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1.
Pharmaceutics ; 16(3)2024 Mar 15.
Artigo em Inglês | MEDLINE | ID: mdl-38543298

RESUMO

It is evident that radiolabeled drug delivery systems hold great promise in the field of lung cancer management. The combination of therapeutic agents with radiotracers not only allows for precise localization within lung tumors but also enables real-time monitoring of drug distribution. This approach has the potential to enhance targeted therapy and improve patient outcomes. The integration of advanced imaging modalities, such as positron emission tomography (PET) and single-photon emission computed tomography (SPECT), has played a crucial role in the non-invasive tracking of radiolabeled drugs. These techniques provide valuable insights into drug pharmacokinetics, biodistribution, and tumor-targeting efficiency, offering clinicians the ability to personalize treatment regimens. The comprehensive analysis of preclinical and clinical studies presented in this review underscores the progress made in the field. The evidence suggests that radiolabeled drug delivery systems have the potential to revolutionize oncology by offering precise, targeted, and image-guided therapeutic interventions for lung cancer. This innovative approach not only enhances the effectiveness of treatment but also contributes to the development of personalized medicine strategies, tailoring interventions to the specific characteristics of each patient's cancer. The ongoing research in this area holds promise for further advancements in lung cancer management, potentially leading to improved outcomes and quality of life for patients.

2.
Ther Deliv ; 2024 Mar 12.
Artigo em Inglês | MEDLINE | ID: mdl-38469701

RESUMO

Aim: This study explores chia oil, rich in ω-3 fatty acids and nutraceutical components, as a potential remedy for diseases, especially those linked to inflammation and cancer. Methods/materials: A chia oil-based nanoemulsion, developed through single emulsification, underwent comprehensive analysis using various techniques. In vitro and in vivo assays, including macrophage polarization, nitrite and cytokine production, cellular uptake and biodistribution, were conducted to assess the anti-inflammatory efficacy. Results & conclusion: Results reveal that the chia nanoemulsion significantly inhibits inflammation, outperforming pure oil with twice the efficacy. Enhanced uptake by macrophage-like cells and substantial accumulation in key organs indicate its potential as an economical and effective anti-inflammatory nanodrug, addressing global economic and health impacts of inflammation-related diseases.

3.
ACS Chem Neurosci ; 15(4): 699-715, 2024 Feb 21.
Artigo em Inglês | MEDLINE | ID: mdl-38305187

RESUMO

Atomic force microscopy (AFM) is a scanning probe microscopy technique which has a physical principle, the measurement of interatomic forces between a very thin tip and the surface of a sample, allowing the obtaining of quantitative data at the nanoscale, contributing to the surface study and mechanical characterization. Due to its great versatility, AFM has been used to investigate the structural and nanomechanical properties of several inorganic and biological materials, including neurons affected by tauopathies. Tauopathies are neurodegenerative diseases featured by aggregation of phosphorylated tau protein inside neurons, leading to functional loss and progressive neurotoxicity. In the broad universe of neurodegenerative diseases, tauopathies comprise the most prevalent, with Alzheimer's disease as its main representative. This review highlights the use of AFM as a suitable research technique for the study of cellular damages in tauopathies, even in early stages, allowing elucidation of pathogenic mechanisms of these diseases.


Assuntos
Doença de Alzheimer , Doenças Neurodegenerativas , Tauopatias , Humanos , Microscopia de Força Atômica/métodos , Tauopatias/metabolismo , Proteínas tau/metabolismo , Doença de Alzheimer/metabolismo , Doenças Neurodegenerativas/metabolismo , Neurônios/metabolismo
4.
Pharmaceutics ; 16(2)2024 Feb 08.
Artigo em Inglês | MEDLINE | ID: mdl-38399306

