Department of Polymer Science and Engineering, Graduate School of Health Sciences and Technology, Sungkyunkwan University, Suwon 440-746, Republic of Korea.
J Control Release. 2012 Jun 28;160(3):692-8. doi: 10.1016/j.jconrel.2012.04.012. Epub 2012 Apr 13.
Polymeric nanoparticles, capable of encapsulating imaging agents and therapeutic drugs, have significant advantages for simultaneous diagnosis and therapy. Nonetheless, improvements in the loading contents of the active agents are needed to achieve enhanced imaging and effective therapeutic outcomes. Aiming to make these improvements, a hydrotropic micelle (HM) was explored to encapsulate superparamagnetic iron oxide nanoparticles (SPIONs) as the magnetic resonance (MR) imaging agent and paclitaxel (PTX) as the hydrophobic anticancer drug. Owing to its hydrotropic inner core with hydrophobic nature, HM could effectively encapsulate both of PTX and SPION via the simple dialysis method. The hydrodynamic size of HM increased from 68 to 178nm after physical encapsulation of SPION and PTX. Transmission electron microscopy analysis of HM bearing SPION and PTX (HM-SPION-PTX) revealed a spherical morphology with SPION clusters in the micelle cores. The micelles released PTX in a sustained manner. The bare HM and HM-SPION showed no toxicity to SCC7 cells, whereas HM-PTX and HM-SPION-PTX showed dose-dependent cytotoxicity that was lower than free PTX. HM-SPION-PTX exhibited 8.1-fold higher T(2) relaxivity than HM-SPION, implying potential of HM-SPION-PTX as the contrast agent for MR imaging. When systemically administered to tumor-bearing mice, HM-SPION-PTX was effectively accumulated at the tumor site, allowing its detection using MR imaging and effective therapy. Overall, these results suggested that HM-SPION-PTX is a promising candidate for combined diagnosis and treatment of cancer.
聚合物纳米粒子能够包裹成像剂和治疗药物,对于同时进行诊断和治疗具有显著的优势。然而,为了实现增强的成像和有效的治疗效果,需要提高活性药物的载药量。为了实现这些改进,本研究探索了一种水溶助长胶束(HM)来包裹超顺磁性氧化铁纳米粒子(SPION)作为磁共振(MR)成像剂和紫杉醇(PTX)作为疏水性抗癌药物。由于其具有疏水性的水溶助长内核,HM 可以通过简单的透析方法有效地包裹 PTX 和 SPION。SPION 和 PTX 物理包裹后,HM 的水动力粒径从 68nm 增加到 178nm。透射电子显微镜分析表明,载有 SPION 和 PTX 的 HM(HM-SPION-PTX)具有球形形态,SPION 簇位于胶束内核中。载药胶束以持续的方式释放 PTX。裸 HM 和 HM-SPION 对 SCC7 细胞没有毒性,而 HM-PTX 和 HM-SPION-PTX 则表现出剂量依赖性的细胞毒性,低于游离 PTX。HM-SPION-PTX 的 T(2)弛豫率比 HM-SPION 高 8.1 倍,表明 HM-SPION-PTX 具有作为磁共振成像对比剂的潜力。当系统地给予荷瘤小鼠时,HM-SPION-PTX 能够有效地在肿瘤部位聚集,允许使用磁共振成像进行检测并进行有效的治疗。总的来说,这些结果表明 HM-SPION-PTX 是一种有前途的用于癌症联合诊断和治疗的候选物。
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