Effect of cyclodextrins on physico-chemical and release properties of Eudragit RS 100 microparticles containing glutathione

The objective of this work was to develop a novel microparticulate system based on the mucoadhesive polymer Eudragit-RS 100 and cyclodextrins (CDs), potentially useful for the oral administration of Glutathione (γ–glutamylcysteinylglycine, GSH). For this purpose, an oil-in-oil (O/O) emulsion-solvent evaporation method was used for the preparation of microparticles (MPs) containing GSH alone or together with one of the following CDs: α-, β-, γ-, methyl-β-(Me-β-), hydroxypropyl-β-(HP-β-) or sulfobutylether-β-cyclodextrin (SBE_7m-β-CD). MPs were obtained by emulsifying a mixture of Eudragit RS 100, GSH, CD and magnesium stearate in acetone or acetonitrile with a mixture of liquid paraffin and Span 80. Size, encapsulation efficiency, and drug release of the prepared MPs were evaluated. The results clearly indicated that all the examined properties were dependent on the water-miscible solvents and CD used. In particular, MPs prepared by using acetone or acetonitrile showed different size distributions with mean diameters in the ranges 82–350 and 15–22 μm, respectively. Moreover, encapsulation efficiency values were found to be high in all cases (71–99%) and was significantly affected by the CD type. The GSH release rates were evaluated employing dissolution media with different pH values (1.2, 6.8 and 7.4) and the following rank order was obtained for MPs prepared using acetone: MPs incorporating Me-β-CD > MPs without CD > MPs incorporating the remaining CDs. On the other hand, MPs prepared using acetonitrile gave the highest GSH release rate. Finally, stability of GSH encapsulated in MPs containing HP-β-CD to enzymatic attack by pepsin A, α-chymotrypsin, and γ-glutamyltranspeptidase was also investigated.     

Application of electrochemical reactors for industrial waste-water treatment

The effectiveness of electrochemical reactors for industrial wastewater treatment has been improved since three-dimensional electrodes have been introduced; in fact, limitations of mass transfer can arise, due to the low concentrations of pollutants which may be involved in the process. Three-dimensional electrodes offer a very high electrode area per unit electrode volume and they can act as turbulence promoters or give rise to high linear electrolyte velocity, resulting in high values of mass transport coefficient. However, careful selection of operative parameters is needed in order to obtain high performance. This paper examines the results obtained in our laboratory on the cathodic reduction of copper at RVC electrodes; in particular the interference of dissolved oxygen is studied during the removal of copper from extremely diluted solutions (C < 10 ppm). Some results are also discussed on the removal of organic pollutants by electrochemical oxidation at three-dimensional anode consisting of a fixed bed of carbon pellets.     

Structural deformation and intertube conductance of crossed carbon nanotube junctions

We present a first-principles study of the structure and quantum electronic conductance of junctions consisting of two crossed (5,5) single-walled carbon nanotubes. The structures are determined by constrained minimization of total energy at a given force between the two tubes, simulating the effects of substrate-tube attraction or an applied force. We find that the intertube contact distance is very sensitive to the applied force in the range of 0--10 nN. The intertube conductance is sizable for realistic deformation expected from substrate interaction. The results explain the recent transport data on crossed nanotubes and show that these systems may be potentially useful as electromechanical devices.     

Chemoenzymatic synthesis of optically active α-methylene-γ-carboxy-γ-lactams and γ-lactones

Three α-methylene-γ-carbomethoxy-γ-butyrolactams (methyl α-methylene-pyroglutamates) 11, 12 and 13, differing in the substitution at the heterocyclic nitrogen, as well as the structurally related γ-lactones 14 and 15 were synthesised and resolved enzymatically by hydrolysis of their ester function, mediated by commercially available hydrolytic enzymes. In particular, the α-chymotrypsin proved to be active to all the substrates examined, displaying a different degree of activity and enantioselectivity, this latter increasing significantly towards the substrate with an aromatic substituent at the nitrogen.     

A note on the extension of BV functions in metric measure spaces

In this note, a classical extension result for BV functions due to Yu.D. Burago and V.G. Maz'ja [Yu.D. Burago, V.G. Maz'ja, Potential Theory and Function Theory for Irregular Regions, Seminars in Math., vol. 3, V.A. Steklov Math. Inst., Leningrad, 1969 (translated from Russian)] is generalized to the abstract setting of doubling metric measure spaces endowed with a differentiation structure called D-structure.     

New phosphorylating reagents for deoxyribonucleosides and oligonucleotides

New phosphorylating reagents 1 and 2 were prepared in three steps from 4-hydroxybenzaldehyde. They showed good efficiency in the solid phase synthesis of 5′-phosphate monoester nucleosides. End-phosphate DNA sequence synthesis demonstrated the efficiency of the new reagents (1 and 2) according to the general procedure of automated DNA synthesis. The oxidation of P(III) to P(V) and the removal of benzyl protecting groups were achieved in a single step by treatment with a 0.02 M I₂/pyridine/H₂O solution. Due to this one-pot treatment, it is possible to use the phosphorylating reagents (1 and 2) for the synthesis of base-sensitive ODNs. The reagents 1 and 2 are unique among phosphorylating reagents.     

The Relevance of the Collaborative Effect in Determining the Performances of Photorefractive Polymer Materials

A derivative of 2‐methylindole, 3‐[2‐(4‐nitrophenyl)ethenyl]‐1‐allyl‐2‐methylindole, NPEMI‐A, is studied for its photoconductivity and photorefractivity behaviour. Its blends with the organic polymer poly‐(2,3‐dimethyl‐N‐vinylindole), PVDMI, are also investigated. Due to the expected and devised mutual solubility of the two components of the blends, it is possible to carry out measurements with the weight percent of the chromophore NPEMI‐A changing from zero to 100. Films were produced by a squeezing process between two ITO‐covered glass sheets. No opacity phenomena, that are so common for many other organic blends due to the segregation of the dissolved chromophore, are observed. The photorefractive optical gain Γ₂ is obtained as a function of the chromophore content. Differential scanning calorimetry measurements (DSC) are also carried out to obtain the whole change of the glass transition temperature T_g as a function of the amount of chromophore contained in the blends. From the experimental trend of T_g a meaningful quantitative estimate of the value of the electrostatic interactions acting in the studied blends, is obtained. The importance of the value of T_g, and of the electrostatic interactions, in determining the extent of the photorefractivity is clearly evident. The results are compared for NPEMI‐A (Γ₂=210 cm^?1) and for NPEMI‐E (Γ₂ ≈ 2000 cm^?1) that has a N‐2‐ethylhexyl group instead of a N‐allyl group. The Pockels and Kerr contributions and—for the first time—a “collaborative effect” of the photorefractivity of NPEMI‐A are distinguished and quantitatively evaluated.