Devanna Nayakanti

In recent past, the investigations on antimicrobial activity of metal-based nanoparticles gained significant interest by implantation of nanotechnology to synthesize the nanoparticles in nanoregion due to their high surface area and high reactivity. Especially, the antimicrobial agents play a pivotal role in various fields where the biological contamination occurs. For instance, microbes control the control the contamination of food in food packaging, in textile industry they can restrict the growth of microorganisms owing to sweat, in medicine they can reduce the risk of contamination in invasive and routine interventions. Owing to their enhanced specific surface area as reduced particle size lead to improved surface activity, zinc based nano particles exhibit good antimicrobial properties. Further, zinc oxide is ecofriendly material which impacts photocatalysis and photo oxidizing on biological and chemical species. This review focused on recent advancements in zinc based nano materials for antimicrobial applications. Specifically, this briefly discussed the various synthesis techniques, shape of various materials, different dopants that enhance the antimicrobial activity of zinc oxide along with antimicrobial properties of those materials.

In present work, nickel doped zinc ferrite nanoparticles were prepared via hydrothermal technique. The prepared nanopowders undergone various characterization techniques such as X-ray diffraction (XRD), scanning electron microscope (SEM), Fourier-transform infrared spectroscope (FTIR), vibrating sample magnetometer (VSM) and antimicrobial activity. Further, the XRD analysis revealed that the presence of sharp diffraction peaks and cubic-structure of the prepared samples. SEM analysis revealed that there is a significant degree of agglomeration in the samples, whereas VSM studies revealed the magnetic behaviour and cation distribution in the prepared samples. The prepared nanopowder has also been evaluated for its antimicrobial properties against both Gram-negative bacteria (Enterobacter aerogenes) and Gram-positive bacteria (Enterococcus faecalis). An increasing in the ratio of nickel to zinc in ferrite nanoparticles led to an evident rise in their activity. These nanoparticles with enhanced structure and antimicrobial properties could find applications in hygiene, therapeutic and textile fields.

Objective: An attempt has made in fabricating solid dispersions (SDs) by taking lercanidipine hydrochloride (LCD) as a model drug. Methods: The SDs were made using a poly mix of poly vinyl pyrrolidone (PVP) K-30, Poloxamer-188, and hydroxy propyl methyl cellulose (HPMC) K4M. Different proportions of LCD: polymer mix in 1:1, 1:3, 1:5, and 1:7 ratios were fabricated as SDs by solvent evaporation and melting method, further compressed into tablets. The LCD SDs were assessed for physicochemical, and LCD release possessions. Results: The results were observed to be attractive with the increase in solubility LCD SD (F-3 and F-7) with 1:5 ratios of LCD. Conclusion: The study concludes that the poly mix of PVP K-30, Poloxamer-188, and HPMC K4M and was found to be a better combination for elevating the solubility and release of LCD from the SDs.

Aim: For the Method development and validation of Anabasine and Nornicotine in human plasma LC-MS/MS technique is used. Methodology: Operated in positive electron spray ionization which removes the hardness in ions. Metoprolol is used as an internal standard. Mass analyzers are used to determine the mass to charge ratio. Liquid chromatography separates mixture components in the basis of differences in affinity for stationary and mobile phase. It removes undesired impurities. It increases reproducibility, sensitivity, robustness, detection of low-level proteins. C18 Column (Phenomenex Luna C18, 5 μm, 50*4.6mm ID) is used to for high resolution and peak area. Calibration curve is constructed with the help of linear regression. During the entire process no instability is found. Results: m/z values of Anabasine are 162.84(Q₁), 134.68(Q₃) and for Nornicotine are 148.90(Q₁), 79.82(Q₃). Back calculated curve is calculated at different concentrations from 1-1000ng/ml and their accuracy range from 97-105% for Anabasine and 93-108% for Nornicotine. In Anabasine and Nornicotine the precision and accuracy are calculated by Intra-batch and inter-batch. In the process of multi-step preparation, consider n=6 for intra-batch and n=18 for inter-batch the values obtained are between the nominal concentrations i.e., 90-110%. For each analyte the coefficients of variation are below nominal criteria <15%. For Anabasine and Nornicotine the average recovery rate is 98.3% and 94.3%.

The present study involves the design, synthesis, characterization and molecular docking studies of biologically active quinazolin-4-ones, which were synthesized by condensing 2-amino-4-substituted phenylthiazole with N-methylbenzoxazin-4-one. The N-methylbenzoxazin-4-one and 2-amino-4- substituted phenylthiazole were synthesized from N-methylanthranilic acid and substituted ketones, respectively. The ADME properties determined the synthetic accessibility of quinazolin-4-ones by in silico Swiss ADME. The colorectal anticancer screening was done by using cell HT-29 human colorectal adenocarcinoma based on molecular docking studies on 3GC7-the structure of p38alpha in complex with dihydroquinazolinone. Finally, compounds 5Dh8, 5DF6, 5Db2 and 5Di9 exhibited better activity at a concentration < 10 μg/mL when compared to 5-fluorouracil. The ADME properties revealed that all the compounds were within the range and docking studies showed the highest binding with glide score -7.19 and -7.027 Kcal/mol compared to the target protein -10.67 Kcal/mol.

