Folate-conjugated and pH-triggered doxorubicin and paclitaxel co-delivery micellar system for targeted anticancer drug delivery,Materials Chemistry Frontiers

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Folate-conjugated and pH-triggered doxorubicin and paclitaxel co-delivery micellar system for targeted anticancer drug delivery
Materials Chemistry Frontiers ( IF 6.0 ) Pub Date : 2018-06-05 00:00:00 , DOI: 10.1039/c8qm00217g
Lijing Niu _{1,

2,

3,

4} , Feiyan Zhu _{4,

5,

6,

7,

8} , Bowen Li _{1,

2,

3,

4} , Lingling Zhao _{1,

2,

3,

4,

9} , Hongze Liang _{1,

2,

3,

4} , Yinghua Yan _{1,

2,

3,

4} , Hui Tan _{4,

8,

9,

10}

Affiliation

A folate-conjugated and pH-sensitive polymeric micellar system for the co-delivery of DOX and PTX was studied. A doxorubicin conjugated prodrug was synthesized via Schiff's base reaction. Subsequently, folate was grafted onto the prodrug and PTX was encapsulated. Sustained drug release of both DOX and PTX from the polymeric micelles was observed and the release rate could be accelerated by decreasing the media pH. A cellular uptake assay revealed that the polymeric micelles were internalized in the cytoplasm via endocytosis by SW1353 cells, and the cellular uptake was enhanced for the folate-conjugated micelles due to an active FR-mediated endocytosis pathway, showing stronger red fluorescence compared to that of non-folate micelles. The in vitro anticancer efficiency of the polymeric micellar system was evaluated using a cytotoxicity assay by incubating different drug formulations with the SW1353 cells. Both free drugs and micellar formulations displayed inhibition of cell growth at different levels, while the folate-conjugated dual-drug loaded polymeric micelles (Folate–Oxd–DOX/PTX) displayed a much lower IC₅₀ value than other drug formulations, indicating a desirable in vitro anticancer efficiency due to the synergistic effect of co-delivery and active targeting. Thus, the polymeric micellar system is a promising platform for targeted cancer chemotherapy.

中文翻译：

叶酸偶联和pH触发的阿霉素和紫杉醇共递送胶束系统用于靶向抗癌药物递送

研究了叶酸-共轭和pH敏感的聚合物胶束系统，用于DOX和PTX的共递送。阿霉素结合的前药是通过席夫碱反应合成的。随后，将叶酸接枝到前药上并封装PTX。观察到聚合物胶束中DOX和PTX的持续药物释放，并且可以通过降低培养基pH值来加快释放速率。细胞摄取分析表明，SW1353细胞通过内吞作用将高分子胶束内化，并通过活性FR介导的内吞途径增强了叶酸偶联胶束的细胞摄取，与之相比，红色荧光更强。非叶酸胶束。在体外通过将不同的药物制剂与SW1353细胞一起孵育，使用细胞毒性测定法评估了聚合物胶束系统的抗癌效率。游离药物和胶束制剂均显示出不同水平的细胞生长抑制作用，而叶酸偶联的双药物负载聚合物胶束（Folate–Oxd–DOX / PTX）显示出比其他药物制剂低得多的IC ₅₀值，表明是理想的由于共同递送和主动靶向的协同作用，体外抗癌效率提高。因此，聚合物胶束系统是靶向癌症化疗的有前途的平台。

更新日期：2018-06-05

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