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首页> 外文期刊>Biomaterials >The efficiency of tumor-specific pH-responsive peptide-modified polymeric micelles containing paclitaxel
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The efficiency of tumor-specific pH-responsive peptide-modified polymeric micelles containing paclitaxel

机译：含紫杉醇的肿瘤特异性pH响应肽修饰的聚合物胶束的效率

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The acidic pH in tumor tissues could be used for targeting solid tumors. In the present study, we designed a tumor-specific pH-responsive peptide H 7K(R 2) 2, which could respond to the acidic pH in tumor tissues, and prepared H 7K(R 2) 2-modified polymeric micelles containing paclitaxel (PTX-PM-H 7K(R 2) 2) in order to evaluate their potential targeting of tumor cells and tumor endothelial cells and their anti-tumor activity in mice with tumor cells. PTX-PM-H 7K(R 2) 2 was prepared by a thin-film hydration method. The invitro release of PTX from PTX-PM-H 7K(R 2) 2 was tested. The invitro targeting characteristics of H 7K(R 2) 2-modified polymeric micelles on HUVEC (human umbilical vein endothelial cells) and MCF-7 (human breast adenocarcinoma cells) were evaluated. The invivo targeting activity of H 7K(R 2) 2-modified polymeric micelles and the invivo anti-tumor activity of PTX-PM-H 7K(R 2) 2 were also investigated in MCF-7 tumor-bearing mice. The released PTX from the PTX-PM-H 7K(R 2) 2 was not affected by the pH. The targeting activity of the H 7K(R 2) 2-modified polymeric micelles was demonstrated by invitro flow cytometry and confocal microscopy as well as invivo biodistribution. PTX-PM-H 7K(R 2) 2 produced very marked anti-tumor and anti-angiogenic activity in MCF-7 tumor-bearing mice invivo.
机译：肿瘤组织中的酸性pH可用于靶向实体瘤。在本研究中，我们设计了一种可以对肿瘤组织中的酸性pH作出反应的肿瘤特异性pH响应肽H 7K（R 2）2，并制备了含有紫杉醇（H 7K（R 2）2修饰的聚合物胶束（ PTX-PM-H 7K（R 2）2），以评估其对肿瘤细胞和肿瘤内皮细胞的潜在靶向性以及在具有肿瘤细胞的小鼠中的抗肿瘤活性。通过薄膜水合法制备PTX-PM-H 7K（R 2）2。测试了PTX从PTX-PM-H 7K（R 2）2的体外释放。评估了H 7K（R 2）2修饰的聚合物胶束对HUVEC（人脐静脉内皮细胞）和MCF-7（人乳腺腺癌细胞）的体外靶向特性。还研究了MCF-7荷瘤小鼠中H 7K（R 2）2修饰的聚合物胶束的体内靶向活性和PTX-PM-H 7K（R 2）2的体内抗肿瘤活性。从PTX-PM-H 7K（R 2）2释放的PTX不受pH的影响。通过体外流式细胞术和共聚焦显微镜以及体内生物分布证明了H 7K（R 2）2修饰的聚合物胶束的靶向活性。 PTX-PM-H 7K（R 2）2在体内荷MCF-7荷瘤小鼠中产生了非常明显的抗肿瘤和抗血管生成活性。

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