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Rapid delivery of paclitaxel with an organic solvent-free system based on a novel cell penetrating peptide for suppression of tumor growth
Journal of Materials Chemistry B ( IF 6.1 ) Pub Date : 2017-08-31 00:00:00 , DOI: 10.1039/c7tb01259d
Yuping Wei 1, 2, 3 , Liang Zhang 1, 2, 3 , Yankai Fu 1, 2, 2, 3, 4 , Xia Xu 3, 5
Affiliation  

Paclitaxel (PTX) is widely used to treat ovarian, breast, lung, pancreatic, cervical and other cancers, however, the cell uptake and utilization of PTX is greatly limited by its slow penetration rate and poor solubility in water. Therefore, it is of great interest to develop an efficient method for PTX delivery to improve its cellular uptake and utilization. A novel cell penetrating peptide, RRRRRWW (R7), is developed to accelerate the translocation of PTX into HeLa cells in the organic solvent-free system to suppress tumor growth. There is no significant cytotoxicity induced by the peptide alone even after 24 h incubation at 1 mM at 37 °C for both cancer cells and normal cells. In contrast, 30 min treatment with the R7/PTX complex leads to a significant decrease in the cell viability. The intracellular PTX concentration of the R7/PTX complex group is 3 fold that of the free PTX group. The in vivo animal experiments show that the tumor is dramatically suppressed by a tail vein injection of the R7/PTX complex. This system provides a novel approach for the delivery of PTX into tumor cells to efficiently suppress tumor growth.

中文翻译:

使用基于新型细胞穿透肽的无有机溶剂系统快速递送紫杉醇,可抑制肿瘤生长

紫杉醇(PTX)被广泛用于治疗卵巢癌,乳腺癌,肺癌,胰腺癌,宫颈癌和其他癌症,但是,PTX的细胞吸收和利用受到其缓慢的渗透速度和在水中的不良溶解性的极大限制。因此,开发一种有效的PTX递送方法以改善其细胞摄取和利用是非常令人感兴趣的。开发了一种新型的细胞穿透肽RRRRRRWW(R7),可在无有机溶剂的系统中加速PTX向HeLa细胞的转运,从而抑制肿瘤的生长。即使在1 mM于37°C孵育24小时后,对于癌细胞和正常细胞也没有单独的肽引起明显的细胞毒性。相反,用R7 / PTX复合物处理30分钟会导致细胞活力显着下降。R7 / PTX复合物组的细胞内PTX浓度是游离PTX组的3倍。这体内动物实验表明,通过尾静脉注射R7 / PTX复合物可显着抑制肿瘤。该系统提供了将PTX递送至肿瘤细胞以有效抑制肿瘤生长的新颖方法。
更新日期:2017-09-18
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