One-pot synthesis of glutathione-responsive amphiphilic drug self-delivery micelles of doxorubicin–disulfide–methoxy polyethylene glycol for tumor therapy†,Journal of Materials Chemistry B

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One-pot synthesis of glutathione-responsive amphiphilic drug self-delivery micelles of doxorubicin–disulfide–methoxy polyethylene glycol for tumor therapy†
Journal of Materials Chemistry B ( IF 6.1 ) Pub Date : 2017-11-30 00:00:00 , DOI: 10.1039/c7tb02817b
Xiao Duan _{1,

2,

3,

4,

5} , Ting Bai _{1,

2,

3,

4,

5} , Junjie Du _{1,

2,

3,

4,

5} , Jie Kong _{1,

2,

3,

4,

5}

Affiliation

We present a novel glutathione-responsive amphiphilic drug self-delivery (DSD) micelle with one-pot synthesis to synergistically address the problems of controlled drug release, degradability, drug tracing and in vivo accumulated toxicity. The anticancer drug doxorubicin (DOX), disulfide-based diacrylate (DSDA) and amino-polyethylene glycol monomethyl ether were linked by Michael addition in one-pot synthesis. The accumulative release rate of DOX analogues with drug activity from the micelles was 67.9% under pH 7.4 and GSH = 1 mg mL⁻¹ conditions after 72 h. The cell uptake experiment showed that the micelles of DOX–DSDA–PEG were indeed taken up by A549 cells and distributed to cell nuclei. The in vitro cell viability of A549 cells was evaluated by CCK-8 and Muse Annexin V & Dead Cell Kit. The results illustrated that the completely biodegradable micelles with glutathione-responsive bonds in the backbone are an effective drug self-delivery system for tumor therapy in the future.

中文翻译：

一锅合成阿霉素-二硫化物-甲氧基聚乙二醇的谷胱甘肽反应性两亲药物自递送胶束†

我们提出了一种新型的谷胱甘肽反应性两亲药物自递送（DSD）胶束与一锅合成，以协同解决受控药物释放，可降解性，药物追踪和体内累积毒性的问题。一锅合成中通过迈克尔加成法将抗癌药阿霉素（DOX），二硫化物基二丙烯酸酯（DSDA）和氨基聚乙二醇单甲醚连接在一起。在pH 7.4和72 h后，GSH = 1 mg mL ^-1的条件下，具有药物活性的DOX类似物从胶束的累积释放率为67.9％。细胞吸收实验表明，DOX-DSDA-PEG的胶束确实被A549细胞吸收并分布到细胞核中。在体外通过CCK-8和Muse Annexin V和Dead Cell Kit评估A549细胞的细胞存活率。结果表明，骨架中具有谷胱甘肽反应键的完全可生物降解的胶束是将来用于肿瘤治疗的有效药物自递送系统。

更新日期：2017-11-30

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