Taste masking of enalapril maleate by microencapsulation in Eudragit EPO® microparticles.

Microencapsulation is one of the most commonly used taste masking techniques. It can be accomplished by various methods, including coacervation, solvent evaporation, extrusion and spray-drying. Enalapril maleate, a bitter-tasting ACE-inhibitor, is available worldwide in conventional tablet formulations and as oral solution in the USA. The purpose of this study was to develop enalapril-loaded microparticles using spray-drying and to test their taste masking potential. Eudragit EPO® was used as a taste masking polymer for the preparation of a drugpolymer suspension. The suspension was then spray-dried under the following conditions: inlet temperature 65 °C, outlet temperature 30 °C, aspiration 100% and pump rate 10%. The drug-to-polymer ratio was varied and seven different microparticle models were developed. The yield of spray-dried particles ranged from of 51.3 to 85.4%, drug loading varied from 7.75 to 24.69% and encapsulation efficiency ranged from 58.5 to 95.7%. The particle size varied between 5.00 µm and 17.47 µm and the moisture content varied between 7.1% and 10.3%. In vitro taste assessment revealed minimal or no ENA release in artificial saliva. In vivo studies (with experimental animals and healthy volunteers) were used to evaluate the taste masking potential of spray-dried microparticles of enalapril maleate and Eudragit EPO®.

Activation of KCNQ channels located on the skeletal muscle membrane by retigabine and its influence on the maximal muscle force in rat muscle strips.

Retigabine is a new antiepileptic drug with the main mechanism of action: activation of voltage-gated potassium channels (Kv7) represented in many tissues including the excitable cells-neuronal and muscular. The aim of this article is to determine the role of potassium channels located on the skeletal muscle membrane in the in vivo and in vitro reduction of muscle contractile activity induced by retigabine. We studied the effects of retigabine on the motor function in vivo using a bar holding test and exploratory activity using open field test in rats. Electrical field stimulation (EFS) was applied to skeletal muscle strips in vitro in order to evaluate muscular activity. We registered a significant decrease in the muscle tone and exploratory activity of rats, treated orally with 60 mg/kg bw retigabine. In vitro experiments showed decrease in the maximal muscle force of strips in the presence of retigabine in the medium after both indirect (nerve-like) and direct (muscle-like) stimulation. The effects were fully antagonized by XE-991 (Kv7 channel blocker), which supports our hypothesis about the relation between these types of potassium channels and the observed change in the muscle force. Based on these results, we can conclude that skeletal muscle Kv7 channels play a significant role in the myorelaxation and reduced muscle force registered after treatment with Kv7 channels openers (e.g., retigabine). The hyperpolarization of skeletal muscle membrane caused by accelerated K(+) efflux may be the underlying cause for the effect of retigabine on the muscle tone.

Effect of modification of light-harvesting complex II on fluorescence properties of thylakoid membranes of Arabidopsis thaliana.

The 77 K chlorophyll fluorescence spectra of Arabidopsis thaliana mutants deficient in lipid fatty acid desaturation have been used in order to further explore the influence of the modification of LHC II after mutation and proteolitic treatment on the energy transfer between the chlorophyll-protein complexes, as well as on the structure-function relationship in the supramolecular complex of Photosystem II. The gaussian decomposition and analysis of the fluorescence bands associated with PS II complex show the controversial action of the trypsin in the investigated thylakoid membranes. This reveals that the organization of PS II complexes is different in the wild type and both mutants indicating altered connection between the LHC II and the RC core complexes of PS II in both mutants. The results obtained demonstrate that different amounts of oligomer and monomer forms of LHC II in the mutants (LK3 and JB67), arising from lipid modification, are responsible for different proteolytic action in their thylakoid membranes.

Electric properties of thylakoid membranes from pea mutants with modified carotenoid and chlorophyll-protein complex composition.

Surface electric properties of thylakoid membranes from wild type and two mutant forms, Coeruleovireus 2/16 and Costata 2/133, of pea are investigated by electric light scattering and microelectrophoretic measurements. Characterization of the chlorophyll-protein complexes in thylakoid membranes reveals that the relative ratio of oligomeric (LHC II(1)) to monomeric (LHC II(3)) forms of the light-harvesting Chl a/b complex of Photosystem II is lower (3.34) in 2/133 mutant and higher (6.62) in 2/16 mutant than in wild type (4.57). This is accompanied by elevated amounts and a considerable reduction of all carotenoids in 2/16 and 2/133 mutant, respectively, as compared to the wild type. The concomitant variations of the permanent dipole moment (transversal charge asymmetry), electric polarizability and electrokinetic charge of the thylakoid membranes from both the mutants are discussed in terms of the differences in the supramolecular (oligomeric) organization of the light-harvesting complexes II within the photosynthetic apparatus.

Surface electric properties of thylakoid membranes from Arabidopsis thaliana mutants.

Electric light scattering measurements of thylakoid membranes from wild type and two mutant forms (JB67 and LK3) of Arabidopsis thaliana have shown that application of external electric pulses induces electric dipole moments of different origin. The asymmetric surface charge distribution and electric polarizability are significantly altered by the lipid modification. Mild trypsin treatment of Arabidopsis thylakoids leading to digestion of small polypeptides from the light-harvesting chlorophyll a/b protein complex of photosystem II (LHCP II) gives evidence for a lower content of LHCP II in the mutant forms. The results demonstrate the significance of the level of thylakoid lipid unsaturation in determining the surface charge distribution through changes either in the pigment-protein content and membrane appression induced by the lipid modification or in the exposure of charged polypeptides on the thylakoid membrane surface(s) arising from alteration of the lipid geometry.