Theranostic Macromolecules Research Center, Department of Polymer Science and Engineering, Sungkyunkwan University, Suwon 440-746, South Korea.
J Control Release. 2011 Oct 10;155(1):11-7. doi: 10.1016/j.jconrel.2010.09.012. Epub 2010 Sep 18.
A series of pH-responsive polymeric micelles is developed to act as intelligent carriers to deliver iron oxide (Fe(3)O(4)) nanoparticles and respond rapidly to an acidic stimuli environment for magnetic resonance imaging (MRI). The polymeric micelle can be self-assembled at physiological pH by a block copolymer, consisting of a hydrophilic methoxy poly(ethylene glycol) (PEG) and a pH-responsive poly(β-amino ester)/(amido amine) block. Consequently, the Fe(3)O(4) nanoparticles can be well encapsulated into polymeric micelles due to the hydrophobic interaction, shielded by a PEG coronal shell. In an acidic environment, however, the pH-responsive component, which has ionizable tert-amino groups on its backbone, can become protonated to be soluble and release the hydrophobic Fe(3)O(4) nanoparticles. The Fe(3)O(4)-loaded polymeric micelle was measured by dynamic light scattering (DLS), superconducting quantum interference device (SQUID) and a 3.0T MRI scanner. To assess the ability of this MRI probe as a pH-triggered agent, we utilize a disease rat model of cerebral ischemia that produces acidic tissue due to its pathologic condition. We found gradual accumulation of Fe(3)O(4) nanoparticles in the brain ischemic area, indicating that the pH-triggered MRI probe may be effective for targeting the acidic environment and diagnostic imaging of pathologic tissue.
一系列 pH 响应性聚合物胶束被开发出来作为智能载体,用于输送氧化铁 (Fe(3)O(4)) 纳米颗粒,并对酸性刺激环境做出快速响应,用于磁共振成像 (MRI)。聚合物胶束可以通过嵌段共聚物在生理 pH 值下自组装,该嵌段共聚物由亲水性甲氧基聚乙二醇 (PEG) 和 pH 响应性聚 (β-氨基酯)/(酰胺基胺) 嵌段组成。因此,由于疏水相互作用,Fe(3)O(4)纳米颗粒可以很好地包裹在聚合物胶束中,被 PEG 冠层外壳屏蔽。然而,在酸性环境中,具有可电离叔氨基的 pH 响应性成分会质子化而变得可溶,并释放出疏水性的 Fe(3)O(4)纳米颗粒。通过动态光散射 (DLS)、超导量子干涉装置 (SQUID) 和 3.0T MRI 扫描仪测量负载 Fe(3)O(4)的聚合物胶束。为了评估这种 MRI 探针作为 pH 触发剂的能力,我们利用脑缺血疾病大鼠模型,由于其病理状况,该模型会产生酸性组织。我们发现 Fe(3)O(4)纳米颗粒逐渐在脑缺血区域积累,表明 pH 触发的 MRI 探针可能对靶向酸性环境和病理性组织的诊断成像有效。
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