Utah-Inha DDS and Advanced Therapeutics, B-403 Meet-You-All Tower, Songdo Technopark, 7-50, Songdo-dong, Yeonsu-gu, Incheon 406-840, Republic of Korea; Department of Chemistry, Faculty of Science, Mahidol University, Nakhon Pathom 73170, Thailand.
J Colloid Interface Sci. 2014 Feb 1;415:70-6. doi: 10.1016/j.jcis.2013.09.049. Epub 2013 Oct 17.
Herein, we introduced amine-functionalized core-shell nanoparticles (Polymethyl methacrylate/Polyethyleneimine; PMMA/PEI) with surface primary amines (3.15×10(5) groups/particle) and uniform size distribution (150-200nm) that were prepared by one-step photo-induced emulsion polymerization. Further PEI-surface was modified with diethylenetriamine pentaacetic acid (DTPA) and introduced with Gd(III). The modified particles possessing DTPA can entrap a high content of Gd(III) ions of over 5.5×10(4)Gd/particle with stable chelation (no release of free Gd) at least 7h. The Gd-DTPA-conjugated core-shell nanoparticles (PMMA/PEI-DTPA-Gd NPs) enhanced the MRI intensity more than Primovist (a commercial hepatic contrast agent). Moreover, the PMMA/PEI-DTPA-Gd NPs showed non-cytotoxicity up to 250μM in normal liver cells. Thus, in vitro data suggested the PMMA/PEI-DTPA-Gd NPs is promising delivery system as a superior MRI contrast agent, especially for hepatic lesion targeted MR imaging.
在此，我们介绍了一种胺功能化的核壳纳米粒子（聚甲基丙烯酸甲酯/聚乙烯亚胺；PMMA/PEI），其表面带有伯胺（3.15×10^5 个/粒子）和均匀的粒径分布（150-200nm），是通过一步光诱导乳液聚合制备的。进一步，PEI 表面用二亚乙基三胺五乙酸（DTPA）修饰，并引入 Gd（III）。具有 DTPA 的修饰粒子可以螯合超过 5.5×10^4 Gd/粒子的高含量 Gd（III）离子，在至少 7 小时内稳定螯合（没有游离 Gd 的释放）。Gd-DTPA 共轭核壳纳米粒子（PMMA/PEI-DTPA-Gd NPs）增强了 MRI 强度，超过了普美显（一种商业肝造影剂）。此外，PMMA/PEI-DTPA-Gd NPs 在正常肝细胞中最高可达 250μM 时没有细胞毒性。因此，体外数据表明 PMMA/PEI-DTPA-Gd NPs 是一种有前途的作为优异 MRI 造影剂的递送系统，特别是用于肝病变靶向 MRI 成像。
