聚己内酯载药微球的制备及释药性能研究  

Preparation and Release Study of Drug Loaded Poly(ε-caprolactone)Microspheres

作　　者：胡运玖 左奕[2] 邬均[1] 李玉宝[2] 孟纯阳[3] 王尖[2] 蒋电明[1] 

机构地区：[1]重庆医科大学附属第一医院骨科,重庆400016 [2]四川大学纳米生物材料研究中心分析测试中心,成都610064 [3]济宁医学院附属医院骨科,济宁272000

出　　处：《材料导报》2015年第2期29-32,56,共5页Materials Reports

基　　金：国家自然科学基金(81171685)

摘　　要：首次以利福喷丁为模型药物、聚己内酯为载体材料,制备了用于长效抑制骨结核生长的利福喷丁聚己内酯缓释微球,观察其理化特性和体外释放性能。采用O/W乳化溶剂挥发法制备载利福喷丁聚己内酯微球,系统考察了投药量、聚乙烯醇的浓度、乳化速度对微球形貌、粒径、载药量和包封率的影响。通过对制备工艺的优化,得到最佳制备条件是乳化速度300r·min-1,投药量20mg,聚乙烯醇的浓度2%。所制备的载利福喷丁聚己内酯微球圆整,表面有微孔,大小分布均匀,粒径分布较窄,平均粒径为(27.249±0.256)μm、载药量(3.098±0.011)%、包封率(34.078±0.123)%。实验结果表明:聚己内酯是负载利福喷丁的一种理想控释材料。Microspheres of Rifapentine（RFT）-poly（ε-caprolactone）（PCL）were fabricated by oil-in-water（O/W）solvent evaporation method to fabricate a long-time controlled-release system.The effect of technological parameters such as stirring speed of the emulsion,the volume ratio of drug and the concentration of PVA on the morphology,size distribution,drug loading and entrapment efficiency of the microspheres were evaluated.The RFT-PCL microspheres were characterized systematically by using SEM,FT-IR,XRD and in vitro drug release behavior.The optimal preparation conditions were as follows：speed of mechanical stirring 300r·min^-1,quantity of drug 20 mg,and polyvinyl alcohol concentration 2%.The RFT-PCL microsphere display an average particle size of（27.249±0.256）μm with（3.098±0.011）wt% drug loading amount and（34.078±0.123）% entrapment efficiency,while presenting spherical shape,microbore surface,uniform size distribution and narrow particle size distribution.The results indicated that poly（ε-caprolactone）is an ideal carrier material for Rifapentine to prepare a controlled-release delivery system.

关 键 词：利福喷丁 聚己内酯 载药微球 O/W法 

分 类 号：TB34[一般工业技术—材料科学与工程] R318[医药卫生—生物医学工程]