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通过纳米二氨基四氯的纳米颗粒成分将顺铂靶向递送至肿瘤异种移植物。

Targeted delivery of cisplatin to tumor xenografts via the nanoparticle component of nano-diamino-tetrac.

机构信息

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.

出版信息

Nanomedicine (Lond). 2017 Feb;12(3):195-205. doi: 10.2217/nnm-2016-0315. Epub 2017 Jan 19.

Abstract

AIM

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.

RESULTS

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.

CONCLUSION

NDAT markedly enhances cisplatin delivery to urinary bladder cancer xenografts and increases drug efficacy.

摘要

目的

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。

材料与方法

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。

结果

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。

结论

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。

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