Medicated Straws Based on Electrospun Solid Dispersions

Novel medicated straws were developed based on drug-loaded electrospun fibers prepared by direct current electrospinning (DCES) and high-speed electrospinning (HSES) of scaled-up productivity. Good quality micro- and nanofibers were electrospun using both techniques despite the multiple times higher throughput rate of HSES based on the scanning electron microscopic imaging (SEM). Solid state analyses revealed that the poorly soluble model drug carvedilol (CAR) was dispersed in an amorphous form in the electrospun polyvinylpyrrolidone (PVPK30) fibers. In vitro dissolution studies revealed ultrafast drug release from the prepared fibrous formulations inserted into plastic straws. Based on the results the developed drug delivery system is suitable for storing the formulation in a solid dosage form and in situ turning it into liquid form when administered

Detailed cytotoxicity assessment of the formulated herbicide roundup classic and its constituents

Cytotoxicity of the globally market-leading herbicide ROUNDUP CLASSIC formulation and its components such as the active ingredient glyphosate and the formulating agent POEA (a mixture of polyethoxylated tallow amines) were investigated on the murine neuroectodermal stem cell-like (NE-4C) and osteoblastic (MC3T3-E1) cell lines. The cytotoxic and genotoxic effects on cell viability and cell cycles were evaluated based on the results of flow cytometry, enzymatic-assays, and alkaline single cell gel electrophoresis (Comet) assays, furthermore, the effects on cell morphology and dynamic mass redistribution of cellular contents were assessed with the use of the label-free Epic BenchTop optical biosensor on MC3T3-E1 cells adhered on the surface of the biosensor. Differences in the sensitivity of the investigated cell lines were detected, while the MC3T3-E1 cell line indicated less sensitivity to the effects of the treatments. Furthermore, differences were also observed in the sensitivity of the performed assays. The order of the inhibitory potency of the investigated compounds was as follows: glyphosate IPA salt << ROUNDUP CLASSIC < POEA. The applied Epic technique provides an effective tool for the real-time detection of cytotoxicity

Green tea polyphenol tailors cell adhesivity of RGD displaying surfaces: multicomponent models monitored optically

The interaction of the anti-adhesive coating, poly(L-lysine)-graft-poly(ethylene glycol) (PLL-g-PEG) and its Arg-Gly-Asp (RGD) functionalized form, PLL-g-PEG-RGD, with the green tea polyphenol, epigallocatechin-gallate (EGCg) was in situ monitored. After, the kinetics of cellular adhesion on the EGCg exposed coatings were recorded in real-time. The employed plate-based waveguide biosensor is applicable to monitor small molecule binding and sensitive to sub-nanometer scale changes in cell membrane position and cell mass distribution; while detecting the signals of thousands of adhering cells. The combination of this remarkable sensitivity and throughput opens up new avenues in testing complicated models of cell-surface interactions. The systematic studies revealed that, despite the reported excellent antifouling properties of the coatings, EGCg strongly interacted with them, and affected their cell adhesivity in a concentration dependent manner. Moreover, the differences between the effects of the fresh and oxidized EGCg solutions were first demonstrated. Using a semiempirical quantumchemical method we showed that EGCg binds to the PEG chains of PLL-g-PEG-RGD and effectively blocks the RGD sites by hydrogen bonds. The calculations supported the experimental finding that the binding is stronger for the oxidative products. Our work lead to a new model of polyphenol action on cell adhesion ligand accessibility and matrix rigidity

A newly identified specific biological activity of glyphosate - inhibition of RGD-binding integrins

In this study we investigated the inhibitory effect of the widely used broad-spectrum herbicide active ingredient glyphosate and its related analogues on αVβ3 integrin binding to the shortest oligopeptide recognizing motif of integrins, the arginine-glycine-aspartic acid (RGD) sequence. Integrin binding characteristics were assessed in a modified enzyme linked immunosorbent assay (ELISA) and by a label-free optical biosensor technique. At 22 mM, glyphosate reached full inhibition of αVβ3, and the inhibitory activity of its main metabolite, aminomethylphosphonic acid (AMPA) was also above 95%, while another environmentally relevant metabolite, sarcosine exerted only a weaker effect, approximately 35% inhibition. In turn, the half maximal inhibitory concentration (IC50) of glyphosate and AMPA were reported to be 2.7±0.5 mM and 1.3±0.2 mM, respectively. The inhibitory effects of the other related compounds investigated (acetylglycine, glycine and iminodiacetic acid) at the same concentration, 22 mM were below 50%. Inhibitory effects on cell adhesion to RGD-modified surfaces by whole cells containing several types of RGD-binding integrins including αVβ3 were detected using the biosensor technique, where the integrin antagonist activity of glyphosate was also demonstrated

Ubiquiter circovirus sequences raise challenges in laboratory diagnosis: The case of honey bee and bee mite, reptiles, and free living amoebae

Circoviruses of pigs and birds are established pathogens, however, the exact role of other, recently described circoviruses and circovirus-like viruses remains to be elucidated. The aim of this study was the detection of circoviruses in neglected host species, including honey bees, exotic reptiles and free-living amoebae by widely used broad-spectrum polymerase chain reaction (PCR) assays specific for the replication initiation protein coding gene of these viruses. The majority of sequences obtained from honey bees were highly similar to canine and porcine circoviruses, or, were distantly related to dragonfly cycloviruses. Other rep sequences detected in some honey bees, reptiles and amoebae showed similarities to various rep sequences deposited in the GenBank. Back-to-back PCR primers designed for the amplification of whole viral genomes failed to work that suggested the existence of integrated rep-like elements in many samples. Rolling circle amplification and exonuclease treatment confirmed the absence of small circular DNA genomes in the specimens analysed. In case of honey bees Varroa mite DNA contamination might be a source of the identified endogenous rep-like elements. The reptile and amoebae rep-like sequences were nearly identical with each other and with sequences detected in chimpanzee feces raising the possibility that detection of novel or unusual rep-like elements in some host species might originate from the microbial community of the host. Our results indicate that attention is needed when broad-spectrum rep gene specific polymerase chain reaction is chosen for laboratory diagnosis of circovirus infections