RESUMO

Infectious and Parasitic Diseases (IPD) remain a challenge for medicine due to several interconnected reasons, such as antimicrobial resistance (AMR). American tegumentary leishmaniasis (ATL) is an overlooked IPD causing persistent skin ulcers that are challenging to heal, resulting in disfiguring scars. Moreover, it has the potential to extend from the skin to the mucous membranes of the nose, mouth, and throat in both humans and various animals. Given the limited effectiveness and AMR of current drugs, the exploration of new substances has emerged as a promising alternative for ATL treatment. Arrabidaea brachypoda (DC). Bureau is a native Brazilian plant rich in dimeric flavonoids, including Brachydin (BRA), which displays antimicrobial activity, but still little has been explored regarding the development of therapeutic formulations. In this work, we present the design of a low-cost liquid formulation based on the use of Pluronic F127 for encapsulation of high BRA concentration (LF-B500). The characterization techniques revealed that BRA-loaded F127 micelles are well-stabilized in an unusual worm-like form. The in vitro cytotoxicity assay demonstrated that LF-B500 was non-toxic to macrophages but efficient in the inactivation of forms of Leishmania amazonensis promastigotes with IC50 of 16.06 µg/mL. The results demonstrated that LF-B500 opened a new perspective on the use of liquid formulation-based natural products for ATL treatment.

5.
Exp Eye Res ; 240: 109791, 2024 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-38253307

RESUMO

The cornea is a fundamental ocular tissue for the sense of sight. Thanks to it, the refraction of two-thirds of light manages to participate in the visual process and protect against mechanical damage. Because it is transparent, avascular, and innervated, the cornea comprises five main layers: Epithelium, Bowman's layer, stroma, Descemet's membrane, and endothelium. Each layer plays a key role in the functionality and maintenance of ocular tissue, providing unique ultrastructural and biomechanical properties. Bullous Keratopathy (BK) is an endothelial dysfunction that leads to corneal edema, loss of visual acuity, epithelial blisters, and severe pain, among other symptoms. The corneal layers are subject to changes in their biophysical properties promoted by Keratopathy. In this context, the Atomic Force Microscopy (AFM) technique in air was used to investigate the anterior epithelial surface and the posterior endothelial surface, healthy and with BK, using a triangular silicone tip with a nominal spring constant of 0.4 N/m. Six human corneas (n = 6) samples were used for each analyzed group. Roughness data, calculated by third-order polynomial adjustment, adhesion, and Young's modulus, were obtained to serve as a comparison and identification of morphological and biomechanical changes possibly associated with the pathology, such as craters and in the epithelial layer and exposure of a fibrotic layer due to loss of the endothelial cell wall. Endothelial cell membrane area and volume data were calculated, obtaining a relevant comparison between the control and patient. Such results may provide new data on the physical properties of the ocular tissue to understand the physiology of the cornea when it has pathology.


Assuntos
Doenças da Córnea , Edema da Córnea , Humanos , Endotélio Corneano/metabolismo , Lâmina Limitante Posterior/metabolismo , Edema da Córnea/metabolismo , Córnea/patologia , Doenças da Córnea/patologia
6.
Int J Pharm ; 652: 123765, 2024 Mar 05.
Artigo em Inglês | MEDLINE | ID: mdl-38195032

RESUMO

Despite the successful use of the radiopharmaceutical radium-223 dichloride ([223Ra]RaCl2) for targeted alpha therapy of castration-resistant prostate cancer patients with bone metastases, some short-term side effects, such as diarrhea and vomiting, have been documented, causing patient discomfort. Hence, we prepared a nanosized micellar solution of [223Ra]RaCl2 and evaluated its biodistribution, pharmacokinetics, and induced biochemical changes in healthy mice up to 96 h after intraperitoneal administration as an alternative to overcome the previous limitations. In addition, we evaluated the bone specificity of micellar [223Ra]RaCl2 in patient-derived xenografts in the osteosarcoma model. The biodistribution studies revealed the high bone-targeting properties of the micellar [223Ra]RaCl2. Interestingly, the liver uptake remained significantly low (%ID/g = 0.1-0.02) from 24 to 96 h after administration. In addition, the micellar [223Ra]RaCl2 exhibited a significantly higher uptake in left (%ID/g = 0.85-0.23) and right (%ID/g = 0.76-0.24) kidneys than in small (%ID/g = 0.43-0.06) and large intestines (%ID/g = 0.24-0.09) over time, suggesting its excretion pathway is primarily through the kidneys into the urine, in contrast to the non-micellar [223Ra]RaCl2. The micellar [223Ra]RaCl2 also had low distribution volume (0.055 ± 0.003 L) and longer elimination half-life (28 ± 12 days). This nanosystem was unable to change the enzymatic activities of alanine aminotransferase, aspartate aminotransferase, gamma GT, glucose, and liquiform lipase in the treated mice. Finally, microscopic examination of the animals' osteosarcoma tumors treated with micellar [223Ra]RaCl2 indicated regression of the tumor, with large areas of necrosis. In contrast, in the control group, we observed tumor cellularity and cell anaplasia, mitotic figures and formation of neoplastic extracellular bone matrix, which are typical features of osteosarcoma. Therefore, our findings demonstrated the efficiency and safety of nanosized micellar formulations to minimize the gastrointestinal excretion pathway of the clinical radiopharmaceutical [223Ra]RaCl2, in addition to promoting regression of the osteosarcoma. Further studies must be performed to assess dose-response outcomes and organ/tissue dosimetry for clinical translation.


