ABSTRACT
The focus of solid microneedles technology to date has largely been on cosmetology, vaccination, and insulin delivery, etc. However, limited information is available about the safety of solid polymer microneedles applied in different parts of the human body. In consideration of the different application sites of cosmetology, vaccination, and insulin delivery involved with microneedles technique, factors influencing user acceptance to microneedles including the length and density as well as the size of microneedle patches were systematically investigated by applying different microneedle patches on the forehead, forearm, and abdomen skins of 18 healthy human participants. Multiple insertion tests demonstrated that solid microneedles with a length of 400 µm, a density of 100 MN/cm2, and an array size of 10 × 10 were optimal for forehead pretreatment. Microneedles with lengths of 400 and 600 µm, densities of 49 and 100 MN/cm2, and an array size of 10 × 10 caused less pain and slight skin irritation in the forearm, whereas 400 µm height, 49 and 100 MNs/cm2 densities, and 5 × 5, 10 × 10, and 10 × 20 arrays of the solid microneedles were not considered painful and were well-tolerated in abdomen insertion. In conclusion, the optimization of the dimensions of microneedles according to application sites could improve medication compliance and the safety of clinical use of solid microneedles.
ABSTRACT
A series of metronidazole-thiazole derivatives has been designed, synthesized and evaluated as potential antibacterial inhibitors. All the synthesized compounds were determined by elemental analysis, 1H NMR and MS. They were also tested for antibacterial activity against Escherichia coli, Bacillus thuringiensis, Bacillus subtilis and Pseudomonas aeruginosa as well as for the inhibition to FabH. The results showed that compound 5e exhibited the most potent inhibitory activity against E. coli FabH with IC50 of 4.9µM. Molecular modeling simulation studies were performed in order to predict the biological activity of proposed compounds. Toxicity assay of compounds 5a, 5b, 5d, 5e, 5g and 5i showed that they were noncytotoxic against human macrophage. The results revealed that these compounds offered remarkable viability.
ABSTRACT
A series of metronidazolethiazole derivatives has been designed, synthesized and evaluated as potential antibacterial inhibitors. All the synthesized compounds were determined by elemental analysis, (1)H NMR and MS. They were also tested for antibacterial activity against Escherichia coli, Bacillus thuringiensis, Bacillus subtilis and Pseudomonas aeruginosa as well as for the inhibition to FabH. The results showed that compound 5 e exhibited the most potent inhibitory activity against E. coli FabH with IC50 of 4.9 lM. Molecular modeling simulation studies were performed in order to predict the biological activity of proposed compounds. Toxicity assay of compounds 5 a, 5 b, 5 d, 5 e, 5 g and 5 i showed that they were noncytotoxic against human macrophage. The results revealed that these compounds offered remarkable viability.
