Self‐Assembly Drug Delivery System Based on Programmable Dendritic Peptide Applied in Multidrug Resistance Tumor Therapy,Macromolecular Rapid Communications

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Self‐Assembly Drug Delivery System Based on Programmable Dendritic Peptide Applied in Multidrug Resistance Tumor Therapy
Macromolecular Rapid Communications ( IF 4.2 ) Pub Date : 2017-09-27 , DOI: 10.1002/marc.201700490
Si Chen ₁ , Jin-Xuan Fan ₂ , Wen-Xiu Qiu ₂ , Li-Han Liu ₂ , Han Cheng ₂ , Fan Liu ₁ , Guo-Ping Yan ₁ , Xian-Zheng Zhang ₂

Affiliation

In recent decades, diverse drug delivery systems (DDS) constructed by self‐assembly of dendritic peptides have shown advantages and improvable potential for cancer treatment. Here, an arginine‐enriched dendritic amphiphilic chimeric peptide CRRK(RRCG(Fmoc))₂ containing multiple thiol groups is programmed to form drug‐loaded nano‐micelles by self‐assembly. With a rational design, the branched hydrophobic groups (Fmoc) of the peptides provide a strong hydrophobic force to prevent the drug from premature release, and the reduction‐sensitive disulfide linkages formed between contiguous peptides can control drug release under reducing stimulation. As expected, specific to multidrug resistance (MDR) tumor cells, the arginine‐enriched peptide/drug (PD) nano‐micelles show accurate nuclear localization ability to prevent the drug being pumped by P‐glycoprotein (P‐gp) in vitro, as well as exhibiting satisfactory efficacy for MDR tumor treatment in vivo. This design successfully realizes stimuli‐responsive drug release aimed at MDR tumor cells via an ingenious sequence arrangement.

中文翻译：

基于可编程树突肽的自组装给药系统在多药耐药肿瘤治疗中的应用

在最近几十年中，通过树突状肽的自组装构建的多种药物递送系统（DDS）在癌症治疗方面显示出优势和可改进的潜力。在这里，一个富含精氨酸的树状两亲嵌合肽CRRK（RRCG（Fmoc））₂包含多个硫醇基团的程序可通过自组装形成载药纳米胶束。通过合理的设计，肽的支链疏水基团（Fmoc）提供了强大的疏水力来防止药物过早释放，并且连续肽之间形成的具有还原敏感性的二硫键可以在减少刺激的情况下控制药物的释放。正如预期的那样，特异于多药耐药性（MDR）肿瘤细胞的富含精氨酸的肽/药物（PD）纳米胶束具有精确的核定位能力，可以防止药物在体外被P-糖蛋白（P-gp）泵送，以及在体内MDR肿瘤治疗方面显示出令人满意的疗效。该设计通过巧妙的序列安排成功实现了针对MDR肿瘤细胞的刺激响应药物释放。

更新日期：2017-09-27

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