Assuntos
Neoplasias Ósseas , Osteossarcoma , Neoplasias de Próstata Resistentes à Castração , Humanos , Masculino , Animais , Camundongos , Compostos Radiofarmacêuticos/farmacocinética , Distribuição Tecidual , Eliminação Renal , Neoplasias Ósseas/tratamento farmacológico , Neoplasias Ósseas/radioterapia , Osteossarcoma/tratamento farmacológico , Neoplasias de Próstata Resistentes à Castração/patologia
7.
Curr Med Chem ; 2024 Jan 23.
Artigo em Inglês | MEDLINE | ID: mdl-38265391

RESUMO

INTRODUCTION: Nanoceria is a well-known nanomaterial with various properties, including antioxidant, proangiogenic, and therapeutic effects. Despite its potential, there are still aspects that require further exploration, particularly its anti-inflammatory and antimicrobial activities. METHOD: The global demand for novel anti-inflammatory and antimicrobial drugs underscores the significance of understanding nanoceria in both contexts. In this study, we evaluated the effect of nanoceria on macrophage polarization to better understand its anti-inflammatory effects. Additionally, we investigated the mechanism of action of nanoceria against Cryptococcus neoformans (ATCC 32045), Candida parapsilosis (ATCC 22019), Candida krusei (ATCC 6258), and Candida albicans. RESULT: The results demonstrated that nanoceria can polarize macrophages toward an anti-inflammatory profile, revealing the cellular mechanisms involved in the anti-inflammatory response. Concerning the antimicrobial effect, it was observed that nanoceria have a more pronounced impact on Candida parapsilosis, leading to the formation of pronounced pores on the surface of this species. CONCLUSION: Finally, biochemical analysis revealed transitory alterations, mainly in liver enzymes. The data support the use of nanoceria as a potential anti-inflammatory and antimicrobial drug and elucidate some of the mechanisms involved, shedding light on the properties of this nanodrug.

8.
3 Biotech ; 13(11): 352, 2023 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-37810191

RESUMO

The ineffectiveness of azole drugs in treating Vulvovaginal Candidiasis (VVC) and Recurrent Vulvovaginal Candidiasis (RVVC) due to antifungal resistance of non-albicans Candida has led to the investigation of inorganic nanoparticles with biological activity. Silver nanoparticles (AgNPs) are important in nanomedicine and have been used in various products and technologies. This study aimed to develop a vaginal cream and assess its in vitro antimicrobial activity against Candida parapsilosis strains, specifically focusing on the synergy between AgNPs and miconazole. AgNPs were synthesized using glucose as a reducing agent and sodium dodecyl sulfate (SDS) as a stabilizer in varying amounts (0.50, 0.25, and 0.10 g). The AgNPs were characterized using UV-Visible (UV-Vis) and Fourier-Transform Infrared (FT-IR) spectroscopies, X-Ray Diffraction (XRD), Dynamic Light Scattering (DLS), Scanning Electron Microscopy (SEM), and Energy Dispersive X-Ray Analysis (EDX). Fifty strains of Candida parapsilosis were used to evaluate the synergistic activity. AgNPs synthesized with 0.5 g SDS had an average size of 77.58 nm and a zeta potential of -49.2 mV, while AgNPs with 0.25 g showed 91.22 nm and -47.2 mV, respectively. AgNPs stabilized with 0.1 g of SDS were not effective. When combined with miconazole, AgNPs exhibited significant antifungal activity, resulting in an average increase of 80% in inhibition zones. The cream developed in this study, containing half the miconazole concentration of commercially available medication, demonstrated larger inhibition zones compared to the commercial samples.

