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  • Author or Editor: Muhammad Khan x
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Abstract  

The solvent extraction of thorium(IV) (4.3·10–4M) from nitric acid solution by bis-2-(butoxyethyl ether) (butex or DBC) has been studied. It has been investigated as a function of nitric acid, extractant and metal ion concentration. The effect of equilibration time, diverse ions and salting-out agent on the extraction has also been examined. Among anions, fluoride, phosphate, oxalate and perchlorate have reduced the extraction. Cations such as Na(I), K(I), Ca(II), Zn(II), Al(III), Ti(IV), Zr(IV) except Sr(II) and Pb(II) do not interfere in the extraction. The extraction is enhanced upto 97% in three stages at 6M HNO3 having 2.94M NaNO3 as salting-out agent. The extraction is found to be independent of thorium concentration in the range studied (4.3·10–4–4.3·10–2M). The temperature (18–45°C) has an adverse effect on the extraction. A 1% solution of ammonium bifluoride is found to be a good stripping solution and recovery of thorium is >98%.

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The radiolabeling of trovafloxacin dithiocarbamate (TVND) with technetium-99m using [99mTc-N]2+ core was investigated and biologically assessed as prospective infection imaging agent. The achievability of the 99mTcN-TVND complex as a future MRSA infection radiotracer was investigated in artificially methicillin-resistant Staphylococcus aureus (MRSA) infected male Sprague–Dawley rats (MSDR). Radiochemically the 99mTcN-TVND complex was characterized in terms of radiochemical purity (RCP) in saline, in vitro permanence in serum, in vitro binding with MRSA and biodistribution in living and heat killed MRSA infected MSDR. Radiochemically the complex showed stability in saline with a 97.90 ± 0.22% yield and serum at 37 °C up to 4 h. The 99mTcN-TVND complex showed saturated in vitro binding with MRSA. Normal in vivo uptake in the MRSA infected MDRS was observed with a five fold uptake in the infected muscle as compared to inflamed and normal muscles. The high RCP values, in vitro permanence in serum, better in vitro binding with MRSA, biodistribution behavior and the target to non-target (infected to inflamed muscle) ratios posed the 99mTcN-TVND complex as a promising MRSA infection radiotracer.

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Abstract  

99mTc–rufloxacin (99mTc–RUN) complex was prepared by reaction of different amounts of reduced sodium pertechnetate with different amount of Rufloxacin (RUN) antibiotic for the in vivo scintigraphic localization of the Staphylococcus aureus (S. aureus) infectious foci in Male Wister Rats (MWR) model. The 99mTc–RUN complex was radiochemically and biologically characterized in terms of radiochemical stability in saline, serum, in vitro binding with S. aureus and biodistribution in artificially infected with S. aureus MWR. The 99mTc–RUN complex showed stability more than 90% up to 240 min in normal saline with a maximum stability value of 98.10 ± 0.18% at 30 min after reconstitution. At 37 °C the complex showed in vitro permanence in serum up to 16 h with 13.90% side products during incubation. The 99mTc–RUN complex showed saturated in vitro binding with S. aureus at different intervals with a maximum uptake value of 71.50%. Infected to normal muscle, infected to inflamed and inflamed to normal muscles ratios were approximately 6.04, 4.31 and 1.40. Based on the stability of the complex in saline, serum, in vitro binding with S. aureus and biodistribution results, the 99mTc–RUN complex is recommended for in vivo scintigraphic localization of the S. aureus in vivo infectious foci in human.

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Abstract  

In the current investigation radiosynthesis of the 99mTc-trovafloxacin (99mTc-TVN) complex and its biodistribution in male Wistar rats (MWR) artificially infected with live and heat killed methicillin resistant Staphylococcus aureus (MRSA) was studied. Further the complex was evaluated in terms of the radiochemical stability in normal saline, in vitro stability in serum and in vitro binding with MRSA. The complex showed radiochemical purity (RCP) in normal saline with a maximum value of 97.30 ± 0.52% at 30 min after its reconstitution. The RCP value went down to 90.45 ± 0.48% within 4 h. In serum at 37 °C, the complex showed permanence up to 4 h but within 16 h of incubation the production of undesirable side product of 17.25% (free and radio-colloid) was observed. In buffer the labeled TVN showed saturated in vitro binding with live MRSA. The uptake of the complex in the thigh of the MWR infected with live MRSA was almost five fold than those infected with heat killed MRSA. The high RCP values, in vitro stability in serum, saturated in vitro binding with MRSA and promising biodistribution with six fold higher accumulation in the infected organ of the MWR infected with live MRSA established the usefulness of the 99mTc-TVN as a promising MRSA infection radiotracer.

