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A chemo-drug such as cisplatin is effective for cancer treatment but remains non-specific, is susceptible to drug resistance, and induces several side effects on organ systems. Zeolitic imidazolate framework-8, a type of MOF, has gained attention, including as a drug delivery method for targeted cancer therapeutics. In this study, ZIF-8/Silica nanocomposite was synthesized using a one-pot hydrothermal technique using the Stober technique. We studied the effect of phyto-synthesized GPt and chemo-drug cisplatin CPt on ZIF-8/Silica for targeted efficacy of cancer therapy. The texture, morphology, and chemical environment of Pt on ZIF-8/Silica were analyzed using different characterization techniques such as XRD, FT-IR, BET, diffuse reflectance spectroscopy, SEM-EDX, TEM, zeta potential, and TGA analysis. The isothermal behavior of CPt and GPt adsorption was investigated using isotherm models like Langmuir, Freundlich, and Temkin isotherm. The adsorption kinetics indicating the adsorption efficiency of GPt and CPt are influenced by the concentration of Pt complex and the adsorption sites of ZIF-8/Silica. A high entrapment efficiency and loading capacity of GPt (86% and 4.3%) and CPt (91% and 4.5%) were evident on ZIF-8/Silica. The nanocomposite showed a pH-sensitive Pt release using a dialysis membrane technique. For instance, a high release of GPt (93%) was observed under pH = 6.6 in 72 h, while the release reduced to 50% at pH 7.4 in 72 h. The anti-cancer activity of nanoformulations was studied in vitro using MCF7 (breast cancer cells) and HFF-1 (human foreskin fibroblast) cells. The findings demonstrated that GPt is as effective as CPt; the EC50 value for MCF7 cells treated with ZIF-8/Silica/Cp/PEG was 94.86 µg/mL, whereas for ZIF-8/Silica/GPt/PEG it was 60.19 µg/mL.
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Antineoplásicos , Nanocompostos , Neoplasias , Zeolitas , Humanos , Cisplatino/farmacologia , Platina , Zeolitas/química , Espectroscopia de Infravermelho com Transformada de Fourier , Dióxido de Silício/química , Antineoplásicos/farmacologia , Imidazóis/farmacologia , Imidazóis/química , Neoplasias/tratamento farmacológicoRESUMO
Root-to-shoot translocation of nanoparticles (NPs) is a matter of interest due to their possible unprecedented effects on biota. Properties of NPs, such as structure, surface charge or coating, and size, determine their uptake by cells. This study investigates the size effect of iron oxide (Fe3O4) NPs on plant uptake, translocation, and physiology. For this purpose, Fe3O4 NPs having about 10 and 100 nm in average sizes (namely NP10 and NP100) were hydroponically subjected to barley (Hordeum vulgare L.) in different doses (50, 100, and 200 mg/L) at germination (5 days) and seedling (3 weeks) stages. Results revealed that particle size does not significantly influence the seedlings' growth but improves germination. The iron content in root and leaf tissues gradually increased with increasing NP10 and NP100 concentrations, revealing their root-to-shoot translocation. This result was confirmed by vibrating sample magnetometry analysis, where the magnetic signals increased with increasing NP doses. The translocation of NPs enhanced chlorophyll and carotenoid contents, suggesting their contribution to plant pigmentation. On the other hand, catalase activity and H2O2 production were higher in NP10-treated roots compared to NP100-treated ones. Besides, confocal microscopy revealed that NP10 leads to cell membrane damages. These findings showed that Fe3O4 NPs were efficiently taken up by the roots and transported to the leaves regardless of the size factor. However, small-sized Fe3O4 NPs may be more reactive due to their size properties and may cause cell stress and membrane damage. This study may help us better understand the size effect of NPs in nanoparticle-plant interaction.