9.
Biophys Rev ; 15(4): 611-623, 2023 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-37681101

RESUMO

The world is frequently afflicted by several viral outbreaks that bring diseases and health crises. It is vital to comprehend how viral assemblies' fundamental components work to counteract them. Determining the ultrastructure and nanomechanical characteristics of viruses from a physical standpoint helps categorize their mechanical characteristics, offers insight into new treatment options, and/or shows weak spots that can clarify methods for medication targeting. This study compiles the findings from studies on the ultrastructure and nanomechanical behavior of SARS-CoV-2, ZIKV (Zika virus), and CHIKV (Chikungunya virus) viral particles. With results that uncovered aspects of the organization and the spatial distribution of the proteins on the surface of the viral particle as well as the deformation response of the particles when applied a recurring loading force, this review aims to provide further discussion on the mechanical properties of viral particles at the nanoscale, offering new prospects that could be employed for designing strategies for the prevention and treatment of viral diseases. Supplementary Information: The online version contains supplementary material available at 10.1007/s12551-023-01075-4.

10.
J Funct Biomater ; 14(9)2023 Sep 18.
Artigo em Inglês | MEDLINE | ID: mdl-37754891

RESUMO

Breast cancer is a leading cause of cancer-related mortality among women worldwide, with millions of new cases diagnosed yearly. Addressing the burden of breast cancer mortality requires a comprehensive approach involving early detection, accurate diagnosis, effective treatment, and equitable access to healthcare services. In this direction, nano-radiopharmaceuticals have shown potential for enhancing breast cancer diagnosis by combining the benefits of nanoparticles and radiopharmaceutical agents. These nanoscale formulations can provide improved imaging capabilities, increased targeting specificity, and enhanced sensitivity for detecting breast cancer lesions. In this study, we developed and evaluated a novel nano-radio radiopharmaceutical, technetium-99m ([99mTc]Tc)-labeled trastuzumab (TRZ)-decorated methotrexate (MTX)-loaded human serum albumin (HSA) nanoparticles ([99mTc]-TRZ-MTX-HSA), for the diagnosis of breast cancer. In this context, HSA and MTX-HSA nanoparticles were prepared. Conjugation of MTX-HSA nanoparticles with TRZ was performed using adsorption and covalent bonding methods. The prepared formulations were evaluated for particle size, PDI value, zeta (ζ) potential, scanning electron microscopy analysis, encapsulation efficiency, and loading capacity and cytotoxicity on MCF-7, 4T1, and MCF-10A cells. Finally, the nanoparticles were radiolabeled with [99mTc]Tc using the direct radiolabeling method, and cellular uptake was performed with the nano-radiopharmaceutical. The results showed the formation of spherical nanoparticles, with a particle size of 224.1 ± 2.46 nm, a PDI value of 0.09 ± 0.07, and a ζ potential value of -16.4 ± 0.53 mV. The encapsulation efficiency of MTX was found to be 32.46 ± 1.12%, and the amount of TRZ was 80.26 ± 1.96%. The labeling with [99mTc]Tc showed a high labeling efficiency (>99%). The cytotoxicity studies showed no effect, and the cellular uptake studies showed 97.54 ± 2.16% uptake in MCF-7 cells at the 120th min and were found to have a 3-fold higher uptake in cancer cells than in healthy cells. In conclusion, [99mTc]Tc-TRZ-MTX-HSA nanoparticles are promising for diagnosing breast cancer and evaluating the response to treatment in breast cancer patients.