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Abstract  

In the present study synthesis of the 99mTc–CNN complex and its efficacy as a prospective Staphylococcus aureus (S. aureus) infection imaging agent was assessed. The 99mTc–CNN complex was characterized in terms of stability in saline, serum, in vitro binding with S. aureus and in vivo percent absorption in male Wister rats (MWR) infected with live and heat killed S. aureus. Radiochemically the 99mTc–CNN complex showed stable behavior in saline and serum at different intervals. At 30 min after reconstitution the complex showed maximum radiochemical purity (RCP) yield of 97.55 ± 0.22%. The RCP yield decreased to 90.50 ± 0.18% within 240 min. In serum, 18.15% unwanted side product was appeared within 16 h of the incubation. In vitro saturated binding with S. aureus was observed at different intervals with a 62.00% maximum at 90 min. Normal percent in vivo uptake was observed in MWR artificially infected with live S. aureus with a five times higher in the infected muscle as compared to the inflamed and normal muscles. No difference in the percent uptake of the complex in MWR infected with heat killed S. aureus in the infected, inflamed and normal muscles were observed. Based on the promising in vitro and in vivo radiochemical and biological characteristics, we recommend the 99mTc–CNN complex for in vivo localization of the S. aureus infectious foci.

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Abstract  

In the current investigation the complexation of derivatized temafloxacin with 99mTc using [99mTc(CO)3(H2O)3]+ precursor was assessed. The tricarbonyl complex of the temafloxacin dithiocarbamate (99mTc(CO)3-TAND) was characterized in terms of radiochemical purity (RCP) yield in saline, in vitro radiochemical stability in serum, in vitro binding with Streptococci pneumoniae and biodistribution in male Wister rats (MWR) artificially infected with living and heat killed Streptococci pneumoniae. The 99mTc(CO)3-TAND complex showed 98.10 ± 15% RCP value at 30 min of the reconstitution and remained more than 90% stable up to 120 min in normal saline at room temperature. In serum a stable behavior with the appearance of 15.30% unwanted side product up to 16 h of incubation was observed. A saturated in vitro binding with Streptococci pneumoniae was observed. The complex showed almost six times higher uptake in the infected muscle as compared to the inflamed and normal muscles of the MWR infected with living Streptococci pneumoniae. Insignificant difference in the uptake of the tracer in the infected, inflamed and normal muscles of the MWR infected with heat killed Streptococci pneumoniae was noted. Based on the elevated RCP in saline, in vitro stability in serum at 37 °C, saturated in vitro binding with pathogens and better biodistribution behavior with higher accumulation of the tracer in target organs confirmed the suitability of the 99mTc(CO)3-TAND complex as promising infection radiotracer.

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Abstract  

Synthesis of the 99mTc(CO)3–trovafloxacin dithiocarbamate (99mTc(CO)3–TVND) complex and biological characterization in artificially Staphylococcus aureus (S. aureus) infected rats model was assessed. The suitability of the complex was evaluated and compared with 99mTcN–TVND, in terms of radiochemical immovability in saline, in vitro permanence in serum, in vitro binding with S. aureus and biodistribution in Male Sprague-Dawley rats (MSDR). After 30 min of the reconstitution both the complexes showed maximum radiochemical stabilities in saline and remain more than 90% stable up to 120 min. However the 99mTc(CO)3–TVND showed to some extent higher stability than 99mTcN–TVND complex. In serum 1.75% less de-tagging was observed than 99mTcN–TVND complex. Both the complexes showed saturated in vitro binding with S. aureus and no significant difference were observed between the uptakes. Six fold uptakes were noted in the infected muscle as compared to the inflamed and normal muscles of the MDSR. The uptake of the 99mTc(CO)3–TVND in infected muscle of the MSDR was 2.25% high as compared to the 99mTcN–TVND complex. Based on radiochemical stabilities in saline, serum, in vitro binding with MRSA and significantly higher uptake in the infected muscle, we recommend both the complexes for in vivo investigation of the MRSA infection in human.