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Hordeum , Hordeum/metabolismo , Tamanho da Partícula , Bioacumulação , Peróxido de Hidrogênio/metabolismo , Plântula , Nanopartículas Magnéticas de Óxido de FerroRESUMO
Objective: To enhance the brain bioavailability of S-allyl-l-cysteine (SC) by developing novel S-allyl-l-cysteine chitosan nanoparticles (SC CS NPs) and examining the quantity of SC by developing a novel method of ultra-high performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) in ischemic rat brain treatment. Methods: The ionotropic gelation method was used to develop S-allyl cysteine-loaded CS NPs. The 4-factor, 5-level central composite design was optimized to determine the effect of independent variables, i.e., particle size, polydispersity index (PDI), zeta potential, EE, and loading capacity, together with their characterization, followed by drug release and intranasal permeation to enhance the brain bioavailability and examination of their neurobehavioral and biochemical parameters with their histopathological examination. Results: SC CS NPs were optimized at the particle size of 93.21 ± 3.31 nm (PDI: 0.317 ± 0.003), zeta potential of 44.4 ± 2.93, and drug loading of 41.23 ± 1.97% with an entrapment efficiency of 82.61 ± 4.93% having sustain and controlled release (79.92 ± 3.86%) with great permeation (>80.0%) of SC. SC showed the retention time of 1.021 min and 162.50/73.05 m/z. SC showed good linearity in the range of 5.0-1300.0 ng mL-1, % inter-and-intraday accuracy of 96.00-99.06% and CV of 4.38-4.38%. We observed significant results, i.e., p < 0.001 for improved (AUC)0-24 and Cmax delivered via i.v. and i.n. dose. We also observed the highly significantly observations of SC CS NPs (i.n.) based on their treatment results for the biochemical, neurobehavioral, and histopathological examination in the developed ischemic MCAO brain rat model. Conclusion: The excellent significant role of mucoadhesive CS NPs of SC was proven based on the enhancement in the brain bioavailability of SC via i.n. delivery in rats and easy targeting of the brain for ischemic brain treatment followed by an improvement in neuroprotection based on a very small dose of SC.
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In nanotherapeutics, gaining insight about the drug interaction with the pore architecture and surface functional groups of nanocarriers is crucial to aid in the development of targeted drug delivery. Manganese ferrite impregnated graphene oxide (MnFe2O4/GO) with a two-dimensional sheet and spherical silica with a three-dimensional interconnected porous structure (MnFe2O4/silica) were evaluated for cisplatin release and cytotoxic effects. Characterization studies revealed the presence of Mn2+ species with a variable spinel cubic phase and superparamagnetic effect. We used first principles calculations to study the physisorption of cisplatin on monodispersed silica and on single- and multi-layered GO. The binding energy of cisplatin on silica and single-layer GO was ~1.5 eV, while it was about double that value for the multilayer GO structure. Moreover, we treated MCF-7 (breast cancer cells) and HFF-1 (human foreskin fibroblast) with our nanocomposites and used the cell viability assay MTT. Both nanocomposites significantly reduced the cell viability. Pt4+ species of cisplatin on the spinel ferrite/silica nanocomposite had a better effect on the cytotoxic capability when compared to GO. The EC50 for MnFe2O4/silica/cisplatin and MnFe2O4/GO/cisplatin on MCF-7 was: 48.43 µg/mL and 85.36 µg/mL, respectively. The EC50 for the same conditions on HFF was: 102.92 µg/mL and 102.21 µg/mL, respectively. In addition, immunofluorescence images using c-caspase 3/7, and TEM analysis indicated that treating cells with these nanocomposites resulted in apoptosis as the major mechanism of cell death.
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Zinc oxide nanoparticles (ZnO NPs) are a promising platform for their use in biomedical research, especially given their anticancer and antimicrobial activities. This work presents the synthesis of ZnO NPs doped with different amounts of rare-earth ions of ytterbium (Yb) and cerium (Ce) and the assessment of their anticancer and antimicrobial activities. The structural investigations indicated a hexagonal wurtzite structure for all prepared NPs. The particle size was reduced by raising the amount of Ce and Yb in ZnO. The anticancer capabilities of the samples were examined by the cell viability MTT assay. Post 48-h treatment showed a reduction in the cancer cell viability, which was x = 0.00 (68%), x = 0.01 (58.70%), x = 0.03 (80.94%) and x = 0.05 (64.91%), respectively. We found that samples doped with x = 0.01 and x = 0.05 of Yb and Ce showed a better inhibitory effect on HCT-116 cancer cells than unadded ZnO (x = 0.00). The IC50 for HCT-116 cells of Ce and Yb co-doped ZnO nanoparticles was calculated and the IC50 values were x = 0.01 (3.50 µg/mL), x = 0.05 (8.25 µg/mL), x = 0.00 (11.75 µg/mL), and x = 0.03 (21.50 µg/mL). The treatment-doped ZnO NPs caused apoptotic cell death in the HCT-116 cells. The nanoparticles showed inhibitory action on both C. albicans and E. coli. It can be concluded that doping ZnO NPs with Yb and Ce improves their apoptotic effects on cancer and microbial cells.
