ABSTRACT
The possibility of one-step creating of pH-sensitive mesostructured silica-based nanocontainers with exceptionally high payload using associates of two antiseptics (including hydrolyzable one) as templates is demonstrated. The effects of the template nature and the conditions of the sol-gel process on the porous structure of silica nanocontainers are studied and discussed. The kinetics of the templating drug release from such containers is studied and some features of this process are analyzed. It is shown that the drug release rate can be tuned by varying the medium pH. The bactericidal activity of two encapsulated antiseptics against the Staphylococcus aureus is evaluated in vitro by agar diffusion method with replacement of agar with agarose. The diameters of the inhibition zones for silica-based containers loaded with antiseptics increased with the pre-diffusion time at 4⯰C. At the same time, empty containers (after elimination of antiseptics by etching) did not reveal any bactericidal properties.
Subject(s)
Benzalkonium Compounds/pharmacology , Decamethonium Compounds/pharmacology , Drug Carriers/chemistry , Drug Liberation , Nanoparticles/chemistry , Silicon Dioxide/chemistry , Staphylococcus aureus/drug effects , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/pharmacology , Benzalkonium Compounds/chemistry , Decamethonium Compounds/chemistry , Porosity , Surface PropertiesABSTRACT
The effect of 5 tetracyclines on the barrier and transport properties of the small intestine epithelium was studied. The barrier properties were estimated by a change in the ionic selectivity and conductivity of the epithelium, as well as by enterocyte linkage. The current of the short circuit served the characteristics of the Na transport system state. Dimethylchlortetracycline, methacycline and oxytetracycline in concentrations of 10(-7) g/ml decreased the epithelium conductivity and increased the cell linkage. Tetracycline and methacycline in concentrations of 10(-9) g/ml had an analogous effect. The effect was observed 10--20 minutes after the start of incubation with the substance. No effect on the current of the short circuit was observed within the concentrations of 10(-4) to 10(-9) g/ml. It is suggested that the decreased conductivity and increased linkage are due to adsorption of the tetracycline molecules in the region of close cell contacts.
