RESUMO
AIM: To elucidate the interactions, uptake mechanisms and cytotoxicity profile of glucose-functionalized gold nanoparticles (2GF-GNPs), for expanding and advancing the recently proposed technology of metabolic-based cancer detection to a variety of cancer diseases. METHODS: Several cell types with different metabolic features were used to assess the involvement of GLUT-1 and different endocytosis pathways in 2GF-GNP uptake, and the cytotoxicity profile of 2GF-GNPs. RESULTS: Cellular uptake of 2GF-GNP strongly correlated with GLUT-1 surface expression, and occurred mainly through clathrin-mediated endocytosis. 2GF-GNPs showed no toxic effect on cell cycle and proliferation. CONCLUSION: These findings promote development of metabolic-based cancer detection technologies, and suggest that 2GF-GNPs may enable specific cancer detection in a wide range of tumors characterized by high GLUT-1 expression.
Assuntos
Meios de Contraste/administração & dosagem , Transportador de Glucose Tipo 1/genética , Nanopartículas Metálicas/administração & dosagem , Neoplasias/diagnóstico por imagem , Células A549 , Ciclo Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Meios de Contraste/química , Citocalasina B/farmacologia , Endocitose/efeitos dos fármacos , Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos , Glucose/química , Glucose/metabolismo , Transportador de Glucose Tipo 1/antagonistas & inibidores , Ouro/química , Ouro/farmacologia , Humanos , Nanopartículas Metálicas/química , Neoplasias/genética , Neoplasias/patologia , Tomografia Computadorizada por Raios XRESUMO
Pain is one of the most common patient complaints encountered by health professionals and remains the number one cause of absenteeism and disability. In the current study, analgesic-eluting bioresorbable porous structures prepared using the freeze-drying of inverted emulsions technique were developed and studied. These drug-eluting structures can be used for coating fibers or implants, or for creating standalone films. They are ideal for forming biomedically important structures that can be used for various applications, such as wound dressings that provide controlled release of analgesics to the wound site in addition to their wound dressing role. Our investigation focused on the effects of the inverted emulsion's parameters on the shell microstructure and on the resulting drug-release profile of ibuprofen and bupivacaine. The release profiles of ibuprofen formulations exhibited a diffusion-controlled pattern, ranging from several days to 21 days, whereas bupivacaine formulations exhibited an initial burst release followed by a three-phase release pattern over a period of several weeks. Higher organic to aqueous phase ratios and higher polymer contents reduced the burst release of both drugs and prolonged their release due to lower porosity. Overall, the drug-eluting porous structures loaded with either ibuprofen or bupivacaine demonstrated a promising potential for use in various applications that require pain relief.