Response of Fibroblasts MRC-5 to Flufenamic Acid-Grafted MCM-41 Nanoparticles.

Recently, flufenamic acid (FFA) was discovered among fenamates as a free radical scavenger and gap junction blocker; however, its effects have only been studied in cancer cells. Normal cells in the surroundings of a tumor also respond to radiation, although they are not hit by it directly. This phenomenon is known as the bystander effect, where response molecules pass from tumor cells to normal ones, through communication channels called gap junctions. The use of the enhanced permeability and retention effect, through which drug-loaded nanoparticles smaller than 200 nm may accumulate around a tumor, can prevent the local side effect upon controlled release of the drug. The present work, aimed at functionalizing MCM-41 (Mobil Composition of Matter No. 41) silica nanoparticles with FFA and determining its biocompatibility with human fibroblasts MRC-5 (Medical Research Council cell strain 5). MCM-41, was synthesized and characterized structurally and chemically, with multiple techniques. The biocompatibility assay was performed by Live/Dead technique, with calcein and propidium-iodide. MRC-5 cells were treated with FFA-grafted MCM-41 for 48 h, and 98% of cells remained viable, without signs of necrosis or morphological changes. The results show the feasibility of MCM-41 functionalization with FFA, and its potential protection of normal cells, in comparison to the role of FFA in cancerous ones.

Synthesis, characterization, and biodistribution studies of (99m)Tc-labeled SBA-16 mesoporous silica nanoparticles.

Along with anti-cancer drug delivery researches, many efforts have been done to develop new tracers for diagnostic applications. Based on advances in molecular imaging, nanoparticles can be used to visualize, characterize and measure biological process at molecular and cellular level. Therefore, the purpose of this study was to synthesize, characterize and radiolabeled mesoporous silica nanoparticles (MSNs) for in vivo applications. The nanoparticles were synthesized, functionalized with 3-aminopropyltriethoxysilane (APTES) and then, anchored with diethylenetriaminepentaacetic acid (DTPA). Particles were physicochemical characterized by elemental analysis (CHN), thermogravimetric analysis (TGA), Fourier transform infrared spectroscopy (FTIR), and zeta potential, and were morphologically characterized by scanning electron microscopy (SEM), low-angle X-ray diffraction (XRD) and transmission electron microscopy (TEM) techniques. Results indicate that functionalization process was successfully achieved. Next, functionalized silica nanoparticles were radiolabeled with technetium-99m showing high radiochemical yields and high radiolabeled stability. These findings allow the use of the particles for in vivo applications. Biodistribution and scintigraphic images were carried out in healthy mice in order to determine the fate of the particles. Results from in vivo experiments showed high uptake by liver, as expected due to phagocytosis. However, particles also showed a significant uptake in the lungs, indicated by high lung-to-non-target tissue ratio. In summary, taking into account the great potential of these silica mesoporous structures to carry molecules this platform could be a good strategy for theranostic purposes.

Ordered mesoporous silica carrier system applied in nanobiothecnology

Ordered mesoporous materials like SBA15 possess a network of channels and pores of well-defined size in the nanoscale range (2-50 nm). This particular pore architecture makes them suitable candidates for hosting and delivery under appropriate conditions of a variety of molecules of pharmaceutical interest, including radiopharmaceuticals. The characteristics of SBA-15 prepared in different temperatures and the behavior of this system regarding microencapsulation of a model drug were investigated. The calcined samples were formed in 0.2 g disks and were soaked in a solution of atenolol used as a model drug. The modification of the aging temperature provoked changes in the structure of the pores, indicating the presence of microporosity and connections between mesopores. Aging the materials at a higher temperature resulted in no microporosity and this fact influenced the control of the release of the model drug.

Recentes estudos conduziram à descoberta da sílica mesoporosa com estrutura hexagonal, que apresenta elevada área superficial (700 a 1000 m²/g), tamanho de poros grande (5 a 9 nm) e espessura fina de parede do poro (3,5 a 5,3 nm), chamado SBA-15. Essas características fazem destes materiais matrizes adequadas para a incorporação e liberação controlada, sob condições apropriadas, de uma série de biomoléculas, principalmente radiofármacos. As características do SBA-15 preparado em diferentes temperaturas de envelhecimento e o comportamento desse sistema com relação ao micreoencapsulamento de uma droga modelo foi investigado. As amostras calcinadas foram conformadas em discos e imersas em uma solução saturada de atenolol, usado como droga modelo. A variação na temperatura de tratamento provoca algumas mudanças na estrutura dos poros, indicando a presença de microporosidade e interconectividade entre os mesoporos em condições específicas. Foi observado que materiais envelhecidos a elevadas temperaturas não apresentam microporosidades, e esse fato pode influenciar no controle da liberação da droga.