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1.
Metallomics ; 3(10): 1041-8, 2011 Oct.
Article in English | MEDLINE | ID: mdl-21833405

ABSTRACT

The aim of this study was to radiolabel ciprofloxacin (Cip) and nitrofuryl thiosemicarbazone (NFT) with the fac-[(99m)Tc(CO)(3)(H(2)O)(3)](+) core and to evaluate the ability of the radiopharmaceuticals as tracers in detecting sites of infection. Cip and NFT were radiolabeled with the fac-[(99m)Tc(CO)(3)(H(2)O)(3)](+) core and characterized by RHPLC. The stabilities of the preparations were evaluated in saline and rat serum. In vitro binding studies of the radiopharmaceuticals with S. aureus were performed. Biodistribution studies were conducted at different time points after injecting (i.v.) the radiopharmaceuticals in rats (intramuscularly infected with S. aureus) as well as in rats with sterile inflammation. To assess the infection targeting capacity of (99m)Tc-tricarbonyl ciprofloxacin and nitrofuryl thiosemicarbazone, (99m)Tc(v)O-Cip and (99m)Tc(v)O-NFT were used as control. Scintigraphic imaging studies of tricarbonyl compounds and (99m)Tc(v)O-Cip were performed at 4 h after injection. The radiochemical purities of (99m)Tc(CO)(3)-Cip and (99m)Tc(CO)(3)-NFT were between 97-98% as determined by thin layer chromatography (TLRC) and RHPLC; no further purification is necessary before injection. The radiopharmaceuticals exhibited substantial stability when incubated in isotonic saline and serum up to 24 h. Biodistribution studies showed maximum uptake in the infected rat thigh muscle at 4 h post injection and washing out at slower rate from the infected site than the oxo technetium chelate. The mean ratios of uptake in infected/non-infected thighs were 3.87:1, 3.41:1 and 3.17:1 for (99m)Tc(CO)(3)-Cip, (99m)Tc(CO)(3)-NFT and (99m)Tc(v)O-Cip respectively. During scintigraphic studies, infection sites appeared quite distinctly with (99m)Tc(CO)(3)-Cip and (99m)Tc(CO)(3)-NFT, comparable to the behaviour with (99m)Tc(v)O-Cip. These results encouraged us for further development of infection imaging radiopharmaceuticals based on the (99m)Tc-tricarbonyl core.


Subject(s)
Ciprofloxacin , Radiopharmaceuticals , Staphylococcal Infections/diagnostic imaging , Technetium , Thiosemicarbazones , Animals , Ciprofloxacin/chemistry , Ciprofloxacin/metabolism , Radionuclide Imaging , Radiopharmaceuticals/chemistry , Radiopharmaceuticals/metabolism , Rats , Rats, Sprague-Dawley , Staphylococcal Infections/diagnosis , Staphylococcus aureus/isolation & purification , Staphylococcus aureus/metabolism , Technetium/chemistry , Technetium/metabolism , Thiosemicarbazones/chemistry , Thiosemicarbazones/metabolism
2.
Pharmazie ; 64(7): 445-9, 2009 Jul.
Article in English | MEDLINE | ID: mdl-19694181

ABSTRACT

The objectives of our study were to prepare a biodegradable nanoparticulate system of chloramphenicol (CHL) and to evaluate its ability to prolong in vitro release of CHL compared to free drug suspension (FDS). CHL-loaded polylactide-co-glycolide nanoparticles (CHL-PLGA-NPs) were prepared by an emulsion/solvent evaporation method using ethyl acetate and polyvinyl alcohol. CHL-PLGA-NPs were characterized by particle size, zeta potential, infrared spectra, drug entrapment efficiency and in vitro release kinetics measurement. Sonication was done with an ultrasound pulse sonicator at 70 W, 30 kHz for 60 s to produce stable NPs of mean size range from 277 nm to 433 nm. Drug to polymer ratio (D:P) was selected as formulation variable and significantly influenced entrapment efficiency (approximately 30% to 66%) and release (p < 0.05). Entrapment of CHL in biodegradable NPs significantly prolonged drug release compared to FDS and thus implies potential antibiotic delivery system for ocular application.


Subject(s)
Anti-Bacterial Agents/administration & dosage , Chloramphenicol/administration & dosage , Anti-Bacterial Agents/chemistry , Biotransformation , Chemistry, Physical , Chloramphenicol/chemistry , Delayed-Action Preparations , Diffusion , Emulsions , Microscopy, Electron, Scanning , Nanoparticles , Solvents , Spectrophotometry, Infrared , Spectroscopy, Fourier Transform Infrared
3.
Phys Rev Lett ; 100(6): 067204, 2008 Feb 15.
Article in English | MEDLINE | ID: mdl-18352508

ABSTRACT

The electronic structure of a prototype dilute magnetic semiconductor (DMS), Ga(1-x)MnxAs, is studied by magnetic circular dichroism (MCD) spectroscopy. We prove that the optical transitions originated from impurity bands cause the strong positive MCD background. The MCD signal due to the E0 transition from the valence band to the conduction band is negative indicating that the p-d exchange interactions between the p carriers and d spin is antiferromagnetic. The negative E0 MCD signal also indicates that the hole doping of the valence band is not so large as previously assumed. The impurity bands seem to play important roles for the ferromagnetism of Ga(1-x)MnxAs.

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