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Hollow silica spheres (HSS) exhibited high-specific surface area, low toxicity, low density, and good biocompatibility. The effectivity of HSS material can be improved further by loading nanoparticles for smart biological applications. In this work, magnetic nanoparticle (iron oxide; Fe3O4)-loaded pure HSS (c-HSS-Fe) were synthesized successfully using a template-free chemical route and investigated for their anticancer cell proliferation capabilities against cancerous cell lines: human colorectal carcinoma cells (HCT-116). The structure, morphology, chemical bonding, and thermal stability of the prepared HSS derivatives were studied using spectroscopic and microscopic techniques. Our analyses confirmed the successful preparation of Fe3O4 loaded HSS material (sphere diameter â¼515 nm). The elemental analysis revealed the existence of Fe along with Si and O in the Fe3O4 loaded HSS material, thus reaffirming the production of the c-HSS-Fe product. The effects of silica spheres on HCT-116 cells were examined microscopically and by MTT assays. It was observed that the c-HSS-Fe demonstrated dose-dependent behavior and significantly reduced the cancer cell proliferation at higher doses. Our results showed that c-HSS-Fe was more effective and profound in reducing the cancer cells' activities as compared to unloaded HSS material where the cancer cells have undergone nuclear disintegration and fragmentation. It is concluded that c-HSS-Fe is a powerful bio-active material against cancerous cells.
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BACKGROUND: The constant rise of microbial biofilm formation and drug resistance to existing antimicrobial drugs poses a significant threat to community health around the world because it reduces the efficacy and efficiency of treatments, increasing morbidity, mortality, and health-care expenditures. As a result, there is an urgent need to develop novel antimicrobial agents that inhibit microbial biofilm formation. METHODS: The [Ni0.4Cu0.2Zn0.4](Fe2-xDyx)O4(x≤0.04) (Ni-Cu-Zn) nano spinel ferrites (NSFs) have been synthesized by the sol-gel auto-combustion process and were characterized by X-ray diffraction (XRD), scanning electron microscopy (SEM), energy dispersive x-ray (EDX) and transmission electron microscopy (TEM). The antimicrobial, antibiofilm and antiproliferative activities of Ni-Cu-Zn NSFs were also examined. RESULTS: The XRD pattern confirms the secondary phase DyFeO3 and Fe2O3 for substituted Dy3 + samples, and the crystallite size ranged from 10 to 19 nm. TEM analysis of NSFs revealed that the particles were cube-shaped and 15nm in size. NSFs exhibited significant antimicrobial, antibiofilm and antiproliferative activity. At concentration of 1 mg/mL, it was found that the NSFs (ie, x=0.0, x=0.01, x=0.02, x=0.03 and x=0.04) inhibit biofilm formation by 27.6, 26.2, 58.5, 33.3 and 25% for methicillin-resistant Staphylococcus aureus (MRSA) and 47.5, 43.5, 48.6, 58.3 and 26.6% for Candida albicans, respectively. SEM images demonstrate that treating MRSA and C. albicans biofilms with NSFs significantly reduces cell adhesion, colonization and destruction of biofilm architecture and extracellular polymeric substances matrices. Additionally, SEM and TEM examination revealed that NSFs extensively damaged the cell walls and membranes of MRSA and C. albicans. Huge ultrastructural alteration such as deformation, disintegration and separation of cell wall and membrane from the cells was observed, indicating significant loss of membrane integrity, which eventually led to cell death. Furthermore, it was observed that NSF inhibited the cancer cell growth and proliferation of HCT-116 in a dose-dependent manner. CONCLUSION: The current study demonstrated that the synthesized Ni-Cu-Zn NSFs could be used to develop potential antimicrobial surface coatings agents for a varieties of biomedical-related materials and devices in order to prevent the biofilms formation and their colonization. Furthermore, the enhanced antiproliferative properties of manufactured SNFs suggest a wide range of biomedical applications.
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Anti-Infecciosos , Staphylococcus aureus Resistente à Meticilina , Antibacterianos/farmacologia , Antifúngicos/farmacologia , Biofilmes , Compostos Férricos , Testes de Sensibilidade Microbiana , ZincoRESUMO
Recently, titanium dioxide (TiO2) nanomaterials have gained increased attention because of their cost-effective, safe, stable, non-toxic, non-carcinogenic, photocatalytic, bactericidal, biomedical, industrial and waste-water treatment applications. The aim of the present work is the synthesis of electrospun TiO2 nanofibers (NFs) in the presence of different amounts of air-argon mixtures using sol-gel and electrospinning approaches. The physicochemical properties of the synthesized NFs were examined by scanning and transmission electron microscopies (SEM and TEM) coupled with energy-dispersive X-ray spectroscopy (EDX), ultraviolet-visible spectroscopy and thermogravimetric analyzer (TGA). The antibacterial and antibiofilm activity of synthesized NFs against Gram-negative Pseudomonas aeruginosa and Gram-positive methicillin-resistant Staphylococcusaureus (MRSA) was investigated by determining their minimum bacteriostatic and bactericidal values. The topological and morphological alteration caused by TiO2 NFs in bacterial cells was further analyzed by SEM. TiO2 NFs that were calcined in a 25% air-75% argon mixture showed maximum antibacterial and antibiofilm activities. The minimum inhibitory concentration (MIC)/minimum bactericidal concentration (MBC) value of TiO2 NFs against P. aeruginosa was 3 and 6 mg/mL and that for MRSA was 6 and 12 mg/mL, respectively. The MIC/MBC and SEM results show that TiO2 NFs were more active against Gram-negative P. aeruginosa cells than Gram-positive S. aureus. The inhibition of biofilm formation by TiO2 NFs was investigated quantitatively by tissue culture plate method using crystal violet assay and it was found that TiO2 NFs inhibited biofilm formation by MRSA and P. aeruginosa in a dose-dependent manner. TiO2 NFs calcined in a 25% air-75% argon mixture exhibited maximum biofilm formation inhibition of 75.2% for MRSA and 72.3% for P. aeruginosa at 2 mg/mL, respectively. The antibacterial and antibiofilm results suggest that TiO2 NFs can be used to coat various inanimate objects, in food packaging and in waste-water treatment and purification to prevent bacterial growth and biofilm formation.
