Solubilization of Glibenclamide with β-Cyclodextrin & its Derivatives

Gilbenclamide, a widely used potent hypoglycaemic agent was solubllized using β -Cyclodextrin and β -Cyclodextrin derivatives. Complexes were prepared by kneading method in a molar ratio of 1:1 of the drug and the cyclodextrlns respectively. The Glibenclamide β -Cyelocextrin complex was characterized and evaluated by I.R. studies, Differential Scanning Calorimotry 6 X-ray diffractometry. The in-vitro dissolution rates of drug from inclusion complexes of β Cyclodextrins and its derivatives were compared. A significant Improvement In dissolution lor, rates of Gllbenclamide was observed with Inclusion complexes of all the Cyclodextrins. However, the solubilizing effect was more in case of β-Cyclodextrin derivatives.     

Emergence of Gold‐Mesoporous Silica Hybrid Nanotheranostics: Dox‐Encoded,Folate Targeted Chemotherapy with Modulation of SERS Fingerprinting for Apoptosis Toward Tumor Eradication

Strategically fabricated theranostic nanocarrier delivery system is an unmet need in personalized medicine. Herein, this study reports a versatile folate receptor (FR) targeted nanoenvelope delivery system (TNEDS) fabricated with gold core silica shell followed by chitosan–folic acid conjugate surface functionalization by for precise loading of doxorubicin (Dox), resembled as Au@SiO₂‐Dox‐CS‐FA. TNEDS possesses up to 90% Dox loading efficiency and internalized through endocytosis pathway leading to pH and redox‐sensitive release kinetics. The superior FR‐targeted cytotoxicity is evaluated by the nanocarrier in comparison with US Food and Drug Administration (FDA)‐approved liposomal Dox conjugate, Lipodox. Moreover, TNEDS exhibits theranostic features through caspase‐mediated apoptosis and envisages high surface plasmon resonance enabling the nanoconstruct as a promising surface enhanced Raman scattering (SERS) nanotag. Minuscule changes in the biochemical components inside cells exerted by the TNEDS along with the Dox release are evaluated explicitly in a time‐dependent fashion using bimodal SERS/fluorescence nanoprobe. Finally, TNEDS displays superior antitumor response in FR‐positive ascites as well as solid tumor syngraft mouse models. Therefore, this futuristic TNEDS is expected to be a potential alternative as a clinically relevant theranostic nanomedicine to effectively combat neoplasia.     

Chaos in fractional ordered Liu system

Present paper deals with fractional version of a dynamical system introduced by C. Liu, L. Liu and T. Liu [C. Liu, L. Liu, T. Liu, A novel three-dimensional autonomous chaos system, Chaos Solitons Fractals 39 (4) (2009) 1950–1958]. Numerical investigations on the dynamics of this system have been carried out. Properties of the system have been analyzed by means of Lyapunov exponents. Furthermore the minimum effective dimensions have been identified for chaos to exist in commensurate and incommensurate orders. It is noteworthy that the results obtained are consistent with the analytical conditions given in the literature.     

An overhead and resource contention aware analytical model for overloaded Web servers

A Web server, when overloaded, shows a severe degradation of goodput initially, with the eventual settling of goodput as load increases further. Traditional performance models have failed to capture this behavior. In this paper, we propose an analytical model, which is a two-stage and layered queuing model of the Web server, which is able to reproduce this behavior. We do this by explicitly modelling the overhead processing, the user abandonment and retry behavior, and the contention for resources, for the FIFO and LIFO queuing disciplines. We show that LIFO provides better goodput in most overload situations. We compare our model predictions with experimental results from a test bed and find that our results match well with measurements.     

<Emphasis Type="Italic">New-Age</Emphasis>: A Negative Bias Temperature Instability-Estimation Framework for Microarchitectural Components

Degradation of device parameters over the lifetime of a system is emerging as a significant threat to system reliability. Among the aging mechanisms, wearout resulting from Negative Bias Temperature Instability (NBTI) is of particular concern in deep submicron technology generations. While there has been significant effort at the device and circuit level to model and characterize the impact of NBTI, the analysis of NBTI’s impact at the architectural level is still at its infancy. To facilitate architectural level aging analysis, a tool capable of evaluating NBTI vulnerabilities early in the design cycle has been developed that evaluates timing degradation due to NBTI. The tool includes workload-based temperature and performance degradation analysis across a variety of technologies and operating conditions, revealing a complex interplay between factors influencing NBTI timing degradation.     

