Synthesis of 11-(Piperazin-1-yl)-5H-dibenzo[b,e] [1,4]diazepine on Kilo Scale

Abstract: A synthesis of 11-(piperazin-1yl)-5H-dibenzo [b,e][1,4]diazepine on kilo scale without any chromatographic purification step is reported. Key steps involved are Ullmann condensation, catalytic hydrogenation, and catalyzed cyclization

PERFORMANCE EVALUATION OF TRIBOLOGICAL PROPERTIES OF COTTON SEED OIL FOR MULTI-CYLINDER ENGINE

A lubricant is a substance that reduces friction and wear by providing a protective film between two moving surfaces. Good lubricants possess the properties such as low toxicity, high viscosity index, high load carrying capacity, excellent coefficient of friction, good anti-wear capability, low emission into the environment, high ignition temperature. So tribology related problems can be minimized by proper selection of lubricant from wear consideration. Today, the depletion of reserves of crude oil, the growing prices of crude oil and concern about protecting the environment against pollution have developed the interest towards environment-friendly lubricants. Because of these the purpose of this work is to evaluate the anti-wear characteristics of cottonseed oil and to check the suitability of cottonseed oil as a lubricant for multi-cylinder engine

POTENTIAL OF COTTON SEED OIL AS AN ALTERNATING LUBRICANT FOR MULTI-CYLINDER ENGINE

A lubricant is a substance that reduces friction and wear by providing a protective film between two moving surfaces. Good lubricants possess properties like low toxicity, high load carrying capacity, excellent coefficient of friction, high viscosity index, good anti-wear capability, low emission into the environment, high ignition temperature. Hence tribology related problems can be minimized by proper selection of lubricant. Now a day depletion of reserves of crude oil, growing prices of crude oil and concern about protecting the environment against pollution have created the interest towards environment-friendly lubricants. Hence paper work is related to check the suitability and to evaluate the anti-wear characteristics of cottonseed oil as a lubricant for multi-cylinder engine. Anti-wear testing is carried out on four ball testing machine as per ASTM D 4172. Image Acquisition System is used to check wear preventive characteristic of cottonseed oil by measuring wear scar diameter

Preparation and Characterization of Furosemide-Silver Complex Loaded Chitosan Nanoparticles

Antibiotic-resistant bacteria may result in serious infections which are difficult to treat. In addition, the poor antibiotic pipeline has contributed to the crisis. Recently, a complex of furosemide and silver (Ag-FSE) has been reported as a potential antibacterial agent. However, its poor aqueous solubility is limiting its activity. The purpose of this study was to encapsulate Ag-FSE into chitosan nanoparticles (CSNPs) and evaluate antibacterial efficacy. Ag-FSE CSNPs were prepared using an ionic gelation technique. The particle size, polydispersity index, and zeta potential of Ag-FSE CSNPs were 197.1 ± 3.88 nm 0.234 ± 0.018 and 36.7 ± 1.78 mV, respectively. Encapsulation efficiency was 66.72 ± 4.14%. In vitro antibacterial activity results showed that there was 3- and 6-fold enhanced activity with Ag-FSE CSNPs against E. coli and S. aureus, respectively. Results also confirmed that Ag-FSE CSNPs showed ~44% release within 4 h at pH 5.5 and 6.5. Moreover, release from the CSNPs was sustained with a cumulative release of ~75% over a period of 24 h. In conclusion, encapsulation of Ag-FSE into CSNPs resulted in significant improvement of antibacterial efficacy with a sustained and pH-sensitive release. Therefore, Ag-FSE CSNPs can be considered as a potential novel antibacterial agent against bacterial infections

Formulation and Molecular Dynamics Simulations of a Fusidic Acid Nanosuspension for Simultaneously Enhancing Solubility and Antibacterial Activity

The aim of the present study was to formulate a nanosuspension (FA-NS) of fusidic acid (FA) to enhance its aqueous solubility and antibacterial activity. The nanosuspension was characterized using various in vitro, in silico, and in vivo techniques. The size, polydispersity index, and zeta potential of the optimized FA-NS were 265 ± 2.25 nm, 0.158 ± 0.026, and −16.9 ± 0.794 mV, respectively. The molecular dynamics simulation of FA and Poloxamer-188 showed an interaction and binding energy of −74.42 kJ/mol and −49.764 ± 1.298 kJ/mol, respectively, with van der Waals interactions playing a major role in the spontaneous binding. There was an 8-fold increase in the solubility of FA in a nanosuspension compared to the bare drug. The MTT assays showed a cell viability of 75–100% confirming the nontoxic nature of FA-NS. In vitro antibacterial activity revealed a 16- and 18-fold enhanced activity against <i>Staphylococcus aureus</i> (SA) and methicillin-resistant SA (MRSA), respectively, when compared to bare FA. Flowcytometry showed that MRSA cells treated with FA-NS had almost twice the percentage of dead bacteria in the population, despite having an 8-fold lower MIC in comparison to the bare drug. The in vivo skin-infected mice showed a 76-fold reduction in the MRSA load for the FA-NS treated group compared to that of the bare FA. These results show that the nanosuspension of antibiotics can enhance their solubility and antibacterial activity simultaneously