11.
Pharmaceuticals (Basel) ; 16(8)2023 Aug 15.
Artigo em Inglês | MEDLINE | ID: mdl-37631078

RESUMO

Chagas disease, caused by the Trypanosoma cruzi parasitic protozoan, is a neglected tropical disease (NTD) of significant incidence in Latin America. Transmission to humans and other mammals is mainly via the vector insect from the Reduviidae family, popularly known as the kissing bug. There are other transmission means, such as through congenital transmission, blood transfusions, organ transplantations, and the consumption of contaminated food. For more than 50 years, the disease has been treated with benznidazole and nifurtimox, which are only effective during the acute phase of the disease. In addition to their low efficacy in the chronic phase, they cause many adverse effects and are somewhat selective. The use of nanocarriers has received significant attention due to their ability to encapsulate and release therapeutic agents in a controlled manner. Generally, their diameter ranges from 100 to 300 nanometers. The objective of this scoping review was to perform a search of the literature for the use of nanocarriers as an alternative for improving the treatment of Chagas disease and to suggest future research. Bibliographic searches were carried out in the Web of Science and PubMed scientific databases from January 2012 to May 2023, using the "Chagas disease and Trypanosoma cruzi and nanoparticles" keywords, seeking to gather the largest number of articles, which were evaluated using the inclusion and exclusion criteria. After analyzing the papers, the results showed that nanocarriers offer physiological stability and safety for the transport and controlled release of drugs. They can increase solubility and selectivity against the parasite. The in vitro assays showed that the trypanocidal activity of the drug was not impaired after encapsulation. In the in vivo assays, parasitemia reduction and high survival and cure rates in animals were obtained during both phases of the disease using lower doses when compared to the standard treatment. The scoping review showed that nanocarriers are a promising alternative for the treatment of Chagas disease.

12.
Curr Med Chem ; 2023 Aug 18.
Artigo em Inglês | MEDLINE | ID: mdl-37594105

RESUMO

Radiopharmaceuticals are increasingly playing a leading role in diagnosing, monitoring, and treating disease. In comparison with conventional pharmaceuticals, the development of radiopharmaceuticals does follow the principles of medicinal chemistry in the context of imaging-altered physiological processes. The design of a novel radiopharmaceutical has several steps similar to conventional drug discovery and some particularity. In the present work, we revisited the insights of medicinal chemistry in the current radiopharmaceutical development giving examples in oncology, neurology, and cardiology. In this regard, we overviewed the literature on radiopharmaceutical development to study overexpressed targets such as prostate-specific membrane antigen and fibroblast activation protein in cancer; ß-amyloid plaques and tau protein in brain disorders; and angiotensin II type 1 receptor in cardiac disease. The work addresses concepts in the field of radiopharmacy with a special focus on the potential use of radiopharmaceuticals for nuclear imaging and theranostics.

14.
Toxics ; 11(6)2023 May 30.
Artigo em Inglês | MEDLINE | ID: mdl-37368591

RESUMO

The growing production and application of carbon-based nanomaterials (CNMs) represent possible risks for aquatic systems. However, the variety of CNMs with different physical and chemical properties and different morphology complicate the understanding of their potential toxicity. This paper aims to evaluate and compare the toxic impact of the four most common CNMs, namely multiwalled carbon nanotubes (CNTs), fullerene (C60), graphene (Gr), and graphene oxide (GrO) on the marine microalgae Porphyridium purpureum. The microalgae cells were exposed to the CNMs for 96 h and measured by flow cytometry. Based on the obtained results, we determined no observed effect level (NOEL), and calculated EC10 and EC50 concentrations for growth rate inhibition, esterase activity, membrane potential, and reactive oxygen species (ROS) generation changes for each tested CNM. According to the sensitivity (growth rate inhibition) of P. purpureum, the used CNMs can be listed in the following order (EC50 in mg/L, 96 h): CNTs (2.08) > GrO (23.37) > Gr (94.88) > C60 (>131.0). The toxicity of CNTs was significantly higher than the toxic effect of the other used CNMs, and only this sample caused an increase in ROS generation in microalgae cells. This effect was apparently caused by the high affinity between particles and microalgae associated with the presence of exopolysaccharide coverage on P. purpureum cells.

