Drug Delivery Nanocarriers from a Fully Degradable PEG-Conjugated Polyester with a Reduction-Responsive Backbone.
Drug Delivery Nanocarriers from a Fully Degradable PEG-Conjugated Polyester with a Reduction-Responsive Backbone.
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DOI：
10.1002/chem.201502233
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发表时间：
2015-08
期刊：
影响因子：
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通讯作者：
Basit Yameen;C. Vilos;W. Choi;A. Whyte;Jin-Hua Huang;Lori Pollit;O. Farokhzad
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文献类型：
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作者：
Basit Yameen;C. Vilos;W. Choi;A. Whyte;Jin-Hua Huang;Lori Pollit;O. Farokhzad
还原剂的显著高的细胞内浓度是用于设计被编程用于治疗剂的细胞内递送的纳米载体的极好的内源性刺激。然而，尽管它们具有优异的生物降解性，但响应于细胞内还原环境而完全降解的脂肪族聚酯是罕见的。本文报道了一种由具有二硫键的线性聚酯衍生的还原响应性药物递送纳米载体。通过方便的缩聚工艺合成还原响应性聚酯。在聚酯的末端羧酸基团与聚乙二醇（PEG）缀合后，所得聚合物自组装成能够包封染料和抗癌药物分子的纳米颗粒。还原响应性纳米颗粒响应于细胞内还原环境而显示出快速的有效载荷释放速率，这转化为对PC-3细胞的上级抗癌活性。
The remarkably high intracellular concentration of reducing agents is an excellent endogenous stimulus for designing nanocarriers programmed for intracellular delivery of therapeutic agents. However, despite their excellent biodegradability profiles, aliphatic polyesters that are fully degradable in response to the intracellular reducing environment are rare. Herein, a reduction-responsive drug delivery nanocarrier derived from a linear polyester bearing disulfide bonds is reported. The reduction-responsive polyester is synthesized via a convenient polycondensation process. After conjugation of terminal carboxylic acid groups of polyester to polyethylene glycol (PEG), the resulting polymer self-assembles into nanoparticles that are capable of encapsulating dye and anticancer drug molecules. The reduction-responsive nanoparticles display a fast payload release rate in response to the intracellular reducing environment, which translates into superior anticancer activity towards PC-3 cells.