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The present study reports the preparation of cadmium sulfide (CdS) loaded zinc oxide (ZnO) nanostructured semiconductor material and its anti-bioactivity studies against cancerous and fungus cells. For composite preparation, two different mass ratios of CdS (10 and 20%) were loaded on ZnO (10%CdS/ZnO, 20%CdS/ZnO) using a 532 nm pulsed laser ablation in water media. The structural and morphological analyses confirmed the successful loading of nanoscaled CdS on the surface of ZnO particles, ZnO particles were largely spherical with average size ~50 nm, while CdS about 12 nm in size. The elemental and electron diffraction analyses reveal that the prepared composite, CdS/ZnO contained both CdS and ZnO, thus reaffirming the production of CdS loaded ZnO. The microscopic examination and MTT assay showed the significant impact of ZnO, CdS, and CdS loaded ZnO on human colorectal carcinoma cells (HCT-116 cells). Our results show that the prepared ZnO had better anticancer activities than individual CdS, and CdS loaded ZnO against cancerous cells. For antifungal efficacy, as-prepared nanomaterials were investigated against Candida albicans by examining minimum inhibitory/fungicidal concentration (MIC/MFC) and morphogenesis. The lowest MIC (0.5 mg/mL), and MFC values (1 mg/mL) were found for 10 and 20%CdS/ZnO. Furthermore, the morphological analyses reveal the severe damage of the cell membrane upon exposure of Candida strains to nanomaterials. The present study suggests that ZnO, CdS, and CdS loaded ZnO nanostructured materials possess potential anti-cancer and anti-fungal activities.
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Compostos de Cádmio , Nanoestruturas , Óxido de Zinco , Humanos , Lasers , SulfetosRESUMO
In the present research work, copper oxide-titanium dioxide nanocomposites were synthesized for the first time using advanced pulsed laser ablation in liquid (PLAL) technique for disinfection of drug-resistant pathogenic waterborne biofilm-producing bacterial strains. For this, a series of copper oxide-titanium dioxide nanocomposites were synthesized by varying the composition of copper oxide (5%, 10%, and 20%) with titanium dioxide. The pure titanium dioxide and copper oxide-titanium dioxide nanocomposites were characterized by advanced instrumental techniques. XRD, TEM, FE-SEM, EDX, elemental mapping and XPS analysis results consistently revealed the successful formation of copper oxide-titanium dioxide nanocomposites using PLAL technique. The antibacterial and antibiofilm activities of pure titanium dioxide and copper oxide-titanium dioxide nanocomposites were investigated against biofilm-producing strains of Methicillin-resistant Staphylococcus aureus and Pseudomonas aeruginosa by various methods. Our results revealed that the PLAL synthesized copper oxide-titanium dioxide nanocomposites showed enhanced anti-biofilm and antibacterial activity compared to pure titanium dioxide in a dose-dependent manner against targeted pathogens. Furthermore, the effects of pure titanium dioxide and copper oxide-titanium dioxide nanocomposites on bacterial morphology, biofilm formation, aggregation and their colonization by targeted pathogens were also examined using scanning electron microscopy. Microscopic images clearly showed that the cell envelope of almost all the cells were rumples, rough, had irregularities and abnormal appearance with the major damage being characterized by the formation of "pits". Many depressions and indentations were also seen in their cell envelope and the original shape of Pseudomonas aeruginosa cells changed from normal rod to swollen, large and elongated which indicates the loss of membrane integrity and damage of cell wall and membrane. The findings suggested that PLAL synthesized copper oxide-titanium dioxide nanocomposites have good potential for removal of biofilm or killing of pathogenic bacteria in water distribution network and for wastewater treatment, hospital and environmental applications. In addition, cytotoxic activity of pure TiO2 and PLAL synthesized copper oxide-titanium dioxide nanocomposites against normal and healthy cells (HEK-293) and cancerous cells (HCT-116) were also evaluated by MTT assay. The MTT assay results showed no cytotoxic effects on HEK-293 cells, which suggest TiO2 and PLAL synthesized copper oxide-titanium dioxide nanocomposites are non-toxic to the normal cells.