The aim of this study of this study was to discover the best poloxamer as a solid dispersion carrier for thiocolchicoside (TCS). The compatibility of TCS with excipients was studied by differential scanning colorimetry and fourier transform infrared spectroscopy. Different formulations of solid dispersions (SDs) were made with poloxamer carriers, i.e. poloxamer-108, poloxamer-188, poloxamer-237, poloxamer-338, and poloxamer-407 were made by taking TCS:poloxamer in ratios of 1:1, 1:2, 1:4, and 1:6. The SDs were made by a novel microwave fusion method and compressed using an 8-station tablet compression machine. The fabricated SD tablets were characterized by physicochemical constraints and drug release rates. The release of TCS from the prepared SDs was later analyzed by kinetic models. TCS was observed to be compatible with the poloxamer carriers. The SD formulations showed satisfactory physicochemical constraints and TCS release following first-order release. Among the poloxamer carriers used, poloxamer-188 was the best for increasing the solubility and release rate of TCS from the SDs.

Vanadium(III) complexes having the composition VLCl3 [where L = 2-acetylpyridine acetoylhydrazone (APAH), 2-acetylpyridine benzoylhydrazone (APBH), 2-acetylthiophene acetoylhydrazone (ATAH) and 2-acetylthiophene benzoylhydrazone (ATBH)] have been investigated using physico-chemical and analytical techniques. Molar conductivity data suggested that the complexes are neutral. Structures of all the vanadium(III) complexes are determined based on infrared and UV-visible spectral data. Electronic spectra of vanadium(III) complexes show three peaks suggesting octahedral structure. Comparison of vibrational spectra of hydrazones and complexes suggest that the hydrazones act as neutral tridentate ligands. The ligands and their vanadium derivatives are screened for their bacteria destroying activity against pathogenic bacterial strains viz. Gram-negative E. coli, Gram-positive Bacillus, Gram-positive Staphylococcus aureus and Gram-negative P. aureoginosa. Bacteria destroying activities of present complexes are comparable to the activity of the streptomycin. Complexes show more activity than their respective ligands in the case of Gram-positive Bacillus and Gram-negative P. aureoginosa.

Copper(II) complexes having the formula CuL2 {where, L = 2-acetylthiophene acetoylhydrazone (ATAH), 2-acetylthiophene benzoylhydrazone (ATBH)} have been investigated on the basis of elemental analysis, molar conductivity measurements, magnetic susceptibility, UV-visible, IR and ESR spectral data. Non-electrolytic nature of the complexes are revealed by molar conductance data. IR spectral data suggested that hydrazones act as tridentate ligands. The spin Hamiltonian, orbital reduction and bonding parameters of complexes are calculated using ESR spectra of complexes. The compounds are screened for their antibacterial activities against Pseudomonas aureoginos and Bacillus cereus. Acetoylhydrazones show more antibacterial activity than the corresponding benzoyl hydrazones. Some of the Cu(II) complexes show more activity than hydrazone ligands.

The metabolic syndrome in HIV infected patients is particularly associated with the use protease inhibitors. Atazanavir is an inhibitor of the cytochrome P 450 (CYP) system, in particular CYP3A4 and CYP2C9 which can affect the metabolism of several drugs. To treat metabolic syndrome in HIV patients repaglinide is used and it is a short acting insulin secretagogues undergoing metabolism with CYP 3A4 and CYP 2C8 enzyme system. The purpose of this study was to assess the possible pharmacokinetic and pharmacodynamic drug interaction of repaglinide and atazanavir in healthy, diabetic and impaired hepatic function rats. Human oral therapeutic doses of atazanavir and repaglinide were extrapolated to rats based on the body surface area. The pharmacokinetic parameters and blood glucose concentrations of repaglinide were determined after oral administration of repaglinide alone (0.5 mg/kg) and in the presence of atazanavir (36 mg/kg) in normal, diabetic and hepatic impaired rats. The pharmacokinetics (PK) and blood glucose concentrations of repaglinide were significantly altered in the presence of atazanavir. The peak plasma concentration (Cmax), area under the plasma concentration time profile (AUC) and elimination half-life of repaglinide were significantly (P<0.0001) increased. The repaglinide clearance (CL) was significantly (P<0.0001) decreased in the presence of atazanavir treatment. In the presence of atazanavir, repaglinide hypoglycaemic activity was increased significantly (P<0.0001) when compared with the repaglinide control group. The present study demonstrated the significant difference in the PK/PD changes due to the enhanced bioavailability and decreased total body clearance of repaglinide may be due to the inhibition of the CYP P450 metabolic system, OATP and P-gp transporters by atazanavir.