硫化铼复合纳米颗粒的制备及其表面修饰研究
摘要
放射性药物治疗是重要的肿瘤治疗方法之一。放射性核素铼(~(188)Re)由于具有优良的放射性和化学性能,受到了研究者的关注,包括硫化铼胶体颗粒以及掺杂铼的纳米颗粒。在肿瘤的治疗过程中,提高药物的靶向性,减少其在非靶向部位的聚集是提高抗肿瘤药物疗效的关键。磁靶向以及分子靶向是靶向治疗的两种方式。本文以稳定性同位素铼为原料,制备了具有靶向性的硫化铼复合纳米颗粒。
通过两步合成法,在硫化铼胶体体系中利用四甲基氢氧化铵(TMAOH)沉淀剂制备其粒径范围为5.5nm-12.5nm,磁化强度为24.1emu·g~(-1)的ReS_2/Fe_3O_4磁性复合纳米颗粒。氧化铁与硫化铼的复合不会改变硫化铼的化学态。ReS_2/Fe_3O_4复合颗粒经MPEG-COOH修饰后,磁性降为2.5 emu·g~(-1),并由铁磁性变为超顺磁性,颗粒的稳定性和分散性均得到极大的提高,有利于其在医学方面的应用。
通过改进的St(o|¨)ber方法,制备了具有单分散性的不同粒径的ReS_2/SiO_2复合纳米颗粒,并通过TEM、EDAX等对其表征,研究合成条件及SiO_2对复合颗粒的分散性的影响。以羧甲基壳聚糖(CMC)和3-胺基丙基-三甲氧基硅烷(APTMS)为修饰剂,制备了ReS_2/SiO_2/CMC和ReS_2/SiO_2/APTMS复合纳米颗粒,研究了氨基化前后颗粒形貌和粒径的变化,进而利用叶酸修饰氨基化的复合颗粒,并通过红外和紫外表征复合纳米颗粒的形成及叶酸的负载量。
Radiopharmaceutical therapy is one of tumor therapy methods. Radionuclide ~(188)Re has gained considerable attention due to its excellent radioactivity and chemical property,including rhenium sulfide colloid and nanoparticles containing radionuclide ~(188)Re.It is a key point for the drug efficacy to improve drug targeting and reduce the accumulation of drugs in non-targeting sites in the therapy of tumor.Magnetic targeting and molecule targeting are two means of targeting therapyies.This dissertation describes synthesis of the rhenium sulfide composite nanoparticles with target ability using the stable isotope rhenium as the material.
Through two step process magnetic rhenium sulfide ReS_2/Fe_3O_4 composite nanoparticles with sizes in the range of 5.5-12.5nm was synthesized in the system of rhenium sulfide collid by using tetra methyl ammonium hydroxide(TMAOH) as precipitant.Magnetization of the composite particles were 24.1 emu·g~(-1).The association of rhenium sulfide with iron oxide would not change the electronic state of rhenium sulfide. The magnetization changed from ferromagnetic to superparamagnetic behavior and decreased to 2.5 emu·g~(-1) after it was modified by MPEG-COOH.The modification enhanced the water-solubility and stability of the particles,which was beneficial to their application in medicine.
The monodispersed ReS_2/SiO_2 composite nanoparticles with different sizes were prepared by the modified St(o|¨)ber method and were characterized by TEM,EDAX.The synthesis was analyzed on the coating of SiO_2 and the dispersion of the composite nanoparticles.The composite particles were modified by amido-teminated molecules.ReS_2/SiO_2/CMC and ReS_2/SiO_2/APTMS composite nanoparticles were prepared.The morphology and the size of the particles were compared with the unmodified particles.The modified composite particles were further grafted with folate,and they were characterized by FT-IR and UV-vis to characterize the formation and the loading of folate.
通过两步合成法,在硫化铼胶体体系中利用四甲基氢氧化铵(TMAOH)沉淀剂制备其粒径范围为5.5nm-12.5nm,磁化强度为24.1emu·g~(-1)的ReS_2/Fe_3O_4磁性复合纳米颗粒。氧化铁与硫化铼的复合不会改变硫化铼的化学态。ReS_2/Fe_3O_4复合颗粒经MPEG-COOH修饰后,磁性降为2.5 emu·g~(-1),并由铁磁性变为超顺磁性,颗粒的稳定性和分散性均得到极大的提高,有利于其在医学方面的应用。
通过改进的St(o|¨)ber方法,制备了具有单分散性的不同粒径的ReS_2/SiO_2复合纳米颗粒,并通过TEM、EDAX等对其表征,研究合成条件及SiO_2对复合颗粒的分散性的影响。以羧甲基壳聚糖(CMC)和3-胺基丙基-三甲氧基硅烷(APTMS)为修饰剂,制备了ReS_2/SiO_2/CMC和ReS_2/SiO_2/APTMS复合纳米颗粒,研究了氨基化前后颗粒形貌和粒径的变化,进而利用叶酸修饰氨基化的复合颗粒,并通过红外和紫外表征复合纳米颗粒的形成及叶酸的负载量。
Radiopharmaceutical therapy is one of tumor therapy methods. Radionuclide ~(188)Re has gained considerable attention due to its excellent radioactivity and chemical property,including rhenium sulfide colloid and nanoparticles containing radionuclide ~(188)Re.It is a key point for the drug efficacy to improve drug targeting and reduce the accumulation of drugs in non-targeting sites in the therapy of tumor.Magnetic targeting and molecule targeting are two means of targeting therapyies.This dissertation describes synthesis of the rhenium sulfide composite nanoparticles with target ability using the stable isotope rhenium as the material.
Through two step process magnetic rhenium sulfide ReS_2/Fe_3O_4 composite nanoparticles with sizes in the range of 5.5-12.5nm was synthesized in the system of rhenium sulfide collid by using tetra methyl ammonium hydroxide(TMAOH) as precipitant.Magnetization of the composite particles were 24.1 emu·g~(-1).The association of rhenium sulfide with iron oxide would not change the electronic state of rhenium sulfide. The magnetization changed from ferromagnetic to superparamagnetic behavior and decreased to 2.5 emu·g~(-1) after it was modified by MPEG-COOH.The modification enhanced the water-solubility and stability of the particles,which was beneficial to their application in medicine.
The monodispersed ReS_2/SiO_2 composite nanoparticles with different sizes were prepared by the modified St(o|¨)ber method and were characterized by TEM,EDAX.The synthesis was analyzed on the coating of SiO_2 and the dispersion of the composite nanoparticles.The composite particles were modified by amido-teminated molecules.ReS_2/SiO_2/CMC and ReS_2/SiO_2/APTMS composite nanoparticles were prepared.The morphology and the size of the particles were compared with the unmodified particles.The modified composite particles were further grafted with folate,and they were characterized by FT-IR and UV-vis to characterize the formation and the loading of folate.
引文
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