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International Journal of Peptide Research and Therapeutics - The significant role of proteases in the cancer progression exposed them as potential targets for drug discovery. Regulating protease...  相似文献   
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The objective of this study comprises of developing novel co-spray dried rifampicin phospholipid lipospheres (SDRPL) to investigate its influence on rifampicin solubility and oral bioavailability. Solid-state techniques were employed to characterize the liposphere formulation. SDRPL solubility was determined in distilled water. BACTEC 460TB System was employed to evaluate SDRPL antimycobacterial activity. The oral bioavailability of the lipospheres was evaluated in Sprague Dawley rats. Lipospheres exhibited amorphous, smooth spherical morphology with a significant increase (p?<?0.001) in solubility of SDRPL (2:1), 350.9?±?23 versus 105.1?±?12 μg/ml and SDRPL (1:1) 306.4?±?20 versus 105.1?±?12 μg/ml in comparison to rifampicin (RMP). SDRPL exhibited enhanced activity against Mycobacterium tuberculosis, H37Rv strain, with over twofolds less minimum inhibitory concentration (MIC) than the free drug. Lipospheres exhibited higher peak plasma concentration (109.92?±?25 versus 54.31?±?18 μg/ml), faster T max (two versus four hours), and enhanced area under the curve (AUC0–∞) (406.92?±?18 versus 147.72?±?15 μg h/L) in comparison to pure RMP. Thus, SDRPL represents a promising carrier system exhibiting enhanced antimycobacterial activity and oral bioavailability of rifampicin.  相似文献   
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Here, we report the facile preparation of tunable magnetic Ni-doped near-infrared (NIR) quantum dots (MNIR-QDs) as an efficient probe for targeting, imaging, and cellular sorting applications. We synthesized the MNIR-QDs via a hot colloidal synthesis approach to yield monodisperse and tunable QDs. These hydrophobic QDs were structurally and compositionally characterized and further functionalized with amino-PEG and carboxyl-PEG to improve their biocompatibility. Since QDs are known to be toxic due to the presence of cadmium, we have evaluated the in vitro and in vivo toxicity of our surface-functionalized MNIR-QDs. Our results revealed that surface-functionalized MNIR-QDs did not exhibit significant toxicity at the concentrations used in the experiments and are therefore suitable for biological applications. For further in vitro applications, we covalently linked folic acid to the surface of amino-PEG-coated MNIR-QDs through NHS chemistry to target the folate receptors largely present in the HeLa cells to demonstrate the specific targeting and magnetic behavior of these MNIR-QDs. Improved specificity has been observed with treatment of HeLa cells with the folic acid-linked amino PEG-coated MNIR QDs (FA-PEG-MNIR-QDs) compared to the one without folic acid. Since the synthesized probe has magnetic property, we have also successfully demonstrated sorting between the cells which have taken up the probe with the use of a magnet. Our findings strongly suggest that these functionalized MNIR-QDs can be a potential probe for targeting, cellular sorting, and bioimaging applications.  相似文献   
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Electromagnetic fields (EMFs) can affect living cells due to biochemical changes, followed by changes in levels of trace elements in serum and different organs. This study focuses on the effect of whole body exposure to EMF, presented everywhere in our environment, and on the levels of trace elements in serum, femur, brain, kidney, and liver tissues. The analyses performed on 29 guinea pigs were divided into five groups. Guinea pigs were exposed to a magnetic field of 50 Hz of 1.5 mT. Groups A and B were exposed to the magnetic field for a period of 4 h/day continuously (4 h/day) for 4 and 7 days, respectively. Groups C and D were exposed to the magnetic field for a period of 4 h/day intermittently for 4 and 7 days, respectively. Group E animals were enrolled as control. Copper (Cu), zinc (Zn), calcium (Ca), and magnesium (Mg) levels were determined by atomic absorption spectroscopy in serum, femur, brain, kidney, and liver tissues in all guinea pigs. When compared to the control groups, the changes in the levels of Cu in serum samples, femur, and kidney tissues of the treated groups were statistically significant. The same was also true for the levels of Mg in the brain, kidney, and lung tissues. Our results suggest that in vivo continuous and intermittent exposure to EMF may cause disturbances in homeostasis of bioelements. These effects could be important risk factors for toxic effects of EMF, especially in relation to deterioration of bioelements.  相似文献   
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A novel concept of vaccination, employing virus-antibody complex has been reported for the control of infectious bursal disease in chickens. A comparison of virus replication, serum neutralizing antibody response and pathogenicity in chickens inoculated with the antibody coated virus, prepared by mixing virus and antibody in different ratios (1:1, 1:0.1, 1: 0.01) and virus alone without antibody, has been made. Antibody coated virus (when mixed in certain crucial ratios) replicated to a higher magnitude in the target organ, caused more severe pathogenesis but induced a primary serum neutralizing antibody response almost comparable. The results may have important implications in understanding of pathogenesis and development of control strategies against infectious bursal disease virus, specially employing immune complex vaccine.  相似文献   
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This study reevaluates a surgical technique known as the Chula technique, previously reported in 1991 for correction of frontoethmoidal encephalomeningocele. From 1986 to 1999, 108 patients were operated on with this technique, which could remove the herniation mass, repair dural and bone defects, reconstruct the naso-orbital area, and restore aesthetic facial appearance in a single stage. Formal frontal craniotomy was not necessary. The result has been very satisfying in terms of safety, cure rate, and aesthetic outcome. Spontaneous improvement of lacrimal passage obstruction occurred in 85.2 percent of cases, and dacryocystorhinostomy was required in the rest. There was no mortality. Complications (e.g., wound infection, 6.5 percent; wire extrusion, 3.7 percent; meningitis, 2.8 percent; cerebrospinal fluid leakage, 2.8 percent; and postoperative increased intracranial pressure, 2.8 percent) were much less frequent than in other reports. With a mean follow-up period of 439 days (maximum, 12 years), there has been no recurrence.  相似文献   
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