Reduction-triggered breakable micelles of amphiphilic polyamide amine-g-polyethylene glycol for methotrexate delivery.
Reduction-triggered breakable micelles of amphiphilic polyamide amine-g-polyethylene glycol for methotrexate delivery.
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用于甲氨蝶呤递送的两亲性聚酰胺胺-g-聚乙二醇的还原触发易碎胶束
DOI：
10.1155/2014/904634
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发表时间：
2014
影响因子：
--
通讯作者：
Zhang X
中科院分区：
文献类型：
--
作者：
Huang Y;Liu J;Cui Y;Li H;Sun Y;Fan Y;Zhang X
以S-S键为主链的两亲性PAA-g-PEG型共聚物为原料，制备了含有甲氨蝶呤的还原触发式可破碎聚合物胶束。胶束呈球形，直径小于70 nm。胶束可以将疏水的甲氨蝶呤包裹在疏水核中。胶束的载药量和载药效率与共聚物的化学结构密切相关，分别为2.9%~7.5%和31.9%~82.5%。共聚物中疏水链段越多，载药量和载药效率越高。在正常情况下，这些胶束能够保持稳定，并将大部分甲氨蝶呤保持在核心，通过与共聚物主链上的苯基进行π-π堆积来稳定所结合的甲氨蝶呤。在模拟细胞内隔室的还原环境中，由于还原引发的胶束破裂，整个MTX有效载荷可以迅速释放。这些胶束对KB、4T-1和HepG2等多种癌细胞具有良好的抗增殖活性，尤其是在低药物浓度范围内。
Reduction-triggered breakable polymeric micelles incorporated with MTX were prepared using amphiphilic PAA-g-PEG copolymers having S–S bonds in the backbone. The micelles were spherical with diameters less than 70 nm. The micelles could encapsulate the hydrophobic MTX in the hydrophobic core. The drug loading content and drug loading efficiency of the micelles were highly dependent on the copolymer chemical structure, ranging from 2.9 to 7.5% and 31.9 to 82.5%, respectively. Both the drug loading content and drug loading efficiency increased along with more hydrophobic segments in the copolymers. In normal circumstance, these micelles were capable of keeping stable and hold most of the MTX in the core, stabilizing the incorporated MTX through the π-π stacking with the phenyl groups in the backbone of the copolymers. In reductive environments that mimicked the intracellular compartments, the entire MTX payload could be quickly released due to the reduction-triggered breakage of the micelles. These micelles showed good antiproliferative activity against several cancer cell lines, including KB, 4T-1 and HepG2, especially within the low drug concentration scope.
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