地塞米松聚乳酸羟基乙酸磁性微球体外生物相容性评价

Characteristics and biocompatibility of dexamethasone PLGA magnetic microspheres in vitro

背景磁性微球是近年来出现的一种靶向给药技术,可局部给药,达到控释或缓释效果,减少药物对注射部位的刺激反应,在医学诊断、成像和治疗方面有着广泛的应用。目的制备地塞米松聚乳酸羟基乙酸(poly lactic-co-glycolic acid,PLGA)磁性微球,观察其外观、质量、生物相容性及体外释放等特征。方法制备方法为乳化-溶剂挥发法。质量评价是通过相应方法评估该自制载药微球的外观、跨距、产率、载药量、包封率、体外释放、磁响应性等参数来完成;生物相容性评价则通过检测该自制空白微球的血液及组织相容性来实现。结果该自制微球外观圆整,跨距为(29.66±10.02)μm,产率为(87.25±3.14)%,载药量为(30.33±2.01)%,包封率为(78.89±2.42)%。体外释药模型为Q=4.0844t^(1/2)+6.6602(R^(2)=0.977),其过程无明显突释,第14天的累计释放率为66.99%;磁响应性尚佳。生物相容性检测结果均未见异常。结论该自制PLGA磁性微球质量较好,并有良好的生物相容性。

Background Superparamagnetic iron oxide nanoparticles(SPIONs)represent a simple yet effective system for delivering drugs to targeted tissue sites.The advantages of SPIONs as controlled drug-delivery devices include a decrease in single-dosage size,a continuous drug concentration,decreased systemic side effects,and SPIONs have been widely used in medicine for diagnostic imaging and therapeutic applications.Objective To prepare dexamethasone loaded PLGA(poly lactic-co-glycolic acid)magnetic microsphere and observe its appearance,quality,biocompatibility and in vitro release and so on.Methods The microspheres were prepared by emulsion-solvent evaporation method.The quality was assessed by calculating its shape,span,yield,drug loading,entrapment efficiency,in vitro release and magnetic responsiveness;and the biocompatibility was evaluated by haemocompatibility and histocompatibility test.Results The span of the microspheres was(29.66±10.02)μm with a yield of(87.25±3.14)%.The drug loading and the entrapment efficiency were(30.33±2.01)%and(78.89±2.42)%,respectively.The in vitro release model was Q=4.0844 t^(1/2)+6.6602(R^(2)=0.977),and no obvious sudden release in the process was observed.The cumulative release rate was 66.99%on the 14 th day,with reliable magnetic responsiveness.There was no abnormality in biocompatibility.Conclusion The self-made dexamethasone PLGA magnetic microspheres have good quality and biocompatibility.