载舒尼替尼栓塞微球的制备及体外性质研究

近年来载药微球在栓塞治疗中引起了广泛关注。本研究采用反相悬浮聚合法制备了用于栓塞的聚乙烯醇／丙烯酸微球，首先筛分出粒径在100—1000μm范围的微球，并以舒尼替尼为模型药物，根据离子交换原理制备出载药微球：系统地评价了空白微球（B-Ms）和载药微球（su—Ms）的理化性质：微球的形态、粒径及其分布、平衡含水量、弹性性质等，考察了微球的载药和体外释药的规律。结果显示：微球外观圆整，载药前后微球的粒径均适用于栓塞，载药后微球平衡含水量下降，刚性增加，载药前后微球的弹性均适于栓塞；微球载药量和包封率主要受药液浓度的影响，载药微球在磷酸盐缓冲液（PBS）中缓慢释药，因此，舒尼替尼载药微球具有动脉栓塞治疗的潜在应用价值。

Preparation and characterization of sunitinib-loaded microspheres for arterial embolization

Drug-loaded microspheres have been caused much attention in embotherapy in recent years. In thlS StUdy, poiyvlnyi alcohol/acrylic acid microspheres were prepared by inverse suspension polymerization method. Sunitinih malate （SU） was used as a model drug and loaded on microspheres through ion-exchange mechanism. We investigated the characterization of blank microspheres （B-Ms） and sunitinib-loaded microspheres （SU-Ms） in vitro, including morphology, size distribution, equilibrium water content （EWC）, elasticity, drug loading and drug release. The result showed that both B-Ms and SU-Ms were spherical with smooth surface. The particle size of B-Ms and SU-Ms were both suitable for embolization. Compared with that of B-Ms, the EWC of SU-Ms was decreased and the rigidity of SU-Ms was increased. Drug loading and entrapment efficiency of microspheres were mainly affected by the concentration of sunitinib solution than by the size of microspheres. SU-Ms exhibited a sustained release in phosphate buffer solution （PBS）. Thus, the SU-Ms may have potential application for arterial embolization.