15.
Int J Mol Sci ; 24(12)2023 Jun 12.
Artigo em Inglês | MEDLINE | ID: mdl-37373170

RESUMO

This work is related to the environmental toxicology risk assessment and evaluation of the possible transformation of carbon-based nanomaterials (CNMs) after contact with marine microalgae. The materials used in the study represent common and widely applied multi-walled carbon nanotubes (CNTs), fullerene (C60), graphene (Gr), and graphene oxide (GrO). The toxicity was evaluated as growth rate inhibition, esterase activity, membrane potential, and reactive oxygen species generation changes. The measurement was performed with flow cytometry after 3, 24, 96 h, and 7 days. The biotransformation of nanomaterials was evaluated after 7 days of microalgae cultivation with CNMs by FTIR and Raman spectroscopy. The calculated toxic level (EC50 in mg/L, 96 h) of used CNMs reduced in the following order: CNTs (18.98) > GrO (76.77) > Gr (159.40) > C60 (414.0). Oxidative stress and membrane depolarization were the main toxic action of CNTs and GrO. At the same time, Gr and C60 decreased the toxic action with time and had no negative impact on microalgae after 7 days of exposure even at the concentration of 125 mg/L. Moreover, C60 and Gr after 7 days of contact with microalgae cells obtained structural deformations.


Assuntos
Fulerenos , Microalgas , Nanoestruturas , Nanotubos de Carbono , Nanotubos de Carbono/toxicidade , Fulerenos/toxicidade , Nanoestruturas/toxicidade , Biotransformação
16.
Curr Drug Deliv ; 2023 Apr 25.
Artigo em Inglês | MEDLINE | ID: mdl-37170995

RESUMO

BACKGROUND: Melanoma is a malignant skin cancer type with a high lethality rate due to active metastasis. Among the risk factors for its development is exposure to ultraviolet radiation (UV) and phenotypical characteristics such as clear skin and eyes. Given the difficulties of the conventional therapy, the high cost of the treatment and the low bioavailability of drugs, it is important to develop new therapeutic methods to circumvent this situation. Nanosystems such as micelles, liposomes and nanoparticles present advantages when compared to conventional treatments. OBJECTIVE: The objective of this paper is to carry out a literature review based on articles that dealt with the use of siRNA-loaded nanosystems for the treatment of melanoma, with trials carried out in vivo to assess tumor size. METHODS: The search was conducted in the Web of Science and PubMed databases considering the last 5 years, that is, the period between January 2017 to December 2021. The "SiRNA and Drug Delivery Systems and Melanoma" keywords were used in both databases, and the articles were analyzed using the inclusion and exclusion criteria established for this paper. RESULTS: The results obtained indicated that using siRNA transported via nanosystems was capable of silencing the BRAF tumor genes and of reducing tumor size and weight, not presenting in vitro and/or in vivo toxicity. CONCLUSION: Such being the case, the development of these systems becomes a non-invasive and promising option for the treatment of melanoma.

17.
Colloids Surf B Biointerfaces ; 227: 113351, 2023 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-37244202

RESUMO

Arthritis is a chronic disease that affects, approximately, 1 % of the total global population. It is characterized by chronic inflammation, accompanied in most of the cases of motor disability and sever pain. The main therapies available have high risk of failure and advanced treatments are scarce and highly cost. In this scenario, search for effective, safe and low-cost treatments is quite desirable. Methyl gallate (MG) is a plant-derived phenolic compound described to present remarkable anti-inflammatory effect in experimental models of arthritis. Thus, in this study we formulated nanomicelles of MG using Pluronic (F-127) as matrix and evaluated in vivo the pharmacokinetic, biodistribution and its effect in the mice model of zymosan-induced arthritis. The nanomicelles were formed with a size 126 nm. The biodistribution showed a ubiquitous tissue deposition with a renal excretion. The pharmacokinetics showed elimination half-life of 1.72 h and a clearance of 0.006 L/h. The oral pretreatment with nanomicelles containing MG (3.5 or 7 mg/kg) demonstrated a reduction in total leukocytes, neutrophils, and mononuclear cells from the inflammation site. The data supports the use of methyl gallate nanomicelles as an alternative drug for arthritis. DATA AVAILABILITY: All the data of this study are transparent.


