一种新型普鲁兰微球的制备及其释药性能研究  

Preparation of a novel pullulan microsphere and its drug-release properties

作　　者：田思蓝 袁华兵[1,2] 刘瑾昀 TIAN Silan;YUAN Huabing;LIU Jinyun(Pharmacy Department,the First People's Hospital of Tianmen City,Tianmen,Hubei,431700,China;Hubei Key Laboratory of Occupational Hazard Identification and Control,Wuhan University of Science and Technology,Wuhan,Hubei,430081,China;School of Medicine,Hunan Normal University,Changsha,Hunan,410013,China)

机构地区：[1]天门市第一人民医院药剂科,湖北天门431700 [2]武汉科技大学职业危害识别与控制湖北省重点实验室,湖北武汉430081 [3]湖南师范大学医学院,湖南长沙410013

出　　处：《肿瘤药学》2021年第6期680-685,共6页Anti-Tumor Pharmacy

基　　金：湖北省卫生健康委联合基金项目(WJ2019H169);湖南师范大学大学生创新项目(2019111)。

摘　　要：目的构建一种白血病治疗药物甲氨蝶呤(MTX)的新载体,探讨其对MTX的负载效率及其缓释性。方法采用动态光散射(DLS)和扫描电镜(SEM)对载体载药前后的粒径、电位及形貌进行表征,紫外分光光度法测定MTX的含量。结果平均粒径大小为1098 nm,Zeta电位为0.835 mV,载药后分别为1324 nm、0.727 mV,载药后粒径略有增加。MTX的载药量和包封率分别未(13.44±2.13)%、(58.7±4.6)%。SEM显示,该载体载药前后均为球形结构,证明微球制备成功。体外释放研究表明,微球负载的药物释放明显减缓,游离药物在10 h内可完全释放,但此时微球中的药物释放量仅30.0%左右,72 h仅释放78.6%。结论负载MTX的胆甾醇疏水改性普鲁兰(CHP)微球属于微米级,具有较高的载药量和明显的缓释性。Objective To construct a new carrier of methotrexate(MTX)for the treatment of leukemia,and to investigate its load efficiency and sustained-release of MTX.Methods Dynamic light scattering(DLS)and scanning electron microscope(SEM)were used to characterize the particle size,potential and morphology of the carrier before and after drug loading.The content of MTX was determined by ultraviolet spectrophotometry.Results The average particle size of the carrier was 1098 nm and its Zeta potential was 0.835 mV.After drug loading,the size changed to 1324 nm and the Zeta potential was 0.727 mV.The size of the drug-loaded carrier was increased slightly.The drug-loading rate of MTX were(13.44±2.13)%and encapsulation efficiency of MTX were(58.7±4.6)%.The SEM pictures showed that the carrier has spherical structure before and after drug loading,which proved the successful preparation of microspheres.Our studies showed that the drug release from microspheres was significantly slowed down in vitro.Free drug was almost completely released at 10 h,but the drug in the microspheres was released only about 30.0%at 10 h,and about 78.6%at 72 h.Conclusion The micron-level pharmaceutical preparation of MTX-loaded cholesterol-modified pullulan(CHP)microspheres has been successfully achieved with high drug loading rate and obvious sustained-drug-release property.

关 键 词：缓释性 甲氨蝶呤 动态光散射 扫描电镜 载药量 

分 类 号：R943[医药卫生—药剂学] R979.1[医药卫生—药学]