Gemcitabine has been considered a first-line chemotherapy agent for the treatment of pancreatic cancer. However, the initial response rate of gemcitabine is low and chemoresistance occurs frequently. Aptamers can be effectively internalized into cancer cells via binding to target molecules with high affinity and specificity. In the current study, we constructed an aptamer-based gemcitabine delivery system, APTA-12, and assessed its therapeutic effects on pancreatic cancer cells in vitro and in vivo. APTA-12 was effective in vitro and in vivo in pancreatic cancer cells with high expression of nucleolin. The results of in vitro cytotoxicity assays indicated that APTA-12 inhibited the growth of pancreatic cancer cell lines. In vivo evaluation showed that APTA-12 effectively inhibited the growth of pancreatic cancer in Capan-1 tumor-bearing mice compared to mice that received gemcitabine alone or vehicle. These results suggest that the gemcitabine-incorporated APTA-12 aptamer may be a promising targeted therapeutic strategy for pancreatic cancer.

吉西他滨被认为是治疗胰腺癌的一线化疗药物。然而，吉西他滨的初始反应率较低，并且经常发生化疗耐药。适体通过与靶分子以高亲和力和特异性结合，可以有效地内化到癌细胞中。在本研究中，我们构建了基于适配体的吉西他滨递送系统APTA-12，并在体外和体内评估了其对胰腺癌细胞的治疗效果。APTA-12在体外和体内对核仁素高表达的胰腺癌细胞有效。体外细胞毒性测定结果表明APTA-12抑制胰腺癌细胞系的生长。体内评估表明，与单独接受吉西他滨或媒介物的小鼠相比，APTA-12 能有效抑制 Capan-1 荷瘤小鼠的胰腺癌生长。这些结果表明，吉西他滨掺入的 APTA-12 适体可能是一种有前途的胰腺癌靶向治疗策略。