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Abstract  

In the current study radio complexation of the moxifloxacin dithiocarbamate (MXND) with technetium-99m (99mTc) using the [99mTc–N]2+ core through legend exchange reaction was explored. The 99mTcN–MXND complex was biologically evaluated as a potential radiopharmaceutical for in vivo scintigraphy using artificially infected male sprague–dawley rats (MSDR) with Staphylococcus aureus (S. aureus). The radiochemistry of the complex was explored in terms of radiochemical purity (RCP), in vitro stability in serum at 37 °C for 16 h, in vitro binding with S. aureus and biodistribution in artificially infected with S. aureus MSDR. It was observed that the complex showed stability of more than 90% up to 4 h after reconstitution with a maximum RCP value of 97.55 ± 0.42% at 30 min. The complex showed significantly in vitro stability in serum at 37 °C with an insignificant free species up to 16.50% within 16 h. In vitro saturated binding with S. aureus was noted up to 120 min with maximum value of 73.25% at 90 min of incubation. Almost sixfold uptake was noted in the infected muscle of the MSDR as compared to inflamed and normal muscle. The 97.55 ± 0.42% RCP values, stability in serum with insignificant untagged 16.50% species, 73.25% in vitro binding with S. aureus and sixfold uptake in the target organ posed the 99mTcN–MXND complex as a promising radiopharmaceutical for S. aureus infectious foci.

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Abstract  

In the current investigation tosufloxacin (TSN) was derivatized to its dithiocarbamate (TSND) derivative and its radiolabeling with technetium-99m using [99mTc(CO)3(H2O)3]+ precursor. The labeled TSND (99mTc(CO)3-TSND) was radiochemically characterized in saline and serum and biologically its in vitro binding with Proteus mirabilis (P. mirabilis) and biodistribution in male Wister rats (MWR) artificially infected with live and heat killed P. mirabilis. Radiochemically a stable radio-tricarbonyl TSND complex was observed with a maximum stability of 98.15 ± 0.32% and it remained more than 90% up to 4 h after reconstitution. The stability decreased to 91.00 ± 0.30% from 98.15 ± 0.32% within 4 h. In serum at 37 °C the growth of some unwanted side product decreased the stability by 15.65% within 16 h. The complex showed saturated in vitro binding with P. mirabilis up to 78.50% (90 min). In MWR infected with live P. mirabilis the percent (%) uptake of the complex in blood, liver, spleen, stomach, intestines and kidneys were almost similar to the MWR infected with heat killed. However, the % accumulation of the complex in the infected muscle was six times higher than in the inflamed and normal muscle in MWR infected with live P. mirabilis. On the basis of immovability of the 99mTc(CO)3-TSND complex in normal saline, in vitro permanence in serum, saturated in vitro binding with P. mirabilis and six fold uptake in the infected muscle of the MWR infected with live P. mirabilis as compared to the normal muscle, the suitability of the 99mTc(CO)3-TSND complex is established as a promising infection radiotracer.

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Abstract  

In the current investigation complexation of the gemifloxacin (GIN) with technetium-99 m (99mTc) and its biological evaluation in artificially Streptococcus pneumoniae (S. pneumoniae) infected rats was assessed as potential S. pneumoniae infection radiotracer. Radiochemically the 99mTc-GIN complex was further analyzed in terms of stability in saline, in vitro stability in serum at 37 °C, in vitro binding with S. pneumoniae and biodistribution in artificially S. pneumoniae (living and heat killed) infected rats. The complex was found 97.25 ± 0.25% radiochemically stable in saline at 30 min after reconstitution. The stability of the 99mTc-GIN complex was decreased to 90.50 ± 0.20% within 240 min after reconstitution. In serum the 99mTc-GIN complex showed stable profile with the appearance of 18.85% free tracer within 16 h of incubation. The 99mTc-GIN complex showed saturated in vitro binding with S. pneumoniae after different intervals. Almost five fold uptake was observed in living S. pneumoniae infected muscle of the rats as compared to the inflamed and normal muscle. No significant difference in the uptake of heat killed S. pneumoniae infected, inflamed and normal muscles of the rats. The high RCP yield in saline, in vitro permanence in serum, in vitro binding with living S. pneumoniae and biodistribution in artificially S. pneumoniae infected rats we recommend the 99mTc-GIN as potential S. pneumoniae infection radiotracer.

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