muramidase and hydroxyethylcellulose

The aim of this study was the design of novel S-protected thiolated hydroxyethyl cellulose (HEC) and the assessment of its mucoadhesive properties and biodegradability compared to the corresponding unmodified polymer. Thiolated HEC was S-protected via disulfide bond formation between 6-mercaptonicotinamide (6-MNA) and the thiol substructures of the polymer. In vitro screening of mucoadhesive properties was accomplished using two different methods: rotating cylinder studies and viscosity measurements. Moreover, biodegradability of these polymers by cellulase, xylanase and lysozyme was evaluated. MTT and LDH assays were performed on Caco-2 cells to determine the cytotoxicity of S-protected thiolated HEC. Thiolated HEC displayed 280.09±1.70μmol of free thiol groups per gram polymer. S-protected thiolated HEC exhibiting 270.8±21.11μmol immobilized 6-MNA ligands per gram of polymer was shown being 2.4-fold more mucoadhesive compared to thiolated HEC. No mucoadhesion was observed in case of unmodified HEC. Results were in a good agreement with rheological studies. The presence of free thiol moieties likely caused lower degree of hydrolysis by xylanase, whereas the degradation by both enzymes cellulase and xylanase was more hampered when 6-MNA was introduced as ligand for thiol group's protection. Findings in cell viability revealed that all three conjugates were non-toxic. S-protection of thiolated hydroxyethyl cellulose improved mucoadhesive properties and provided pronounced stability towards enzymatic attack, that makes this excipient superior for non-invasive drug administration over thiolated and unmodified forms.

Topics: Adhesiveness; Animals; Caco-2 Cells; Cellulose; Cysteamine; Drug Stability; Excipients; Glycoside Hydrolases; Humans; Intestinal Mucosa; Muramidase; Niacinamide; Rheology; Sulfhydryl Compounds; Swine

To investigate the effect of saliva substitutes on enamel erosion in vitro.. A total of 204 bovine enamel samples were embedded in acrylic resin and allocated to 17 groups (n=12). The specimens were eroded in an artificial mouth (3 days; 6×30 s/days, flow rate: 2 ml/min) using citric acid (pH: 2.5). Immediately after the erosive attacks, saliva substitutes (12 sprays, 3 gels) were applied. Between the erosive cycles the specimens were rinsed with artificial saliva (flowrate: 0.5 ml/min). A SnCl2/AmF/NaF-containing mouthrinse was used as positive control, water spray served as negative control. Enamel loss was measured profilometrically and the data were analyzed using one-way ANOVA followed by Scheffé's post hoc tests (p<0.05).. Four saliva substitutes increased enamel erosion, probably due to the low pH or the content of citric acid. Several saliva substitutes were able to reduce enamel erosion significantly by 60-90% (in the range of the positive control). The protective potential of these products was in the range of the positive control (reduction of enamel loss to 30% of negative control). The erosion-protective potential of these high-viscous products is probably related to their film-forming properties, leading to a mechanical protection of the surface.. Saliva substitutes containing a very low pH exhibit a distinct erosive potential, while most high-viscous products present an erosion-protective effect. It can be recommended that patients suffering from xerostomia and at high risk for dental erosion should use high-viscous saliva substitutes, but should avoid saliva substitutes with low pH or containing citric acid.. It can be recommended that patients suffering from xerostomia and at high risk for dental erosion should use high-viscous saliva substitutes, but should avoid saliva substitutes with low pH or containing citric acid.

Topics: Aerosols; Animals; Cattle; Cellulose; Citric Acid; Dental Enamel; Diamines; Drug Combinations; Fluorides; Gels; Glucose Oxidase; Hydrogen-Ion Concentration; Lactoperoxidase; Materials Testing; Mouthwashes; Muramidase; Protective Agents; Saliva, Artificial; Sodium Fluoride; Tin Compounds; Tooth Demineralization; Tooth Erosion; Tooth Remineralization; Viscosity

Surface-modified flat-sheet microfiltration membranes were functionalised with poly-L-lysine, polymyxin B, poly(ethyleneimine), L-histidine, histamine, alpha-amylase and DEAE as well as deoxycholate. Their suitability to remove endotoxin from both buffers and protein solutions was examined using bovine serum albumin, murine IgG1 and lysozyme as model proteins. In protein-free solutions reduction from 6000 EU/ml to <0.1 EU/ml was achieved with all applied ligands; only alpha-amylase as well as L-histidine and histamine, when immobilized via the non-ionic spacer bisoxirane, exhibited low clearance factors at neutral pH. The adsorption of endotoxin is mainly ruled by electrostatic interaction forces. Thus in multi-component systems, such as endotoxin-contaminated protein solutions, competing interactions take place: acidic proteins compete with endotoxin for binding sites at the membrane adsorbers, basic proteins compete with the ligands for endotoxin and act as endotoxin carriers. With properly chosen conditions the membrane adsorbers presented here show exceptional effectiveness also in the presence of proteins. They are generally superior to functionalised Sepharose chromatographic sorbents and allow fast processing. They may contribute to reduce the risks in the application of parenterals and diagnostics.

Topics: Adsorption; Animals; Cattle; Cellulose; Dextrans; Drug Contamination; Endotoxins; Hydrogen-Ion Concentration; Ligands; Membranes, Artificial; Muramidase; Nylons; Polyvinyl Alcohol; Serum Albumin; Solutions