文献：Design of pH-sensitive methotrexate prodrug-targeted curcumin nanoparticles for efficient dual-drug delivery and combination cancer therapy

文献链接：https://www.tandfonline.com/doi/full/10.2147/IJN.S152312#d1e205

作者：Jiajiang Xie,Zhongxiong Fan,Yang Li,Yinying Zhang,Fei Yu,Guanghao Su

摘要：

Aim

We designed acid-labile methotrexate (MTX) targeting prodrug self-assembling nanoparticles loaded with curcumin (CUR) drug for simultaneous delivery of multi-chemotherapeutic drugs and combination cancer therapy.

Methods

A dual-acting MTX, acting as both an anticancer drug and as a tumor-targeting ligand, was coupled to 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[aldehyde(polyethylene glycol)-2000] via Schiff’s base reaction. The synthesized prodrug conjugate (DSPE-PEG-Imine-MTX) could be self-assembled into micellar nanoparticles (MTX-Imine-M) in aqueous solution, which encapsulated CUR into their core by hydrophobic interactions (MTX-Imine-M-CUR).

结果

制备的MTX-Imine-M-CUR纳米颗粒由内部疏水性DSPE/CUR核心和外部亲水性双羟基聚乙二醇（PEG）外壳组成，外壳具有自靶向MTX前药冠。

1,2-二硬脂酰-sn-甘油-3-磷酸乙酰胺-N-[醛（聚乙二醇）-2000]和MTX之间的亚胺连接体作为动态共价键，足够强，即使在酸性pH下快速裂解，在生理pH下也能保持完整。MTX-imine-M-CUR可以通过叶酸受体介导的内吞作用选择性有效地将MTX和CUR编码到癌症细胞中，随后通过内体/溶酶体的酸性快速释放CUR和活性形式的MTX。

此外，MTX-Imine-M-CUR在体外和体内的*癌活性明显高于pH不敏感的负载CUR的DSPE-PEGAmide-MTX组装纳米颗粒（MTX-Amide-M-CUR）、负载CUR（M-CUR）的MTX非偶联DSPE-PEG组装胶束纳米颗粒、两种游离药物的组合和单个游离药物。

相关推荐：

TAT-PEG-DSPE

Cy3-iRGD-PEG-DSPE

FITC-iRGD-PEG-DSPE

R8-PEG-DSPE

Angiopep-2-PEG-DSPE

FITC-Angiopep-2-PEG-DSPE

TH-PEG-DSPE

R6H4-PEG-DSPE

以上文章内容来源各类期刊或文献，如有侵权请联系我们删除！