A carrier-free dual-drug nanodelivery system functionalized with aptamer specific targeting HER2-overexpressing cancer cells,Journal of Materials Chemistry B

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A carrier-free dual-drug nanodelivery system functionalized with aptamer specific targeting HER2-overexpressing cancer cells
Journal of Materials Chemistry B ( IF 6.1 ) Pub Date : 2017-11-01 00:00:00 , DOI: 10.1039/c7tb02562a
Kai Jiang _{1,

2,

3} , Longyu Han _{1,

2,

3} , Yan Guo _{1,

2,

3} , Guirong Zheng _{1,

2,

3} , Lulu Fan _{1,

2,

3} , Zhichun Shen _{1,

2,

3} , Ruirui Zhao _{1,

2,

3} , Jingwei Shao _{1,

2,

3}

Affiliation

Exploration of a green carrier to avoid potential systemic toxicity and the unclear metabolic mechanism of traditional nanocarriers is of high importance for cancer therapy. Hence, we developed a carrier-free nanosystem for co-delivery of dual anti-cancer drugs ursolic acid (UA) and doxorubicin (DOX) using a “green” and simple method. The co-assembled nanodrug was further modified with a HER2 aptamer by electrostatic interactions. The co-assembled dual nanodrug presented a spherical morphology with a uniform size (∼108.9 nm) and in a pH-triggered drug release manner. It made UA sensitize DOX to display synergistic anticancer effects at a low dose of DOX. Further, the aptamer surface decoration improved the intracellular drug retention of UA and DOX to as much as 2-fold in HER2 overexpressing cancer cells. In addition, the in vivo results further proved that the co-assembled nanodrug could significantly inhibit the tumor growth with a little side effects. In a word, this novel carrier-free dual-drug nanodelivery system could be a potential drug candidate for HER2 overexpressing cancer therapy, and UA could be used as a “green” nanocarrier for delivery of hydrophobic drugs and fluorescent dyes in cancer treatment and diagnosis.

中文翻译：

以适体特异性靶向过表达HER2的癌细胞为功能的无载体双药物纳米递送系统

探索绿色载体以避免潜在的全身毒性和传统纳米载体的不清楚的代谢机制对癌症治疗具有重要意义。因此，我们开发了一种无载体的纳米系统，可使用“绿色”且简单的方法共同递送双抗癌药物乌索酸（UA）和阿霉素（DOX）。通过静电相互作用，用HER2适体进一步修饰了共组装的纳米药物。共组装的双重纳米药物呈现出球形的形态，大小均匀（〜108.9 nm），并且通过pH触发药物释放。它使UA在低剂量的DOX下使DOX敏感，以显示协同抗癌作用。此外，适体表面修饰在过表达HER2的癌细胞中将UA和DOX的细胞内药物保留提高了两倍。除此之外体内结果进一步证明，共组装的纳米药物可以显着抑制肿瘤的生长，并且具有很小的副作用。简而言之，这种新颖的无载体双药物纳米递送系统可能是过度表达HER2癌症治疗的潜在药物候选者，UA可以用作“绿色”纳米载体，用于在癌症治疗和诊断中递送疏水性药物和荧光染料。

更新日期：2017-11-14

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