Studies of thermoluminescence properties of liquid crystalline N-phenyl substituted phenyl polysiloxane hydroxamic acids.

The investigation of thermoluminescence (TL) glow curves in liquid crystalline side chain N-phenyl-substituted phenyl polysiloxane hydroxamic acids (PHAs) has yielded significant insights. These polymers demonstrated TL behavior when exposed to ß-radiation between 0 and 220°C, indicating inherent luminescent properties when irradiated. Notably, a dose-dependent relationship was observed in reported derivatized polymers; this study elucidates the diverse TL characteristics exhibited by various liquid crystalline side chain N-phenyl-substituted phenyl PHAs when exposed to ß-radiation. Understanding these dose-dependent and dose-independent behaviors enhances the knowledge of their luminescent properties and potential applications in radiation detection.

Estimation of time since death using cardiac troponin I in case of death due to asphyxia and cardiotoxicity of acebutolol.

The objective of this study was to investigate the degradation pattern of cardiac troponin I in rats in vivo, and to determine whether the pattern was dependent on the cause of death, for the purpose of estimating the postmortem interval. The rats were categorized into three distinct groups depending on the factors leading to their demise: the control group, the group experiencing acebutolol-induced cardiotoxicity, and the group affected by asphyxia. The analysis encompassed the isolation and segregation of the protein, subsequently employing Western blotting as a means of visualizing the results. The results revealed a distinct degradation pattern of cTnI into smaller fragments over time, indicating that cardiac troponin I can serve as a reliable marker for estimating the postmortem interval. Furthermore, noteworthy variations were noted in the degradation pattern of cardiac troponin I among the different causes of death, which suggests that this method can also be used to determine whether cardiac failure was the cause of death or not.

Pharmacokinetics of single oral dose trazodone: a randomized, two-period, cross-over trial in healthy, adult, human volunteers under fed condition.

OBJECTIVE: To assess the bioequivalence of single dose trazodone hydrochloride USP 100 mg tablets administered as an oral dose under fed condition. METHODS: This study was an open-label, balanced, randomized, two-sequence, two-treatment, two-period, single oral dose, crossover bioequivalence study in healthy, adult, human subjects under fed conditions. After an overnight fast of at least 10 h, the subjects were served a high fat and high calorie vegetarian breakfast, which they were required to consume within 30 min. A single oral dose (100 mg) of either the test or the reference product was administered to the subjects. The primary pharmacokinetic parameters, maximum plasma concentration (Cmax) and area under the plasma concentration-time curve (AUC) from time zero to last measurable concentration (AUC0-t ) and extrapolated to infinity (AUC0-∞) were compared by an analysis of variance using log-transformed data. Bioequivalence was concluded if the 90% confidence intervals (CIs) of the adjusted geometric mean (gMean) ratios for C max and AUC were within the predetermined range of 80-125%, in accordance with regulatory requirements. RESULTS: For the test formulation, the trazodone gMean Cmax was 1480.9 ng/mL (vs. 1520.2 ng/mL for reference), AUC0-t was 18193.0 ng·h/mL (vs. 18209.8 ng·h/mL) and AUC0-∞ was 19346.3 ng·h/mL (vs. 19393.4 ng·h/mL). The 90% CIs for the ratio (test/reference) were 93.0-102.0% for Cmax, 96.7-103.2% for AUC0-t and 96.1-103.5% for AUC0-∞. There were no deaths or serious adverse events during the conduct of the study. CONCLUSION: Test product when compared with the Reference product meets the bioequivalence criteria with respect to the extent of absorption of trazodone under fed condition.

Curcumin loaded self assembled lipid-biopolymer nanoparticles for functional food applications.

The supramolecular nano-assemblies formed by electrostatic interactions of two oppositely charged lipid and polymer have been made and used as nanocarriers for curcumin to address its bioavailability and solubility issues. These curcumin encapsulated nano-supramolecular assemblies were characterized with respect to their size (dynamic light scattering), morphology (TEM, SEM), zeta potential (Laser Doppler Velocimetry), encapsulation efficiency (EE), curcumin loading (CL) etc. Stability of the nano-assemblies was assessed at different storage times as a function of varying pH and temperature. The physicochemical characterization of nano-assemblies was performed using Fourier Transform Infra Red Spectroscopy (FT-IR) and Differential Scanning Calorimetry (DSC). The in-vitro antioxidant lipid peroxidation (TBARS), radical scavenging (DPPH, NO, H2O2, reducing power) activity assays of powdered curcumin and nano-encapsulated curcumin were performed. It was found that nano-encapsulated curcumin were roughly spherical in shape, presented high positive zeta potential (>30 mV), monodisperse (polydispersity index <0.3), amorphous in nature, stable in the pH range of 2-6 and have enhanced antioxidant potency in comparison to crystalline curcumin in aqueous media. In conclusion, the curcumin encapsulated nanocarriers system has great potential as functional food ingredient of natural origin.