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Antibacterianos/farmacologia , Biofilmes/efeitos dos fármacos , Cobre/química , Farmacorresistência Bacteriana/efeitos dos fármacos , Nanocompostos/química , Titânio/química , Antibacterianos/química , Sobrevivência Celular/efeitos dos fármacos , Células HCT116 , Células HEK293 , Humanos , Staphylococcus aureus Resistente à Meticilina/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Nanocompostos/toxicidade , Tamanho da Partícula , Pseudomonas aeruginosa/efeitos dos fármacos , Pseudomonas aeruginosa/fisiologiaRESUMO
Aim: To synthesize and examine the impact of free Eudragit® RS 100 nanoparticles (LN01), Quantum dots curcumin-loaded Eudragit RS 100 nanoparticles (LN04), and un-encapsulated curcumin nanoparticles (LN06) on cancerous and bacterial cells. Materials & methods: The LN01, LN04, LN06 were synthesized and characterized by Fourier transform infrared, ζ potential, UV-Vis spectroscopy, transmission electron microscopy and scanning electron microscopy and their biological activities were evaluated. Results: LN04 profoundly inhibited the growth of colon (HCT-116) cancerous cells (10.64% cell viability) and breast cancer (MCF-7) cells (10.32% cell viability) with compared to LN01 and LN06. Normal cells (HEK-293) did not show any inhibition after treatments. In addition, LN04 show better inhibitory action on bacterial growth compared with LN01 and LN06. Conclusion: We suggest that LN04 selectively target cancerous and bacterial cells and therefore possess potential anticancer and antibacterial capabilities.
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Bactérias/efeitos dos fármacos , Neoplasias da Mama , Neoplasias do Colo , Curcumina , Nanopartículas , Pontos Quânticos , Neoplasias da Mama/tratamento farmacológico , Neoplasias do Colo/tratamento farmacológico , Curcumina/farmacologia , Células HEK293 , Humanos , Células MCF-7 , Espectroscopia de Infravermelho com Transformada de FourierRESUMO
Nanomaterials (NMs) have emerged in the last decades and are used in many disciplines such as industry, material sciences, biomedicine, biotechnology, bioenergy, and agriculture. The size of the NMs is a critical factor that affects NMs' integration and transfer into the biological systems. Therefore, this study aims at investigating the effect of NMs-size on i) plant growth and physiology, and ii) NMs uptake and translocation in plant tissues. For these purposes, iron (III) oxide (Fe2O3) NMs with varied sizes, 8-10, 20-40, and 30-50â¯nm, have been applied to wheat plants in a hydroponic system. Results showed that Fe2O3 NMs enhanced root length, plant height, biomass, and chlorophyll content of wheat. Confocal microscopy analysis indicated that Fe2O3 NMs cause injury in root-tip cells without a visible toxic symptom. Vibrating sample magnetometer (VSM), and inductively coupled plasma-mass spectroscopy (ICP-MS) analyses of leaf tissues revealed that all tested NMs were up taken by wheat plant and translocated to the leaves. Iron content was found to be dramatically increased in NMs-treated plant tissues, which possibly contributed to the growth enhancement. Experiments confirmed that Fe2O3 NMs with 20-40â¯nm size is much more efficient in plant growth compared to those with 8-10 and 30-50â¯nm size. Overall, Fe2O3 NMs with 20-40â¯nm in size could be proposed as a nano-fertilizer for agricultural applications. On the other hand, the translocation of NMs in the wheat plant requires further investigation of their effects on the end users.
