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首页> 外文会议>International Nuclear Atlantic Conference >ANTI-CEA APTAMERS LABELED WITH ~(99m)Tc: ENCAPSULATION STUDIES IN LONG-CIRCULATING AND pH-SENSITIVE LIPOSOMES, BIODISTRIBUTION AND IMAGING
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ANTI-CEA APTAMERS LABELED WITH ~(99m)Tc: ENCAPSULATION STUDIES IN LONG-CIRCULATING AND pH-SENSITIVE LIPOSOMES, BIODISTRIBUTION AND IMAGING

机译：抗CEA适体标记为〜（99米）TC：长循环和pH敏感脂质体的封装研究，生物分布和成像

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Colorectal cancer (CRC) is one of the leading cancers and the carcinoembryonic antigen (CEA) is a tumor marker widely used in diagnosis since it is overexpressed in tumor cells. Acid nucleic aptamers with high affinity and specificity for this antigen become promising molecules for CRC diagnosis by imaging. However, due to the action of nucleases in vivo, they have been investigated for association with liposomes, such as long-circulating and pH-sensitive liposomes (SPHL) that can be destabilized in the tumor region releasing aptamers and contributing to the CRC diagnosis by scintigraphy. In this work, SpHL containing DOPE, CHEMS and mPEG_(2000)-DSPE were characterized by analyzing mean diameter, polidispersity index and zeta potential. The anti-CEA aptamers Apt3 and Apt3-Amino were labeled with tecnethium-99m and the encapsulation efficiency (EE) of ~(99m)Tc-Apt3 in the SpHL by dehydration-rehydration (modified DRV) and freeze-thaw (FT) were analyzed, both in the presence of cryoprotectants. Biodistribution and scintigraphic images were performed at 1h and 4h post-injection of ~(99m)Tc-Apt3-amino, ~(99m)Tc-Apt3-SpHL or ~(99m)Tc-Apt3-amino-SpHL complexes in Balb/c healthy mice. The SpHL dispersions were homogeneous. The radiolabeling yield with technetium-99m was over 90% for all complexes. By the dehydration-rehydration method, the SpHL increased over 200% after encapsulation procedure. By the freeze-thaw method, the SpHL size increased only 13.7%. Free ~(99m)Tc-Apt3-amino showed to be cleared by renal via with high levels of radioatictivity in the kidney and bladder, however, the ~(99m)Tc-Apt3-SpHL and ~(99m)Tc-Apt3-amino-SpHL clearly indicated high uptake by liver and spleen. The biodistribution of ~(99m)Tc-Apt3-SpHL showed significant uptake of radioactivity by stomach and thyroid indicating less stability of the Apt3 radiolabelling in relation to Apt3-amino.
机译：结肠直肠癌（CRC）是主要癌症之一，癌症中抗原（CEA）是广泛用于诊断的肿瘤标志物，因为它在肿瘤细胞中过表达。具有高亲和力和特异性的酸性核酸型抗原的特异性是通过成像的CRC诊断的有望分子。然而，由于体内核酸酶的作用，已经研究了它们与脂质体相关联，例如可以在肿瘤区释放适体并促进CRC诊断中的肿瘤区中的长循环和pH敏感的脂质体（SPH1）。闪烁图。在这项工作中，通过分析平均直径，调节指数和Zeta电位，表征了含有掺杂剂，Chems和MPEG_（2000）-DSPE的SPH1。通过脱水再水合（改性DRV）和冷冻 - 解冻（FT）标记抗CEA Aptamers APT3和APT3-氨基和〜（99m）TC-APT3的〜（99m）TC-APT3的包封效率（EE）。在低温保护剂存在下分析。生物分布和闪烁图像在1H和4H注射后进行〜（99m）TC-APT3-氨基，〜（99M）TC-APT3-SPHL或〜（99M）TC-APT3-氨基-MPHL复合物在BALB / C中进行健康的老鼠。 SPHL分散体是均匀的。所有复合物的卫生纤维二键产率超过90％以上。通过脱水再水解方法，封装过程后SPH1增加了200％。通过冻融方法，SPHL尺寸仅增加13.7％。 Free〜（99米）TC-APT3-氨基显示肾脏和膀胱中高水平的放射性，然而，〜（99米）TC-APT3-SPHL和〜（99M）TC-APT3-氨基-sphl显然表明肝脏和脾脏的高吸收。 〜（99M）TC-APT3-SPH1的生物分布表明，胃和甲状腺的放射性显着吸收，表明APT3与APT3-氨基相关的APT3放射性标记的稳定性较小。

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