Charge-Conversional and pH-Sensitive PEGylated Polymeric Micelles as Efficient Nanocarriers for Drug Delivery
Charge-Conversional and pH-Sensitive PEGylated Polymeric Micelles as Efficient Nanocarriers for Drug Delivery
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电荷转换和 pH 敏感的聚乙二醇化聚合物胶束作为有效的药物输送纳米载体
DOI：
10.1002/mabi.201400162
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发表时间：
2014-09-01
影响因子：
4.6
通讯作者：
Ji, Jian
中科院分区：
文献类型：
--
作者：
Liu, Gong-Yan;Li, Min;Ji, Jian
通过在聚乙烯亚胺（PEI）上接枝聚乙二醇（PEG）和1，2-顺式环己烷二甲酸酐（1，2-cis-cyclohexane dicarboxylic anhydride，1，2-cis-Cyclohexane），合成了一种新型两亲性共聚物PEG-g-PEI/amide。聚乙二醇化的两亲性共聚物可以组装成具有明确纳米尺寸的聚合物胶束，并成功地将抗癌药物负载到由酰胺形成的胶束核中。具有相邻羧酸基团的酰胺表现出pH依赖性水解，并且可以可逆地屏蔽PEI上胺基的阳离子电荷，使胶束在酸性肿瘤组织环境中具有从负到正的电荷转换性质。同时，酰胺键在酸性pH下的断裂也导致胶束的解体和pH响应性药物释放。这些胶束是有前途的药物递送系统，由于其智能特性：聚乙二醇化，合适的大小，电荷转换，并同时pH敏感的药物释放。
A novel amphiphilic copolymer, poly (ethylene glycol)-graft-polyethyleneimine/amide (PEG-g-PEI/amide), is synthesized by grafting PEG and 1,2-cis-Cyclohexanedicarboxylic anhydride onto the PEI. PEGylated polymeric micelles can be assembled from the amphiphilic copolymers with well-defined nano-sizes, and anticancer drugs are successfully loaded into micelle core formed by the amide. The amides with neighboring carboxylic acid groups exhibit pH-dependent hydrolysis and can reversibly shield the cationic charge of amine groups on the PEI, giving the micelles a charge-conversion property from negative to positive in acidic tumor tissue environment. Meanwhile, the cleavage of amide bonds at acidic pH also results in the disassembly of the micelle and pH-responsive drug release. These micelles are promising drug delivery systems due to their smart properties: PEGylation, suitable size, charge-conversion, and simultaneous pH-sensitive drug release.