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Fertilizantes , Nanopartículas/toxicidade , Desenvolvimento Vegetal/efeitos dos fármacos , Triticum/efeitos dos fármacos , Transporte Biológico , Biomassa , Clorofila/metabolismo , Compostos Férricos/química , Compostos Férricos/farmacologia , Hidroponia , Nanopartículas/química , Folhas de Planta/efeitos dos fármacos , Folhas de Planta/metabolismo , Raízes de Plantas/efeitos dos fármacos , Raízes de Plantas/metabolismo , Triticum/crescimento & desenvolvimento , Triticum/metabolismoRESUMO
Manganese metallic nanoparticles are attractive materials for various biological and medical applications. In the present study, we synthesized unique Mn0.5Zn0.5SmxEuxFe1.8-2xO4 (0.01 ≤ x ≤ 0.05) nanoparticles (NPs) by using the hydrothermal approach. The structure and surface morphology of the products were determined by X-ray powder diffraction (XRD), transmission electron and scanning electron microcopies (TEM and SEM), along with energy dispersive X-ray spectroscopy (EDX). We evaluated the impact of Mn0.5Zn0.5SmxEuxFe1.8-2xO4 NPs on both human embryonic stem cells (HEK-293) (normal cells) and human colon carcinoma cells (HCT-116) (cancerous cells). We found that post-48 h of treatment of all products showed a significant decline in the cancer cell population as revealed by microscopically and the (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) tetrazolium (MTT) assay. The inhibitory concentration (IC50) values of the products ranged between 0.75 and 2.25 µg/mL. When tested on normal and healthy cells (HEK-293), we found that the treatment of products did not produce any effects on the normal cells, which suggests that all products selectively targeted the cancerous cells. The anti-bacterial properties of the samples were also evaluated by Minimum Inhibitory Concentration (MIC) and Minimum Bactericidal Concentration (MBC) assays, which showed that products also inhibited the bacterial growth.
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Multifunctional nanomaterials can be used for dual applications: drug delivery as well as in bioimaging. In current study, we investigated potential use of silica based supports; 3D cage type SiSBA-16 (S-16), monodispersed hydrophilic spherical silica (HYPS) and mesocellular foam (MSU-F) for cisplatin (Cp) delivery. To obtain magnetic resonance characteristics, 10 wt% iron oxide was loaded through enforced adsorption technique. For pH stimuli responsive release of Cp, 10 wt%SPIONs/S-16 was functionalized with 3-(Aminopropyl)triethoxysilane (A) and poly acrylic acid (PAA) termed as 10 wt%SPIONs/S-16-A-Cp and 10 wt%SPIONs/S-16-APAA-Cp. By TEM analysis, the average diameter of the SPIONs was found to range between 10-60 nm. VSM analysis showed saturation magnetization over S-16, HYPS and MSU-F were in the following order: 10 wt%SPIONs/HYPS (4.08 emug-1) > 10 wt%SPIONs /S-16 (2.39 emug-1) > 10 wt%SPIONs/MSU-F (0.23 emug-1). Cp release study using dialysis membrane in PBS solution over 10 wt%SPIONs/S-16 nanoformulations showed highest cumulative release (65%) than 10 wt%SPIONs/MSU-F-A-Cp (63%), 10 wt%SPIONs/HYPS-A-Cp (58%), and Cp-F127/S-16 (53%), respectively. 10 wt%SPIONs/S-16-A-Cp and 10 wt%SPIONs/S-16-APAA-Cp were evaluated for in vitro target anticancer efficiency in human cancer cell lines (colon cancer (HCT 116), cervical cancer (HeLa)) and normal cells (Human embryonic kidney cells (HEK293) using MTT and DAPI staining. 10 wt%SPIONs/S-16-A-Cp treated Hela and HCT116 cancerous cell lines showed significant control of cell growth, apoptotic activity and less cytotoxic effect as compared to Cp and 10 wt%SPIONs/S-16. Target specific Cp release in the cells shows that 10 wt%SPIONs/S-16-A-Cp can be easily upgraded for magnetic resonance imaging capability.
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Cisplatino/administração & dosagem , Neoplasias do Colo/tratamento farmacológico , Portadores de Fármacos , Nanopartículas de Magnetita/química , Dióxido de Silício/química , Neoplasias do Colo do Útero/tratamento farmacológico , Adsorção , Antineoplásicos/administração & dosagem , Apoptose , Linhagem Celular Tumoral , Feminino , Células HCT116 , Células HEK293 , Células HeLa , Humanos , Rim/efeitos dos fármacos , Imageamento por Ressonância Magnética , Microscopia Eletrônica de Transmissão , Difração de Raios XRESUMO
The engineering of multifunctional therapeutics in an integrated single platform is demonstrated using three-dimensional SBA-16 (S-16). 10 wt% iron oxide nanoparticles (Fe) were loaded into the cage type of cubic pores through enforced adsorption technique. Fe/S-16 is then functionalized with amine-based silane (A), polyacrylic acid (P) and cisplatin (Cp). The physicochemical textural analysis showed the formation of nano metal oxide distributions at pore walls of S-16 with magnetization of 2.39 emu/g. S-16 based nanoformulations showed high percentage of Cp adsorption (90%) and percentage cumulative release (60%). in vitro study of Fe/S-16-A-Cp showed high toxicity against breast cancer cell line MCF-7 and normal cell line Human foreskin fibroblast (HFF-1) compared to Fe/S-16 indicating cisplatin profusion inside the cells than free cisplatin. While skin fibroblast seems to be resistant to Fe/S-16-AP-Cp with very high LC50 in compare to MCF-7. This indicates the unrelease of cisplatin in skin fibroblast after Fe/S-16-AP-Cp treatment due to effective encapsulation inside the cubic pores and core blockage due to pH-sensitive polyacrylic acid. Also, these treatments resulted in morphological changes in the cells such as DNA condensation and nuclear fragmentation.
