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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。
In recent years, drug-loaded microspheres have drawn wide attention in the treatment of embolization. In this study, polyvinyl alcohol / acrylic microspheres for embolization were prepared by reversed-phase suspension polymerization. First, microspheres with a particle size of 100-1000 μm were screened and sunitinib was used as a model drug. According to ion exchange The physicochemical properties of microspheres (B-MS) and drug-loaded microspheres (SU-MS) were evaluated systematically: morphology, particle size and distribution of microspheres, equilibrium water content, elasticity Nature, etc., investigated the microspheres drug loading and in vitro release of the law. The results showed that the appearance of the microspheres was round and the diameters of the microspheres before and after drug loading were suitable for embolization. The equilibrium water content of the microspheres decreased and the rigidity increased after drug loading. The microspheres’ The drug dose and entrapment efficiency are mainly affected by the concentration of drug solution. Drug-loaded microspheres release slowly in phosphate buffered saline (PBS). Therefore, sunitinib-loaded microspheres have the potential value of arterial embolization.