A New Approach to the Dissolution Tests Management to Obtain Kinetic and Thermodynamic Data: Release of a Model Drug from Glyceryl Behenate Matrix Tablets

This study is focused on the use of glyceryl behenate as a lipophilic excipient of matrix tablets providing controlled drug release. The aim of this study is to evaluate activation energy (EA) and changes of the thermodynamic parameters (ΔH, ΔS, ΔG) of a dissolution process. These values, which have not yet been published, can lead to better understanding of a drug release mechanism and can extend the use options of glyceryl behenate in the pharmaceutical industry. Values of ΔH, ΔS, ΔG and E_A, providing an overall thermodynamic view on the studied matrix tablets, are evaluated based on the temperature-dependences of the release rate constant of a model drug (temperature range 25 - 45 °C). The studied lipophilic matrix tablets contain 10% to 50% of glyceryl behenate. Dissolution testing is carried out in an aqueous solution of HCl with addition of NaCl (pH1.2). Positive values of ΔH in the range of 3.83 to 56.13 kJ mol^-1 and positive values of ΔG indicate that the dissolution of the studied glyceryl behenate matrix tablets is an endothermic process which does not proceed spontaneously (in a temperature range of 25 - 45 °C). The negative slope of the linear curves of enthalpy-entropy compensation confirms the entropy-driven dissolution. Practical Applications : A better understanding of the dissolution process is an important aspect, e.g., in the field of drug formulation strategy. In this study, it is confirmed that the influence of temperature on the model drug release rate is negligible for tablets containing more than 40% of glyceryl behenate. It is an important result for drug design due to the reduction of risk of a possible dose dumping effect induced by temperature and the prevention of in vivo therapeutic failure.     

Retrovirus-mediated in vitro gene transfer into chicken male germ line cells

Chicken testicular cells, including spermatogonia, transplanted into the testes of recipient cockerels sterilized by repeated gamma-irradiation repopulate the seminiferous epithelium and resume the exogenous spermatogenesis. This procedure could be used to introduce genetic modifications into the male germ line and generate transgenic chickens. In this study, we present a successful retroviral infection of chicken testicular cells and consequent transduction of the retroviral vector into the sperm of recipient cockerels. A vesicular stomatitis virus glycoprotein G-pseudotyped recombinant retroviral vector, carrying the enhanced green fluorescent protein reporter gene was applied to the short-term culture of dispersed testicular cells. The efficiency of infection and the viability of infected cells were analyzed by flow cytometry. No significant CpG methylation was detected in the infected testicular cells, suggesting that epigenetic silencing events do not play a role at this stage of germ line development. After transplantation into sterilized recipient cockerels, these retrovirus-infected testicular cells restored exogenous spermatogenesis within 9 weeks with approximately the same efficiency as non-infected cells. Transduction of the reporter gene encoding the green fluorescent protein was detected in the sperms of recipient cockerels with restored spermatogenesis. Our data demonstrate that, similarly as in mouse and rat, the transplantation of retrovirus-infected spermatogonia provides an efficient system to introduce genes into the chicken male germ line.     

Evaluation of the Antimicrobial Efficacy of N-Acetyl-l-Cysteine,Rhamnolipids, and Usnic Acid—Novel Approaches to Fight Food-Borne Pathogens

In the food industry, the increasing antimicrobial resistance of food-borne pathogens to conventional sanitizers poses the risk of food contamination and a decrease in product quality and safety. Therefore, we explored alternative antimicrobials N-Acetyl-l-cysteine (NAC), rhamnolipids (RLs), and usnic acid (UA) as a novel approach to prevent biofilm formation and reduce existing biofilms formed by important food-borne pathogens (three strains of Salmonella enterica and two strains of Escherichia coli, Listeria monocytogenes, Staphylococcus aureus). Their effectiveness was evaluated by determining minimum inhibitory concentrations needed for inhibition of bacterial growth, biofilm formation, metabolic activity, and biofilm reduction. Transmission electron microscopy and confocal scanning laser microscopy followed by image analysis were used to visualize and quantify the impact of tested substances on both planktonic and biofilm-associated cells. The in vitro cytotoxicity of the substances was determined as a half-maximal inhibitory concentration in five different cell lines. The results indicate relatively low cytotoxic effects of NAC in comparison to RLs and UA. In addition, NAC inhibited bacterial growth for all strains, while RLs showed overall lower inhibition and UA inhibited only the growth of Gram-positive bacteria. Even though tested substances did not remove the biofilms, NAC represents a promising tool in biofilm prevention.     