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Antineoplásicos/química , Antineoplásicos/farmacologia , Neoplasias da Mama/patologia , Cisplatino/química , Cisplatino/farmacologia , Imãs/química , Dióxido de Silício/química , Resinas Acrílicas/química , Aminas/química , Núcleo Celular/efeitos dos fármacos , Núcleo Celular/patologia , Relação Dose-Resposta a Droga , Portadores de Fármacos/química , Humanos , Células MCF-7 , Nanopartículas/químicaRESUMO
The aim of this study was to synthesize a series of nickel(II)phthalocyanines (NiPcs) bearing four 4(3H)-quinazolinone ring system units, (qz)4NiPcs 4a-d. The electronic factors in the 4(3H)-quinazolinone moiety that attached to the NiPc skeleton had a magnificent effect on the antibacterial activity of the newly synthesized (qz)4NiPcs 4a-d against Escherichia coli. The minimum MICs and MBCs value were recorded for compounds 4a, 4b, 4c, and 4d, respectively. The results indicated that the studied (qz)4NiPcs 4a-d units possessed a broad spectrum of activity against Escherichia coli. Their antibacterial activities were found in the order of 4d > 4c > 4b > 4a against Escherichia coli, and the strongest antibacterial activity was achieved with compound 4d.
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Poly (methyl methacrylate) (PMMA) is basically biocompatible polyester with high resistance to chemical hydrolysis, and high drug permeability and the most important characteristics of PMMA is that it does not produce any toxicity. There is not much information about PMMA action on the colon cancer cells. In the present study, we have synthesized PMMA nanoparticles. The distribution pattern of PMMA particles was analysed by Zeta sizer and the size of the particles was calculated by using quasi elastic light scattering (QELS). The surface structure and the morphology of PMMA were characterized by transmission electron microscope (TEM) and scanning electron microscope (SEM), respectively. We have also analysed their effects on cancerous cells (human colorectal carcinoma cells, HCT-116) and normal, healthy cells (human embryonic kidney cells, HEK-293) by using morphometric, MTT, DAPI and wound healing methods. We report that PMMA particles inhibited the cancer cell viability in a dose-dependent manner. The lower dose (1.0 µg/ml) showed a moderate decrease in cancer cell viability, whereas higher dosages (2.5 µg/ml, 5.0 µg/mL and 7.5 µg/mL) showed steadily decrease in the cancer cell viability. We also report that PMMA is highly selective to cancerous cells (HCT-116), as we did not find any action on the normal healthy cells (HEK-293). In conclusion, our results suggest PMMA particles are potential biomaterials to be used in the treatment of colon cancer.
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Neoplasias do Colo/patologia , Polimetil Metacrilato/química , Polimetil Metacrilato/farmacologia , Núcleo Celular/efeitos dos fármacos , Núcleo Celular/patologia , Proliferação de Células/efeitos dos fármacos , Sistemas de Liberação de Medicamentos , Células HCT116 , Células HEK293 , Humanos , Nanopartículas/química , Tamanho da Partícula , Polimetil Metacrilato/metabolismo , Cicatrização/efeitos dos fármacosRESUMO
The fabrication of bioactive polymer nanocomposite coatings with enhanced biocompatibility and surface protection has been a topic of abundant concern in orthopaedic implant applications. Herein, we electrochemically prepared a novel poly (3,4-ethylenedioxythiophene) (PEDOT) based nanocomposite coatings with different contents of fluoro hydroxyapatite (FHA) nanoparticles on a newly developed Ti-Nb-Zr (TNZ) alloy; an appropriate approach to advance the surface features of TNZ implants. FTIR, XRD, and Raman analyses of the coating confirm the successful preparation of PEDOT/FHA nanocomposite, and XPS validate the chemical interaction between FHA and PEDOT matrix. SEM and TEM examination show the uniform distribution of spherical FHA nanoparticles inside the PEDOT matrix. Hardness and contact angle measurement results showed improving in the hardness and surface wettability of the coated samples respectively. Electrochemical corrosion tests specified that the PEDOT/FHA coatings exhibit higher corrosion protection than the pure PEDOT coatings. The fabricated nanocomposite coating supports the cell adsorption and proliferation of MG-63 cells. Moreover, antibacterial studies against Gram positive and negative bacteria reveal the enhanced antibacterial performance of the coated TNZ substrates. Our results show the potential applications of PEDOT/FHA nanocomposite as a most viable coating for the orthopaedic implants.
