The Radiosynthesis Of ¹⁸⁸Re Labelled Stannic Sulfur Solloid And Its Biodistribution In Animals With Tumor

Partâ… : Investigations of Labeling Stannic Sulfur Colloid With Rhenium-¹⁸⁸Objective To investigate the method of labeling stannic sulfur colloid with rhenium-¹⁸⁸, study its stability and size of radioactive colloid.Methods 1 Iabeling with commercial drug kit (SC kit, used for research): (1) The preliminary experiment was adopted to label sulfur colloid with ¹⁸⁸Re, the volume of ¹⁸⁸Re perrhenate was changed and other steps was carried based on SC kit introduction. (2) conditions of labeling stannic sulfur colloid with rhenium-¹⁸⁸ were changed, the volume of stannous chloride (20mg/mg) and sodium thiosulfate (8mg/ml) from 0ml to 1ml, both of them were added into kit in order. 2 Iabeling with reagent designed personally: the below conditions were changed singly (1) Volume of disodiumedetate (4.6mg/ml) from oml to 1.25ml. (2) Volume of sodium thiosulfate from 0ml to 1.25ml (3) Volume of stannous chloride (20mg/mg) 0ml to 1.25ml (4) After ¹⁸⁸Re perrhenate was added into reaction system, the PH value were adjusted with hydrochloric acid and phosphate buffer or sodium hydroxide was changed from 1 to 14. (5) The time of boiling from 1min to 35min (6) labeling efficiency were measured and analyzed at different time. 3 The stability and diameter of colloid were measured.Result The optimum conditions of ¹⁸⁸Re labeling Sn-SC were: 1 Iabeling with SC kit: o.5ml stannous chloride (20mg/mg) and 0.25ml sodium thiosulfate were both added into kit. 2 Iabeling with reagent designed personally: 18.1mg gelatin, 0.5ml disodiumedetate, 0.5ml sodium thiosulfate, 0.5ml stannous chloride were added into system in order, before boiling, PH of the reaction system were adjusted as PH=1 with chlorhydric acid, and the boiling time was 20min; The highest labeling efficiency of the highest labeling efficiency of two methods mentioned above were (99.79±0.31)% and (99.81±0.06)%, there was no significant difference between them. radiochemical purity could remain (93.62±0.64)% after 72h being placed in normal saline (v:v=1:10). The particle′s diameter was D10= (10.83±6.60)μm, D50= (44.91±14.46)μm, D90= (235.29±126.61)μm separately.Conclusion This method of 1abeling stannic sulfur colloid with rhenium-¹⁸⁸ is convenient and high labeling efficiency, favorable stability, big particle colloid were obtained.Partâ…¡: Experimental Study of Biodistribution of ¹⁸⁸Re-SnSC In Animals With TumorObjective To study biodistribution of ¹⁸⁸Re-SnSC in experimental animals with tumor and investigate practicability of radiotherapy for tumor with ¹⁸⁸Re-SnSC.Methods Prepare the ¹⁸⁸Re-SnSC as Partâ… ,high labeling efficient, stable and effective ¹⁸⁸Re-SnSC was obtained. biodistribution of ¹⁸⁸Re-SnSC was investigated through two approach. 1 Infusion via hepatic artery: 0.5ml (2mCi to 5mCi) ¹⁸⁸Re-SnSC (2groups, n=3) and ¹⁸⁸Re perrhenate (1group, n=3) were separa-tely infused into hepatic carcinoma of rabbits, guided by DSA. 2 intratumoral injection directly: 0.05ml (0.05mCi to 0.1mCi) ¹⁸⁸Re-SnSC (7groups, n=4) and ¹⁸⁸Re perrhenate(5groups, n=4) were separately injected intratumorally into center part of pancreatic carcinoma of nude mice. two kinds of experimental animals were scanned on SPECT and were sacrificed at different time point, the blood and major organs were excised and weighed, then the radioactivity count of those organs were measured and %ID/g were calculated.Result 1 Infusion via hepatic artery: The corresponding retention percentages of radioactivity (%ID/g) in tumor were (23.342±11.452)% and (0.713±0.479)% after 1h infusion with ¹⁸⁸Re-SnSC and ¹⁸⁸Re perrhenate, the ratio of %ID/g in tumor to liver were 70.887±19.578 and 2.280±1.155 separately. After 24h infusion the %ID/g in tumor and the ratio of %ID/g in tumor to liver were (8.176±6.836)% and 17.419±13.957 separately. 2 Intratumoral injection directly: The %ID/g in tumor after 0.5h, 1h, 4h, 24h injection with ¹⁸⁸Re-SnSC were (89.53±18.76)%, (104.31±36.72)%, (105.76±39.30)%, (86.22±18.47)% separately, and after 7days still remain (0.323±0.072)%; after 0.5h, 1h, 4h, 24h injection with ¹⁸⁸Re perrhenate the %ID/g in tumor were (17.72±2.46)%, (10.53±3.57)%, (6.24±2.59)%, (0.026±0.003)%. Conclusion ¹⁸⁸Re-SnSC can stay in the tumor with enough time. And it is a highly potential approach to radionuclide therapy for tumor.Partâ…¢: Investigation the Killing Efficiency of ¹⁸⁸Re-SnSC To Pancreatic Carcinoma CellsObjective To investigate the inhibition action of ¹⁸⁸Re-SnSC on pancreatic carcinoma cells.Methods 1 Prepare the ¹⁸⁸Re-SnSC as Partâ… : high labeling efficient, stable and effective ¹⁸⁸Re-SnSC was obtained and was place 30min for experiment in room temperature after radiolabeling. 2 200μl, 1×10⁴ pancreatic carcinoma cells were cultured in one hole on culture board, 0, 0.01, 0.025, 0.05mCi ¹⁸⁸Re-SnSC And 0, 0.01, 0.05mCi ¹⁸⁸Re perrhenate were added into each array on cultured board separately, where cells were cultured. 8 repeat holes were in very array. One culture board were taken out very day for experiment in one week. The light absorption value (OD Value) was examined through MTT assay, then growthcurves were depicted and inhibition ratios were calculated.Result inhibition action of ¹⁸⁸Re-SnSC to pancreatic carcinoma cells rose as dose of ¹⁸⁸Re-SnSC added into cell culture circumstance after 1 to 5 days drug was added. When 1.85MBq ¹⁸⁸Re-SnSC was added into each culture hole, the inhibition ratios on 1, 3, 5, 7day were (33.70±3.74)%, (89.80±1.21)%, (97.43±0.59)%, (92.20±1.18)%,and the maximum inhibition ratio could reach (98.09±0.58)%.Conclusion ¹⁸⁸Re-SnSC had inhibition action on pancreatic carcinoma cells.