Highly stable antibacterial silver nanoparticles as selective fluorescent sensor for Fe³âº ions.

Calix[4]resorcinarene polyhydrazide (CPH) protected water dispersible fluorescent silver nanaoparticles (AgNps) were prepared by one-pot method using water soluble CPH and AgNO3. (CPH) bearing hydrazide group on its periphery acts as a reducing agent and its web type of structure as a stabilizing agent for the formation of calix protected silver nanoparticles (CPH-AgNps). CPH-AgNps were found to be highly stable over 120 days at room temperature and at varied pH. CPH-AgNps were characterized by UV/Vis-spectroscopy, particle size analyzer (PSA), transmission electron microscopy (TEM) and Energy dispersive X-ray analysis (EDX). Duly characterized nanoparticles were explored for their application as sensitive and selective fluorescent chemosensors for various metal ions. It was found that nanoparticles were selective and sensitive only for Fe(3+) ions with the linear range of detection from 0.1 µM to 10 µM. CPH-AgNps were also found to exhibit good antimicrobial activity when compared with standard Chloramphenicol. The selectivity and antimicrobial activity of CPH-AgNps suggests its potential use as a sensor for Fe(III) ions in ecosystems prone to industrial pollution and as an antimicrobial agent in biological applications.

Emerging Strategies and Applications of Layer-by-Layer Self-Assembly.

Layer-by-layer self-assembly is an approach to develop an ultrathin film on solid support by alternate exposure to positive and negative species with spontaneous deposition of the oppositely charged ions. This paper summarizes various approaches used for fabrication of layer-by-layer self-assembly as well as their utility to produce various devices. The layer-by-layer technique is basically used for formation of multilayer films. A variety of nanomaterials use it for the modification of films to enhance their resultant durability as well as strength. Studies have shown that many different types of materials can be used for fabrication of multilayers. Recently the layer-by-layer self-assembly technique has also been used for fabrication of gas sensors, hydrogen sensors and solar-based cells. Various methods, such as spin deposition, calcinations, and dry-transfer printing are being used for fabrication of thin films. In this review, the author summarizes the various interesting properties as well as fabrication strategies of layer-by-layer self-assembly.

Natural polyphenols in the management of major depression.

INTRODUCTION: Natural polyphenols, the non-essential micronutrients, found in array of plant products, are known to affect various physiological and biochemical functions in the body. Studies have shown the protective effect of these polyphenols in different neurological and mental disorders. These polyphenols modulate monoaminergic neurotransmission in the brain and thus possess antidepressant-like activity at least in animal models of depression. AREAS COVERED: The present review discusses the use of these natural polyphenols in the treatment of major depression. The review article discusses the antidepressant potential of some important polyphenols such as amentoflavone, apigenin, chlorogenic acid, curcumin, ferulic acid, hesperidin, rutin, quercetin, naringenin, resveratrol, ellagic acid, nobiletin and proanthocyanidins. The mechanism of action of these polyphenols in the treatment of major depression is also discussed in detail. EXPERT OPINION: There is an exciting prospect in the discovery of natural polyphenols as therapeutic agents in the treatment of major depression.

High throughput screening: an in silico solubility parameter approach for lipids and solvents in SLN preparations.

OBJECTIVE: The present paper describes an in silico solubility behavior of drug and lipids, an essential screening study in preparation of solid lipid nanoparticles (SLN). MATERIALS AND METHODS: Ciprofloxacin HCl was selected as a model drug along with 11 lipids and 5 organic solvents. In silico miscibility study of drug/lipid/solvent was performed using Hansen solubility parameter approach calculated by group contribution method of Van Krevelen and Hoftyzer. Predicted solubility was validated by determining solubility of lipids in various solvent at different temperature range, while miscibility of drug in lipids was determined by apparent solubility study and partition experiment. RESULTS AND DISCUSSION: The presence of oxygen and OH functionality increases the polarity and hydrogen bonding possibilities of the compound which has reflected the highest solubility parameter values for Geleol and Capmul MCM C8. Ethyl acetate, Geleol and Capmul MCM C8 was identified as suitable organic solvent, solid lipid and liquid lipid respectively based on a solubility parameter approach which was in agreement with the result of an apparent solubility study and partition coefficient. CONCLUSION: These works demonstrate the validity of solubility parameter approach and provide a feasible predictor to the rational selection of excipients in designing SLN formulation.

Ciprofloxacin hydrochloride-loaded glyceryl monostearate nanoparticle: factorial design of Lutrol F68 and Phospholipon 90G.