Assuntos
Ligas/farmacologia , Infecções Bacterianas/patologia , Compostos Bicíclicos Heterocíclicos com Pontes/farmacologia , Materiais Revestidos Biocompatíveis/farmacologia , Nanocompostos/química , Nióbio/farmacologia , Polímeros/farmacologia , Próteses e Implantes , Antibacterianos/farmacologia , Linhagem Celular Tumoral , Corrosão , Espectroscopia Dielétrica , Durapatita/química , Durapatita/farmacologia , Técnicas Eletroquímicas , Dureza , Humanos , Testes de Sensibilidade Microbiana , Nanocompostos/ultraestrutura , Espectroscopia Fotoeletrônica , Análise Espectral Raman , Molhabilidade , Difração de Raios XRESUMO
The penetration and transportation of nanoparticles (NPs) inside the cancer cells is critical to study. In this article, cancer cells (HCT-116) were treated with functionalized magnetic NPs for the period of 48 hr and studied their ultrastructure by transmission electron microscopy (TEM). The NPs-treated cells were prepared by chemical fixation and sliced into electron-transparent arbitrary sections (200 × 200 µm2 ) by ultramicrotome. Major events of NPs-cell interaction, such as penetration of NPs, encapsulation of NPs into the intracellular compartments, transportation of NPs, and NPs exit, were examined by TEM to understand the mechanism of cell death. The NPs showed the uniform spherical shape with broad size distribution (100-400 nm), while cells displayed irregular morphology with average diameter ~5 µm. Our results showed the successful penetration of NPs deep into the cell, encapsulation, transportation, and exocytosis. Furthermore, we tested the different concentrations (0, 1.5, 12.5, and 50 µg/ml) of NPs on cancer cells and evaluated the cell viability. Laser confocal microscopy and colorimetric analysis together demonstrated that the cell viability is a dose-dependent phenomenon, where 50 µg/ml specimen showed the highest killing of cancer cells compared to other dosages.
Assuntos
Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Nanopartículas de Magnetita , Colorimetria , Células HCT116 , Humanos , Microscopia Eletrônica de Transmissão , MicrotomiaRESUMO
Nanoformulation involving biocompatible MOFs and magnetic nanocarriers is an emerging multifunctional platform for drug delivery and tumor imaging in targeted cancer therapeutics. In this study, a nanocomposite has been developed comprising Fe/SBA-16 and ZIF-8 (Fe/S-16/ZIF-8) through ultrasonication. The drug delivery of cisplatin was studied using an automated diffusion cell system equipped with a flow type Franz cell. The anticancer activity of Fe/S-16/ZIF-8 was studied in vitro in MCF-7, HeLa cells and Human Foreskin Fibroblast (HFF-1) cells. XRD and d-spacing measurements of Fe/S-16/ZIF-8 using TEM revealed the presence of cubic-structured Fe3O4, γ-Fe2O4 (magnetite), and α-FeOOH (goethite) over an SBA-16/ZIF-8 nanocomposite. The composite showed a surface area of 365 m2 g-1, a pore size of 8.3 nm and a pore volume of 0.33 cm3 g-1. VSM analysis of Fe/S-16/ZIF-8 showed that it possessed paramagnetic behavior with a saturated magnetization value of 2.39 emu g-1. The Fe2+/Fe3+ coordination environment was characterized using diffuse reflectance spectroscopy. The cisplatin drug delivery study clearly showed the synergistic effects present in Fe/S-16/ZIF-8 with over 75% of cisplatin release as compared to that of Fe/S-16 and ZIF-8, which showed 56% and 7.5%, respectively. The morphology analysis of CP/Fe/SBA-16/ZIF-8 using TEM showed an effective transit of nanoparticles into MCF-7 cells. The lethal concentration (LC50) of Fe/SBA-16/ZIF-8 for MCF-7 and HeLa cells is 0.119 mg mL-1 and 0.028 mg mL-1 at 24 h, respectively. For HFF-1 cells, the LC50 is 0.016 mg mL-1. The antibiofilm activity of Fe/SBA-16/ZIF-8 was investigated against biofilm-forming strains of drug resistant P. aeruginosa and MRSA by a microtiter tissue culture plate assay. Overall, nanosized ZIF-8 with a bioactive alkaloid imidazole inside the 3D cage type of SBA-16 pores is found to exhibit both anticancer and antibacterial properties. A Fe/S-16/ZIF-8 composite could be effectively used as a drug and drug delivery system against cancer and promote antibacterial activity.