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OBJECTIVE To explore the method of preparation of 99mTc labeled AntiVEGF McAb 5-FU loaded polylactic acid nanoparticles(99mTc-5-FU-Ab-NPs), and investigate the biological distribution of the nanoparticles in human gas- tric carcinoma xenografts. METHODS Anti-VEGF monoclonal antibodyes(MCAB)in 5-FU-Ab-NPs were labeled with 99mTc using a modified Schwarz method.After isolation of the 99mTc-5-FU-Ab-NPs using a Sephadex G-250 column,the labeling percentage and radiochemical purity were determined using paper chromatog- raphy.The immunocompetence of the 99mTc-5-FU-Ab-NPs as tumor markers was determined using ELISA and immunohistochemistry.99mTc-5-FU-Ab-NPs (experimental group),99mTc-labelled murine multiclonal IgG loaded polylactic acid and nanoparticles(control group)were injected via the tail vein into SCID mice bearing human gastric carcinoma.A radio-immunity ECT image was developed at 2 and 6 h after the injection.Following the ECT imaging, the mice were sacrificed,their tissue and tumor radioactivity distribution determined,and percentage of the injected-dose per gram(%ID/g)and tumor/ nontumor(T/NT)ratio calculated.High performance liquid chromatography (HPLC)was used to determine the 5-FU concentration in the tumor tissue and blood in the mice of both groups. RESULTS The percentage of 99mTc-5-FU-Ab-NPs labeling was 90%~95%.There was no obvious decrease in the antibody activity before and after labeling.The radio-immuno-imaging(RII)showed that the tumor image had developed 2 h after injection of the 99mTc-5-FU-Ab-NPs,and with time it was clearer at the 6th hour fol owing the injection.The%ID/g of the tumor tissue at both 2 h and 6 h after the injection was significantly higher compared to the control group.The tumor%ID/g and the tumor to blood activity ratio(TB)of the experimental group at 6 h following the injection increased compared to that at 2 h,and at the same time,5-FU concentration in the tumor of the experimental group continuously increased over time,and showed a significant difference compared to the 5-FU concentration in the tumor of the control group. CONCLUSION The 99mTc-5-FU-Ab-NPs prepared in this study are adequate to meet the demands of the RII,and the immune targeting ability of the anti-VEGF MCAB is reliable.Six hours after injection,the 99mTc-5-FU-Ab-NPs showed a relatively high specific concentration shadow in the human gastric carcinoma xenografts.
OBJECTIVE To explore the method of preparation of 99mTc labeled AntiVEGF McAb 5-FU loaded polylactic acid nanoparticles (99mTc-5-FU-Ab-NPs), and investigate the biological distribution of the nanoparticles in human gas- tric carcinoma xenografts. METHODS Anti- VEGF monoclonal antibody (MCAB) in 5-FU-Ab-NPs were labeled with 99mTc using a modified Schwarz method. After isolation of the 99mTc-5-FU-Ab- NPs using a Sephadex G-250 column, the labeling percentage and radiochemical purity were determined using paper chromatog- raphy.The immunocompetence of the 99mTc-5-FU-Ab-NPs as tumor markers was determined using ELISA and immunohistochemistry. 99mTc-5-FU-Ab-NPs A radio-immunity ECT image was developed at 2 and 6 h after the injection. After the ECT imaging, the mice were injected via the tail vein into the SCID mice bearing human gastric carcinoma sacrificed, their tissue and tumo r radioactivity distribution determined, and percentage of the injected-dose per gram (% ID / g) and tumor / nontumor (T / NT) ratio calculated. High performance liquid chromatography (HPLC) was used to determine the 5-FU concentration in the RESULTS The percentage of 99mTc-5-FU-Ab-NPs was was 90% ~ 95%. There was no obvious decrease in the antibody activity before and after labeling. radio-immuno -imaging (RII) showed that the tumor image had developed 2 h after injection of the 99mTc-5-FU-Ab-NPs, and with time it was clearer at the 6th hour fol owing the injection.% ID / g of the tumor tissue at both 2 h and 6 h after the injection was significantly higher than to control group. tumor% ID / g and the tumor to blood activity ratio (TB) of the experimental group at 6 h the the injection increased compared to that at 2 h, and at the same time, 5-FU concentration in the tumor of the experimental group continuously increased over time, and sCONCLUSION The 99mTc-5-FU-Ab-NPs prepared in this study are adequate to meet the demands of the RII, and the immune targeting ability of the anti-VEGF MCAB is reliably. After hours after injection, the 99mTc-5-FU-Ab-NPs showed a relatively high specific concentration shadow in the human gastric carcinoma xenografts.