Optimal face templates: the next step in surveillance face recognition

Pattern Analysis and Applications - The paper deals with surveillance face recognition in security applications such as surveillance camera systems or access control systems. Presented research is...     

Development and performance evaluation of natural thermal-insulation materials composed of renewable resources

Because energy efficiency in buildings will be evaluated not only based upon heating demand, but also according to the primary energy demand, the ecological properties of the building materials for the whole assessment has become essential. The demand for green building materials is rising sharply, especially insulating materials from renewable resources. The application of natural materials has become increasingly important as a consequence of the increasing need to conserve energy, use natural materials, incorporate architecture and construction into sustainable development processes, and the recently promulgated discussions on appropriate disposal of used insulation materials such as polystyrene (EPS).Due to the fact that natural materials are more sensitive to moisture, decomposition factors such as temperature, material moisture content, attacks by microorganisms, and possible decomposition of the material or shorter durability, it is necessary to evaluate the degradation rate of built-in materials and also determine their real in situ hygrothermal properties according to their moisture content, and volume changes.This paper describes the results of a research project carried out at the Vienna University of Technology and Brno University of Technology. The objective is to use jute, flax, and hemp to develop a new insulating material from renewable resources with comparable building physics and mechanical properties to commonly used insulations materials. All input components are varied in the tests. The impact of moisture content changes in relation to the rate of change of other properties was the focus of the investigation. The tests results show that the correct combination of natural materials is absolutely comparable with convectional materials.     

Using Assumptions to Distribute CTL Model Checking

In this work we discuss the problem of performing distributed CTL model checking by splitting the given state space into several “partial state spaces” . The partial state space is modelled as a Kripke structure with border states. Each computer involved in the distributed computation owns a partial state space and performs a model checking algorithm on this incomplete structure. To be able to proceed, the border states are augmented by assumptions about the truth of formulas and the computers exchange assumptions about relevant states as they compute more precise information. In the paper we give the basic definitions and present the distributed algorithm.     

Characterization of an antioxidant surfactant-free topical formulation containing Castanea sativa leaf extract

Context: Inclusion of antioxidants in topical formulations can contribute to minimize oxidative stress in the skin, which has been associated with photoaging, several dermatosis and cancer.

Objective: A Castanea sativa leaf extract with established antioxidant activity was incorporated into a semisolid surfactant-free formulation. The objective of this study was to perform a comprehensive characterization of this formulation.

Materials and methods: Physical, microbiological and functional stability were evaluated during 6?months storage at 20?°C and 40?°C. Microstructure elucidation (cryo-SEM), in vitro release and in vivo moisturizing effect (Corneometer® CM 825) were also assessed.

Results and discussion: Minor changes were observed in the textural and rheological properties of the formulation when stored at 20?°C for 6?months and the antioxidant activity of the plant extract remained constant throughout the storage period. Microbiological quality was confirmed at the end of the study. Under accelerated conditions, higher modifications of the evaluated parameters were observed. Cryo-SEM analysis revealed the presence of oil droplets dispersed into a gelified external phase. The release rate of the antioxidant compounds (610?±?70?µgh^?0.5) followed Higuchi model. A significant in vivo moisturizing effect was demonstrated, that lasted at least 4?h after product’s application.

Conclusion: The physical, functional and microbiological stability of the antioxidant formulation was established. Specific storage conditions should be recommended considering the influence of temperature on the stability. A skin hydration effect and good skin tolerance were also found which suggests that this preparation can be useful in the prevention or treatment of oxidative stress-mediated dysfunctions.     

Attomole voltammetric determination of metallothionein

Number of authors have concerned with electrochemical analysis of metallothionein. Recently new electroanalytical techniques enabling determination of MT at picomole level has been suggested. The aim of the presented work was to show advantages and disadvantages of the different electrochemical procedures, which are commonly used for the detection of MT—(i) cyclic voltammetry, (ii) differential pulse voltammetry, and (iii) Brdicka reaction. Primarily we aimed on improvement of the mentioned techniques. Using of reducing agent (tris(2-carboxyethyl)phosphine) and combination of the mentioned method with adsorptive transfer stripping technique (AdTS) were the main improvements of the voltammetric method. The detection limits of metallothionein measured by cyclic voltammetry (CV), differential pulse voltammetry (DPV) and DPV Brdicka reaction were 0.5 pmol, 4 fmol and 10 amol, respectively. In addition AdTS DPV Brdicka reaction was used for the determination of metallothionein in human blood serum of 11-year-old girl, which were lead poisoned.