ATP/pH Dual Responsive Nanoparticle with d‐[des‐Arg10]Kallidin Mediated Efficient In Vivo Targeting Drug Delivery,Small

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ATP/pH Dual Responsive Nanoparticle with d‐[des‐Arg10]Kallidin Mediated Efficient In Vivo Targeting Drug Delivery
Small ( IF 13.0 ) Pub Date : 2016-10-24 , DOI: 10.1002/smll.201602494
Yu Zhang _{1,

2} , Yifei Lu _{1,

2} , Feng Wang _{1,

2} , Sai An _{1,

2} , Yujie Zhang _{1,

2} , Tao Sun _{1,

2} , Jianhua Zhu _{1,

2} , Chen Jiang _{1,

2}

Affiliation

Inflammation has been reported as one significant hallmark of breast cancer in relation to tumor development, metastasis, and invasion. The bradykinin receptor 1 (B1R) is highly expressed on inflammatory breast tumor cells thus providing a promising targeting site for tumor recognition and sufficient receptor mediated endocytosis. In this study, the authors evaluate the targeting efficiency of l‐form and d‐form [des‐Arg¹⁰]kallidin both in vitro and in vivo. To further improve the drug delivery efficiency, the authors establish a dandelion like nanoparticle by combining the polymeric drug conjugates and aptamer complex together. The doxorubicin conjugated polymer is complexed with adenosine‐5′‐triphosphate (ATP) sensitive hybridized aptamer in self‐assembly process by intercalating into the double strand scaffolds. The acid labile conjugating bond and ATP sensitive aptamer endow the nanoparticle with dual responsiveness to intracellular milieu, thus triggering a quick drug release in tumor cells. Remarkable therapeutic effects and tuned in vivo pharmacokinetics profiles are shown by the aptamer complexed drug conjugates nanoparticle with B1R active targeting modification. Therefore the strategies of B1R targeting and ATP/pH dual‐responsiveness nanoparticle help achieve enhanced drug accumulation within tumor cells and efficient chemotherapy for breast cancer.

中文翻译：

具有d- [des-Arg10] Kallidin的ATP / pH双反应纳米颗粒介导的高效体内靶向药物递送。

据报道，炎症是与肿瘤发展，转移和侵袭有关的乳腺癌的重要标志之一。缓激肽受体1（B1R）在炎症性乳腺肿瘤细胞上高度表达，因此为肿瘤识别和足够的受体介导的内吞作用提供了有希望的靶向位点。在这项研究中，作者评估了l形和d形[des-Arg ¹⁰在体外和体内都用] kallidin。为了进一步提高药物递送效率，作者通过将聚合的药物偶联物和适体复合物结合在一起，建立了类似蒲公英的纳米颗粒。通过插入双链支架，在自组装过程中，将阿霉素偶联的聚合物与5'-三磷酸腺苷（ATP）敏感的杂交适体复合。酸不稳定的结合键和ATP敏感的适体使纳米颗粒对细胞内环境具有双重反应，从而触发了肿瘤细胞中的快速药物释放。具有B1R活性靶向修饰的适体复合药物偶联物纳米颗粒显示出显着的治疗效果和体内药物动力学特性的调整。

更新日期：2016-10-24

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