PURPOSE: This investigation was undertaken to develop glyceryl monostearate (Geleol)-based solid lipid nanoparticles (SLNs) of a hydrophilic drug ciprofloxacin HCl. METHODS: Hansen's solubility parameter study was carried out in screening of a suitable carrier and solvent system. Subsequently, SLNs were prepared by solvent diffusion evaporation method and investigated for particle size, polydispersity index (PDI), zeta potential (ZP), entrapment efficiency (EE) and drug release behaviour. RESULTS: Variations in SLN composition resulted in particle sizes between 170 and 810 nm and ZPs between 8 and 14 mV. The maximum EE was found to be 26.3% with particle size of 188.8 nm. SLN can sustain the release of drug for up to 15 h and it shows Higuchi matrix model as the best-fitted model. SLNs were stable without aggregation of particles under storage conditions. CONCLUSIONS: The results of this study provide the framework for further study involving the SLN formulation for hydrophilic drug molecule.

Design, synthesis, and antitubercular evaluation of novel series of 3-benzofuran-5-aryl-1-pyrazolyl-pyridylmethanone and 3-benzofuran-5-aryl-1-pyrazolylcarbonyl-4-oxo-naphthyridin analogs.

Twenty-eight newer 3-benzofuran-5-aryl-1-pyrazolyl-pyridylmethanone and 3-benzofuran-5-aryl-1-pyrazolylcarbonyl-4-oxo-naphthyridin analogs were synthesized by microwave irradiation method and evaluated for in-vitro and in-vivo antitubercular activity against multidrug-resistant M. tuberculosis stains. Structure-activity relationship study was carried out and found NO(2) (o) substituted 3-benzofuran-5-aryl-1-pyrazolylcarbonyl-4-oxo-naphthyridin was most potent antitubercular agent against M. tuberculosis, even better than standard drug isoniazid and comparable with rifampin. Other synthesized compounds 7j, 7f, 7a, 7e and 5d, 5f were found moderate to good activity in in-vitro model at lower IC(50) values 85 microM, 154 microM, 157 microM, 164 microM, 170 microM and 190 microML respectively. In in-vivo animal model compound 7j was drastically reduced the bacterial load in lung and spleen tissues at the dose of 25 mg/kg body weight.

Microwave assisted synthesis of new indophenazine 1,3,5-trisubstruted pyrazoline derivatives of benzofuran and their antimicrobial activity.

2-[1-(5,8-Dihydro quinoxalino[2,3-b]indoloacetyl)-3-(1-benzofuran-2-yl)-4,5-dihydro-1H-pyrazol-5-yl] phenyl derivatives were synthesized from 2-(5,8-dihydro quinoxalino[2,3-b]indol-5-yl) acetohydrazide and (2E)-1-(1-benzofuran-2-yl)-4-phenylbut-2-en-1-ones derivatives using microwave-assisted route. The structures of all the compounds have been established on the basis of analytical and spectral data. Among the 14 compounds IPB-1, IPB-5, IPB-10, IPB-11 and IPB-12 were found good antibacterial activity and MICs were found bellow 10microg/mL against Escherichia coli, Pseudomonas aeruginosa and Streptococcus aureus, which can compared with sparfloxacin and norfloxacin.

Selective extraction, preconcentration and transport studies of thorium(IV) using octa-functionalized calix[4]resorcinarene-hydroxamic acid.

A new calix[4]resorcinarene bearing eight hydroxamic acid groups (C4RAHA) has been synthesized and characterized by FT-IR, 1H-NMR and elemental analysis. Its analytical properties were investigated, and showed high affinity and selectivity toward thorium(IV) in the presence of large quantities of associated metal ions. Thorium(IV) was extracted from an ethyl acetate solution of C4RAHA at pH 4.5. The lambdamax and molar absorptivity (epsilon) for thorium(IV) were 341 nm and 7120 l mol(-1) cm(-1). The complexation of thorium(IV) with C4RAHA has a 4:1 metal:ligand stoichiometry, which is relatively rare. The extracts were directly aspirated in the plasma for ICP-AES measurements for thorium(IV) in the presence of a diversified matrix. The system obeyed Beer's law over the range 0.1 - 6.5 microg ml(-1) of thorium(IV) with a Sandell sensitivity of 0.0325 microg cm(-2). The preconcentration factor and overall stability constant evaluated at 25 degrees C for thorium(IV) were 133 and 15.86, respectively. The complexation was characterized by a favorable enthalpy change. A liquid-membrane transport study of thorium(IV) was carried out from the source to the receiving phase under controlled conditions, and a mechanism of transport proposed. To check the validity of the proposed method, thorium(IV) was determined in monazite sand, rare earth sand and water samples.