Purpose

In this study, we fabricated a nanoplatform to target tumor sites via active and passive targeting effects, thus avoiding the toxic side effects of nanocarriers and improving the efficacy of chemotherapeutic drug delivery.

Methods

A sequential stimulus-responsive nanoparticle that targeted the tumor microenvironment and exhibited dual sensitivity to the reduction condition and matrix metalloproteinase-9 (MMP-9) enzyme was fabricated based on a self-assembled polypeptide-paclitaxel conjugate.

Results

The nanoparticles (48.9 ± 2.1 nm) transformed into rod-like nanostructures (297.1 ± 3.2 nm) in the presence of MMP-9. The rod-like nanostructures were taken up by tumor cells and then sensitive bonds were broken in response to highly expressed GSH in tumor cells to release drugs. This platform showed a tumor inhibition rate of 71.8% in S180-bearing mice and a more effective tumor inhibition rate than Taxol in 4T1-bearing mice.

Conclusion

This platform facilitates the design of enhanced safe and efficient chemotherapy drug delivery.

中文翻译：

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用于增强肿瘤生长抑制和有效药物递送的顺序刺激响应纳米颗粒平台

目的

在这项研究中，我们制造了一个纳米平台，通过主动和被动靶向作用靶向肿瘤部位，从而避免了纳米载体的毒副作用，提高了化疗药物递送的疗效。

方法

基于自组装多肽-紫杉醇偶联物制造了一种靶向肿瘤微环境并对还原条件和基质金属蛋白酶-9 (MMP-9) 酶具有双重敏感性的顺序刺激响应纳米颗粒。

结果

在 MMP-9 存在下，纳米颗粒 (48.9 ± 2.1 nm) 转变为棒状纳米结构 (297.1 ± 3.2 nm)。棒状纳米结构被肿瘤细胞吸收，然后响应于肿瘤细胞中高表达的 GSH 破坏敏感键以释放药物。该平台在 S180 小鼠中的抑瘤率为 71.8%，在 4T1 小鼠中的抑瘤率比紫杉醇更有效。

结论

该平台有助于设计增强的安全有效的化疗药物输送。