Copyright protection using KELM-PSO based multi-spectral image watermarking in DCT domain with local texture information based selection

Multimedia Tools and Applications - Since many years, researchers have been developing techniques for copyright protection. This paper presents a novel approach for copyright protection of...     

Rapid Discovery of Aspartyl Protease Inhibitors Using an Anchoring Approach

Pharmacophore searches that include anchors, fragments contributing above average to receptor binding, combined with one-step syntheses are a powerful approach for the fast discovery of novel bioactive molecules. Here, we are presenting a pipeline for the rapid and efficient discovery of aspartyl protease inhibitors. First, we hypothesized that hydrazine could be a multi-valent warhead to interact with the active site Asp carboxylic acids. We incorporated the hydrazine anchor in a multicomponent reaction and created a large virtual library of hydrazine derivatives synthetically accessible in one-step. Next, we performed anchor-based pharmacophore screening of the libraries and resynthesized top-ranked compounds. The inhibitory potency of the molecules was finally assessed by an enzyme activity assay and the binding mode confirmed by several soaked crystal structures supporting the validity of the hypothesis and approach. The herein reported pipeline of tools will be of general value for the rapid generation of receptor binders beyond Asp proteases.     

Optical and structural properties of electrodeposited polyaniline/Q‐CdS composites

HCl doped polyaniline (PANI)/Q‐CdS composite thin films have been synthesized using the electrodeposition route on indium tin oxide (ITO) coated glass substrates. Three different sizes of CdS quantum dots were uniformly dispersed in PANI matrix. As deposited samples were characterized by X‐ray diffraction (XRD) and X‐ray photoelectron spectroscopy (XPS). Optical properties of the composite structures were investigated by using optical absorption, photoluminescence, and Raman spectroscopy. PANI/Q‐CdS composite showed significant improvement in the thermal behavior as indicated by thermogravimetric analysis (TGA) thermograph. Our results also indicated that the doping state of the nanocomposites was dependent on the size of the CdS nanoparticles and improved with decreasing size. POLYM. COMPOS., 35:1864–1874, 2014. © 2014 Society of Plastics Engineers     

Development, characterization and stabilization of amorphous form of a low Tg drug

The objective of the present study was to develop a stable amorphous form of model drug carvedilol (CAR). The amorphous material produced by melt quench technique was subjected to physico-chemical characterization. Chemical stability of the drug during preparation of glass was tested by HPLC and IR spectroscopy and presence of amorphous form was confirmed by DSC and XRPD. The rate of dissolution and magnitude of the apparent solubility were found to be significantly higher for amorphous CAR than for crystalline CAR, at 25 °C. However at 37 °C, it was observed that dissolution of the amorphous form did not show a noticeable improvement over pure CAR over the period of 60 min, due to formation of cohesive supercooled liquid state. This observation was supported by enthalpy relaxation study, which indicated increase in enthalpy recovery and structural relaxation of amorphous form towards the supercooled liquid region. This indicated the functional inability of amorphous CAR from stability point of view and suggested the need for elevation of T_g. Hence combination of solid dispersion (SD) and surface adsorption techniques was attempted to overcome the functional limitations of amorphous CAR. SD in the ratio of 1:2:2 parts by weight of CAR, PVP (for elevation of T_g) and Aerosil^® 200 (as adsorbent) respectively presented dramatic improvement in rate and extent of drug dissolution. During accelerated stability studies with SD 1:2:2 the dissolution characteristics were slightly decreased over the period of 3 months and no crystallization events were observed. Thus, to exploit the functional advantage of amorphous form of low T_g drugs, formation of ternary SD system is recommended.     

Studies on Dehydration of Sapota (Achras zapota)

Sapota (Achras zapota) is a tropical fruit found in several parts of India. It is one of the most popular fruits besides mango, custard apple, and several others. Once ripe, it needs to be consumed within a couple of days due to the highly perishable nature of this exquisite fruit variety. The best way to increase the shelf-life is through the process of dehydration of peeled sapota. In the present study, the convective air drying of sapota pulp was carried out and compared with low-temperature drying techniques such as heat pump-assisted drying and freeze drying. The sapota paste was dried in a convective dryer to study the effect of operating parameters such as air temperature and air velocity. In addition, the effect of additives such as oat and wheat fibers and the paste thickness on drying was also studied. The critical analysis of dehydrated sapota was carried out in terms of water activity, sugar content, color, and rehydration ratio. The drying data were analyzed using Page's model and Newton's model on the basis of root mean square error (RMSE), reduced χ square (χ²) and correlation coefficient (R²).