Design of meloxicam and lornoxicam transdermal patches: Preparation, physical characterization, ex vivo and in vivo studies

Transdermal patches of meloxicam (MX) and lornoxicam (LX) were aimed to be prepared in order to overcome their side effects by oral application. The strategy was formulation of optimized films to prepare transdermal patches by determination of physical properties and investigation of drug-excipient compatibility. As the next step, in vitro drug release, assesment of anti-inflammatory effect on Wistar Albino rats, ex vivo skin penetration and investigation of factors on drug release from transdermal patches were studied. Hydroxypropyl methylcellulose (HPMC) was concluded to be suitable polymer for formulation of MX and LX transdermal films indicating pharmaceutical quality required. MX and LX transdermal patches gave satisfactory results regarding to the edema inhibition in the assessment of anti-inflammatory effect. MX was found out to be more effective compared to LX on relieving of edema and swelling. These results were supported by data obtained from ex vivo penetration experiments of drug through rat skin. Indicative parameters like log P, molecular weight and solubility constraint on penetration rate of drugs also indicated good skin penetration. Transdermal patches of MX and LX can be suggested to be used especially for the immediate treatment of inflammated area since it displays anti-inflammatory effect, soon.     

Fixed point theorems for Ćirić-type strong almost contractions on partial metric spaces

In the present paper we prove some fixed point theorems for ?iri?-type strong almost contractions on partial metric spaces. We also give an illustrative example.     

The effect of heme environment on the hydrogen abstraction reaction of camphor in P450cam catalysis: a QM/MM study

The discrepancies between the published QM/MM studies (Sch?neboom, J. C.; Cohen, S.; Lin, H.; Shaik, S.; Thiel, W. J. Am. Chem. Soc. 2004, 126, 4017; Guallar, V.; Friesner, R. A. J. Am. Chem. Soc. 2004, 126, 8501) on H-abstraction of camphor in P450cam have largely been resolved. The crystallographic water molecule 903 situated near the oxo atom of Compound I acts as a catalyst for H-abstraction, lowering the barrier by about 4 kcal/mol. Spin density at the A-propionate side chain of heme can occur in the case of incomplete screening but has no major effect on the computed barrier.     

Thermochemistry of N‐heterocyclic carbenes with 5‐, 4‐, 3‐, and 2‐membered rings

N‐heterocyclic carbenes (NHCs) based on imidazole‐2‐ylidene ( 1 ) or the saturated imidazolidine‐2‐ylidene ( 2 ) scaffolds are long‐lived singlet carbenes. Both benefit from inductive stabilization of the sigma lone pair on carbon by neighboring N atoms and delocalization of the N pi lone pairs into the nominally vacant p‐pi atomic orbital at the carbene carbon. With thermochemical schemes G4 and CBS‐QB3, we estimate the relative thermodynamic stabilization of smaller ring carbenes and acyclic species which may share the keys to NHC stability. These include four‐membered ring systems incorporating the carbene center, two trivalent N centers, and either a boron or a phosphorus atom to complete the ring. Amino‐substituted cyclopropenylidenes have been reported but three‐membered rings containing the carbene center and two N atoms are not known. Our calculations suggest that amino‐substituted cyclopropenylidenes are comparable in stability to the four‐membered NHCs but that diazacyclopropanylidenes would be substantially less effectively stabilized. Concluding the series are acyclic carbenes with and without neighboring N atoms and a series of “two‐membered ring” azapropadienenylidene cations of form :C?N?W with W = an electron‐withdrawing agent. We have studied W = NO₂, CH₂(+), CF₂(+), and (CN)₂C(+). Although these systems display a degree of stabilization and carbene‐like electronic structure, the stability of the NHCs is unsurpassed. © 2014 Wiley Periodicals, Inc.     

Influence of Solute–Solvent Interaction on Acid Strength of Some Substituted Phenols in Ethanol–Water Media

The solute–solvent interactions of some phenol derivatives were investigated potentiometrically in 0–60 % (v/v) ethanol–water mixtures. The acidity constants values were correlated with either macroscopic parameters such as molar fraction, permittivity and the solvating ability or microscopic parameters, such as the Kamlet–Taft solvatochromic parameters. Moreover, it is demonstrated that the pK _a values in any ethanol–water mixtures are linearly related to the pK _a values of the phenols in pure water. The slope and intercept parameters of the linear correlations are related with the mole fraction of ethanol. These equations permit accurate calculation of the pK _a values of the studied phenols at any ethanol–water composition.     

Photoactivable peptides for identifying enzyme-substrate and protein-protein interactions

Photoactivated cross-linking of peptides to proteins is a useful strategy for identifying enzyme-substrate and protein-protein interactions in cell lysates as demonstrated by studies on the human hypoxia inducible factor system.     

Linear parameter varying feedforward control synthesis using parameter-dependent Lyapunov function

This paper presents the dynamic feedforward control synthesis for linear parameter varying (LPV) systems. It is assumed that all system matrices are dependent on varying parameters, which are measurable with sensor or observable. The parameters have bounded variation rates. Parameter-dependent Lyapunov function is used for the feedforward control synthesis such that the robust stability is assured for all varying parameters at the time of the operation. The method is formulated in terms of linear matrix inequalities for LPV feedforward controller that guarantees the stability of the transfer matrix having \(L_{2}\) -gain. This compensator is designed by adding on the feedback controller in two degrees of freedom control configuration. This controller can be used for the disturbance attenuation or decreasing the tracking error. The numerical examples and simulations are given to provide the applicability of the proposed solution.     

Improved results on the stability analysis of linear neutral systems with delay decay approach

In this paper, the investigation of the asymptotical stability of linear neutral systems with time-varying delay has been presented. In order to achieve the desired results, the integral inequality approach was used to express relationships between terms of Newton-Leibniz formula technique and was constructed an appropriate Lyapunov-Krasovskii functional. By improving a delay decay approach, the stability criteria for the zero solution of system were formulated as linear matrix inequalities (LMIs) which can be easily solved. Two numerical examples have been given to show the applicability of established assumptions and the effectiveness of proposed method by MATLAB-Simulink.     

Natural radioactivity and hazard-level assessment of Portland cements in Turkey

The natural radioactivity levels and some radiological parameters of Turkish Portland cements (PC) originated in various regions were determined in this study. The activity concentration of cement samples for ²²⁶Ra, ²³²Th, and ⁴⁰K were measured using a gamma-ray spectrometer with high purity germanium radiation detector. The PC samples had activity concentrations of 33.0, 16.7, and 239.5 Bq kg⁻¹ for ²²⁶Ra, ²³²Th, and ⁴⁰K, respectively. The mean value of radium equivalent value (Ra_eq) was found to be 75.4 Bq kg⁻¹. The radium equivalent values in the cement samples were lower than the acceptable level of 370 Bq kg⁻¹. The calculated radiological parameters were found to be below the acceptance levels.