Bult W, Seevinck P R, Krijger G C, Visser T, Kroon-Batenburg L M J, Bakker C J G, Hennink W E, van het Schip A D, Nijsen J F W
Department of Radiology and Nuclear Medicine, University Medical Center Utrecht, Utrecht, The Netherlands.
Pharm Res. 2009 Jun;26(6):1371-8. doi: 10.1007/s11095-009-9848-8. Epub 2009 Feb 25.
The aim of this study was to develop microspheres with an ultra high holmium content which can be neutron activated for radioablation of malignancies. These microspheres are proposed to be delivered selectively through either intratumoral injections into solid tumors or administered via an intravascularly placed catheter.
Microspheres were prepared by solvent evaporation, using holmium acetylacetonate (HoAcAc) crystals as the sole ingredient. Microspheres were characterized using light and scanning electron microscopy, coulter counter, titrimetry, infrared and Raman spectroscopy, differential scanning calorimetry, X-ray powder diffraction, magnetic resonance imaging (MRI), and X-ray computed tomography (CT).
Microspheres, thus prepared displayed a smooth surface. The holmium content of the HoAcAc microspheres (44% (w/w)) was higher than the holmium content of the starting material, HoAcAc crystals (33% (w/w)). This was attributed to the loss of acetylacetonate from the HoAcAc complex, during rearrangement of acetylacetonate around the holmium ion. The increase of the holmium content allows for the detection of (sub)microgram amounts of microspheres using MRI and CT.
HoAcAc microspheres with an ultra-high holmium content were prepared. These microspheres are suitable for radioablation of tumors by intratumoral injections or treatment of liver tumors through transcatheter administration.
本研究的目的是开发一种具有超高钬含量的微球,该微球可通过中子活化用于恶性肿瘤的放射性消融。这些微球建议通过向实体瘤内注射或通过血管内放置的导管给药来选择性递送。
以乙酰丙酮钬(HoAcAc)晶体为唯一成分,通过溶剂蒸发法制备微球。使用光学和扫描电子显微镜、库尔特计数器、滴定法、红外和拉曼光谱、差示扫描量热法、X射线粉末衍射、磁共振成像(MRI)和X射线计算机断层扫描(CT)对微球进行表征。
如此制备的微球表面光滑。HoAcAc微球的钬含量(44%(w/w))高于起始原料HoAcAc晶体的钬含量(33%(w/w))。这归因于在钬离子周围乙酰丙酮重排过程中,乙酰丙酮从HoAcAc络合物中损失。钬含量的增加使得能够使用MRI和CT检测(亚)微克量的微球。
制备了具有超高钬含量的HoAcAc微球。这些微球适用于通过瘤内注射进行肿瘤的放射性消融或通过经导管给药治疗肝肿瘤。