Assuntos
Artrite Experimental , Pessoas com Deficiência , Transtornos Motores , Camundongos , Animais , Humanos , Neutrófilos , Zimosan/efeitos adversos , Artrite Experimental/induzido quimicamente , Artrite Experimental/tratamento farmacológico , Distribuição Tecidual , Inflamação/induzido quimicamente , Inflamação/tratamento farmacológico
18.
Appl Radiat Isot ; 198: 110856, 2023 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-37245319

RESUMO

The development of new drugs that can specifically screen tumors is a global need. When it comes to lung cancer, which is the second main cause of cancer-related deaths, early detection of lung tumors using appropriate imaging is very important. In this study, gemcitabine hydrochloride (GCH) was radiolabeled with [99mTc]Tc under different conditions (changing reducing agent, antioxidant agent, incubation time, pH, [99mTc]Tc activity) and radiolabeling activity (quality control) using Radio Thin Layer Chromatography and paper electrophoresis. The results showed that the most stable complex ([99mTc]Tc-GCH) was prepared using 0.015 mg of stannous chloride as a reducing agent, 0.01 mg of ascorbic acid as an antioxidant and 37 MBq activity at pH 7.4 after 15 min of incubation time. The complex remained stable for 6 h. Cell incorporation studies showed a six-fold higher uptake of [99mTc]Tc-GCH in cancer (A-549) cells (38.42 ± 1.53) than healthy (L-929) cells (6.11 ± 0.17) have shown that it can. In addition, the different behaviors of R/H-[99mTc]Tc confirmed the specificity of this newly developed radiopharmaceutical. Although these studies are preliminary, it has been concluded that [99mTc]Tc-GCH may be a candidate drug for use in nuclear medicine, particularly in the diagnosis of lung cancer.


Assuntos
Neoplasias Pulmonares , Tecnécio , Humanos , Tecnécio/química , Gencitabina , Antioxidantes , Substâncias Redutoras , Compostos Radiofarmacêuticos/química , Neoplasias Pulmonares/diagnóstico por imagem , Controle de Qualidade
19.
ACS Appl Mater Interfaces ; 15(26): 31320-31329, 2023 Jul 05.
Artigo em Inglês | MEDLINE | ID: mdl-37246942

RESUMO

Natural and renewable resources from plants or animals are an important source of biomaterials due to their biocompatibility and high availability. Lignin is a biopolymer present in the biomass of plants, where it is intertwined and cross-linked with other polymers and macromolecules in the cell walls, generating a lignocellulosic material with potential applications. We have prepared lignocellulosic-based nanoparticles with an average size of 156 nm that exhibit a high photoluminescence signal when excited at 500 nm with emission in the near-infrared (NIR) region at 800 nm. The advantage of these lignocellulosic-based nanoparticles is their natural luminescent properties and their origin from rose biomass waste, which eliminates the need for encapsulation or functionalization of imaging agents. Moreover, the in vitro cell growth inhibition (IC50) of lignocellulosic-based nanoparticles is about 3 mg/mL, and no in vivo toxicity was registered up to 57 mg/kg, which suggests that they are suitable for bioimaging applications. In addition, these nanoparticles can circulate in the blood and are excreted in urine. The combined high luminescence signal in NIR, small size, low in vitro toxicity, low in vivo toxicity, and blood circulation support the potential of lignin-based nanoparticles as a novel bioimaging agent.


Assuntos
Lignina , Nanopartículas , Animais , Nanopartículas/toxicidade , Luminescência , Espectroscopia de Luz Próxima ao Infravermelho
20.
Curr Radiopharm ; 16(4): 337-339, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37226787

RESUMO

Nanotechnology has changed the world, with a great impact on industry and medicine. In this commentary, we discuss the importance of radiolabeled nanomaterials for the construction of theranostic, imaging and therapeutic agents in order to pave the future of medicine.


Assuntos
Nanoestruturas , Compostos Radiofarmacêuticos , Compostos Radiofarmacêuticos/uso terapêutico , Nanoestruturas/uso terapêutico , Nanotecnologia , Diagnóstico por Imagem , Nanomedicina Teranóstica
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