Sudha Thangirala, Bharali Dhruba J, Yalcin Murat, Darwish Noureldien He, Debreli Coskun Melis, Keating Kelly A, Lin Hung-Yun, Davis Paul J, Mousa Shaker A
The Pharmaceutical Research Institute, Albany College of Pharmacy and Health Sciences, Rensselaer, NY, USA.
The Pharmaceutical Research Institute, Albany College of Pharmacy and Health Sciences, Rensselaer, NY, USA; Department of Physiology, Veterinary Medicine Faculty, Uludag University, Gorukle, Bursa, Turkey.
Int J Nanomedicine. 2017 Feb 15;12:1305-1315. doi: 10.2147/IJN.S123742. eCollection 2017.
The tetraiodothyroacetic acid (tetrac) component of nano-diamino-tetrac (NDAT) is chemically bonded via a linker to a poly(lactic--glycolic acid) nanoparticle that can encapsulate anticancer drugs. Tetrac targets the plasma membrane of cancer cells at a receptor on the extracellular domain of integrin αvβ3. In this study, we evaluate the efficiency of NDAT delivery of paclitaxel and doxorubicin to, respectively, pancreatic and breast cancer orthotopic nude mouse xenografts. Intra-tumoral drug concentrations were 5-fold (paclitaxel; <0.001) and 2.3-fold (doxorubicin; <0.01) higher than with conventional systemic drug administration. Tumor volume reductions reflected enhanced xenograft drug uptake. Cell viability was estimated by bioluminescent signaling in pancreatic tumors and confirmed an increased paclitaxel effect with drug delivery by NDAT. NDAT delivery of chemotherapy increases drug delivery to cancers and increases drug efficacy.
纳米二氨基四碘甲状腺乙酸（NDAT）中的四碘甲状腺乙酸（tetrac）成分通过连接子化学键合到可封装抗癌药物的聚乳酸-乙醇酸纳米颗粒上。Tetrac在整合素αvβ3细胞外结构域的受体处靶向癌细胞的质膜。在本研究中，我们评估了NDAT分别向胰腺和乳腺癌原位裸鼠异种移植瘤递送紫杉醇和阿霉素的效率。瘤内药物浓度比传统全身给药分别高5倍（紫杉醇；<0.001）和2.3倍（阿霉素；<0.01）。肿瘤体积减小反映了异种移植瘤药物摄取增加。通过胰腺肿瘤中的生物发光信号估计细胞活力，并证实通过NDAT给药的紫杉醇效果增强。化疗的NDAT给药增加了对癌症的药物递送并提高了药物疗效。
