Pharmaceutical Research Institute, Albany College of Pharmacy & Health Sciences, Rensselaer, NY 12144, USA.
Department of Physiology, Faculty of Veterinary Medicine, Uludag University, Gorukle, 16059 Bursa, Turkey.
Nanomedicine (Lond). 2017 Feb;12(3):195-205. doi: 10.2217/nnm-2016-0315. Epub 2017 Jan 19.
Nano-diamino-tetrac (NDAT) targets a receptor on integrin αvβ3; αvβ3 is generously expressed by cancer cells and dividing endothelial cells and to a small extent by nonmalignant cells. The tetrac (tetraiodothyroacetic acid) of NDAT is covalently bound to a poly(lactic-co-glycolic acid) nanoparticle that encapsulates anticancer drugs. We report NDAT delivery efficiency of cisplatin to agent-susceptible urinary bladder cancer xenografts.
MATERIALS & METHODS: Cisplatin-loaded NDAT (NDAT-cisplatin) was administered to xenograft-bearing nude mice. Tumor size response and drug content were measured.
Intratumoral drug concentration was up to fivefold higher (p < 0.001) in NDAT-cisplatin-exposed lesions than with conventional systemic administration. Tumor volume reduction achieved was NDAT-cisplatin > NDAT without cisplatin > cisplatin alone.
NDAT markedly enhances cisplatin delivery to urinary bladder cancer xenografts and increases drug efficacy.
纳米二氨基四（NDAT）靶向整合素 αvβ3 上的受体；αvβ3 在癌细胞和分裂的内皮细胞中大量表达，在非恶性细胞中少量表达。NDAT 的四碘甲状腺氨酸（tetraiodothyroacetic acid）与包裹抗癌药物的聚（乳酸-共-乙醇酸）纳米颗粒共价结合。我们报告了顺铂向对药物敏感的膀胱癌异种移植物中纳米二氨基四（NDAT）的递送效率。
将载有顺铂的 NDAT（NDAT-cisplatin）施用于荷瘤裸鼠。测量肿瘤大小反应和药物含量。
与传统的全身给药相比，NDAT-cisplatin 暴露病变部位的肿瘤内药物浓度高达五倍（p < 0.001）。NDAT-cisplatin 实现的肿瘤体积减少大于 NDAT 无顺铂 > 顺铂单独。
NDAT 显著增强了顺铂向膀胱癌异种移植物的递送，并提高了药物疗效。
