate the deleterious effects of IR in lung tissue. IR causes an increase in GPX level, and APG+IR administration causes a decrease in the level of GPX compared to the control group. Also, the results of this study showed that RVT has significant effects in reducing MDA levels in the short term. In addition, compared to the control group, IR and RVT+IR decrease the activity of SOD in the long term in the lung tissues of rats. Also, the analysis of results showed that weight changes in IR, LA+IR, APG+IR, and control groups were statistically significant.

Conclusion: APG and RVT could prevent tissue damage induced by radiation effects in rat lung tissues. Hence, APG, LA, and RVT could provide a novel preventive action with their potential antioxidant anti-inflammatory properties, as well as their great safety characteristic.

Recent advancements in biomedicine have seen a significant reliance on nanoengineering, as traditional methods often fall short in harnessing the unique attributes of biomaterials. Nanoengineering has emerged as a valuable approach to enhance and enrich the performance and functionalities of biomaterials, driving research and development in the field. This review emphasizes the most prevalent biomaterials used in biomedicine, including polymers, nanocomposites, and metallic materials, and explores the pivotal role of nanoengineering in developing biomedical treatments and processes. Particularly, the review highlights research focused on gaining an in-depth understanding of material properties and effectively enhancing material performance through molecular dynamics simulations, all from a nanoengineering perspective.