Synthesis and biodistribution of novel magnetic-poly(HEMA-APH) nanopolymer radiolabeled with iodine-131 and investigation its fate in vivo for cancer therapy
Synthesis and biodistribution of novel magnetic-poly(HEMA-APH) nanopolymer radiolabeled with iodine-131 and investigation its fate in vivo for cancer therapy
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DOI：
10.1007/s11051-013-2021-7
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发表时间：
2013-09-27
影响因子：
2.5
通讯作者：
Akgol, Sinan
中科院分区：
文献类型：
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作者：
Avcibasi, Ugur;Avcibasi, Nesibe;Akgol, Sinan
在此，我们研究了一种基于甲基丙烯酸 2-羟乙酯 (HEMA) 和苯胺酞因 (APH) 的新型分子在白化 Wistar 大鼠代谢中的生物摄取、分布和放射性药物潜力。为了实现这一目标，我们使用有机合成方法合成了APH，并使用常见的聚合方法（无表面活性剂乳液聚合）将APH与HEMA共聚。在Fe3O4颗粒存在下，我们获得了新一代磁性纳米聚合物，磁性聚(HEMA-APH)。这种新分子通过傅里叶变换红外光谱、扫描电子显微镜、能量色散 X 射线光谱、电子自旋共振、原子力显微镜和 Zeta 粒度分析等多种表征方法进行了化学鉴定和批准。为了评估 mag-poly(HEMA-APH) 在活体代谢中的生物活性和抗癌潜力，通过广泛使用的标记技术（碘原法）使用伽马扩散放射性核素 I-131 对分子进行放射性碘化。薄层放射色谱实验表明，I-131 与纳米聚合物结合，标记率为 90%。进行亲脂性和稳定性实验以确定冷标记的mag-poly（HEMA-APH）在大鼠血液和脂质介质中的状况。结果表明，放射性碘标记的分子在大鼠代谢中作为完整复合物保留了 24 小时，实验亲脂性测定为 0.12 +/- A 0.02。体内成像和生物分布实验结果表明，I-131标记的mag-poly(HEMA-APH)[I-131-mag-poly(HEMA-APH)]在大鼠代谢中高度融入子宫、卵巢、前列腺和肺组织。基于这些结果，可以评价用I-131标记的新型mag-poly(HEMA-APH)分子是一种具有用作抗癌剂的巨大潜力的化合物。该分子是否应用于腺癌细胞模型和荷瘤动物才能获得一定的结果。
Herein, we investigated the biological uptake, distribution, and radiopharmaceutical potential of a novel molecule based on 2-hydroxyethyl methacrylate (HEMA) and anilinephtalein (APH) in the metabolism of Albino Wistar rats. In order to achieve this, we synthesized APH using organic synthesis methods and copolymerized APH with HEMA using a common polymerization method, surfactant-free emulsion polymerization. In the presence of Fe3O4 particles, we obtained a new generation magnetic-nano-scale polymer, magnetic-poly(HEMA-APH). This new molecule was chemically identified and approved by several characterization methods using Fourier transform infrared spectroscopy, scanning electron microscope, energy dispersive X-ray spectroscopy, electron spin resonance, atomic force microscope, and Zeta particle-size analysis. To evaluate the biological activity in live metabolism and anti-cancer potential of mag-poly(HEMA-APH), molecule was radioiodinated by a widely used labeling technique, iodogen method, with a gamma diffuser radionuclide, I-131. Thin-layer radiochromatography experiments demonstrated that I-131 binded to nanopolymer with the labeling yield of 90 %. Lipophilicity and stability experiments were conducted to determine the condition of cold and labeled mag-poly(HEMA-APH) in rat blood and lipid medium. Results demonstrated that radioiodinated molecule stayed as an intact complex in rat metabolism for 24 h and experimental lipophilicity was determined as 0.12 +/- A 0.02. In vivo results obtained by imaging and biological distribution experiments indicated that mag-poly(HEMA-APH) labeled with I-131 [I-131-mag-poly(HEMA-APH)] highly incorporated into tissues of the uterus, the ovarian, the prostate, and the lungs in rat metabolism. Based on these results, it may be evaluated that novel mag-poly(HEMA-APH) molecule labeled with I-131 is a compound which has a significant potential for being used as an anti-cancer agent. Certain results can only be obtained whether this molecule is applied to adenocarcinoma cell models and tumor-bearing animals.