Synthesis and characterization of DOX-conjugated dendrimer-modified magnetic iron oxide conjugates for magnetic resonance imaging, targeting, and drug delivery
Synthesis and characterization of DOX-conjugated dendrimer-modified magnetic iron oxide conjugates for magnetic resonance imaging, targeting, and drug delivery
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DOI：
10.1039/c2jm16792a
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发表时间：
2012-01-01
影响因子：
--
通讯作者：
Wang, Jingyuan
中科院分区：
文献类型：
--
作者：
Chang, Yulei;Liu, Nian;Wang, Jingyuan
构建并表征了一种基于叶酸（FA）与聚（乙二醇）（PEG）修饰的树枝状大分子（PAMAM）与阿霉素（DOX）和超顺磁性氧化铁（Fe3O4）（FA-PEG-PAMAM-DOX@IONPs）缀合的肿瘤靶向和pH响应性药物释放系统。 IONP 由 FA-PEG-G3.5 PAMAM 树枝状聚合物稳定。使用肼作为连接体，通过腙键将抗癌药物 DOX 与氨基稳定的 IONP 的树枝状聚合物片段缀合，腙键可被酸裂解，可用作理想的 pH 响应性药物释放系统。连接到 PAMAM@IONPs 上的 PEG 部分使缀合物在水性介质中具有优异的溶解度和稳定性，这可能会增加循环时间。附着的 FA 可以将缀合物靶向叶酸受体 (FR)。这些新型负载 DOX 的缀合物有可能在将药物输送到目标部位的过程中增强 MRI 对比和癌症治疗的效果。
A tumor targeted and pH-responsive drug release system that is based on folic acid (FA) conjugated to poly(ethylene glycol) (PEG)-modified dendrimers (PAMAM) with doxorubicin (DOX) and superparamagnetic iron oxide (Fe3O4) (FA-PEG-PAMAM-DOX@IONPs) has been constructed and characterized. IONPs were stabilized by FA-PEG-G3.5 PAMAM dendrimers. The anticancer drug DOX was conjugated to the dendrimer segments of amino-stabilized IONPs using hydrazine as the linker via hydrazone bonds, which are acid cleavable and can be used as an ideal pH-responsive drug release system. The PEG moiety attached to the PAMAM@IONPs provides the conjugates with excellent solubility and stability in an aqueous medium, which may increase the circulation time. The attached FA could target the conjugates to the folate receptor (FR). These novel DOX-loaded conjugates have the potential to enhance the effect of MRI contrast and cancer therapy in the course of delivering drugs to the target sites.