Preparation and characterization of budesonide-loaded solid lipid nanoparticles for pulmonary delivery  

布地奈德固体脂质纳米粒肺部给药系统的制备和评价(英文)

作　　者：张沛然[1] 涂盈锋[1] 王硕[2] 王艺辉[1] 谢英[1] 李淼[3] 金义光[3] 

机构地区：[1]北京大学医学部药学院药剂学系,北京100191 [2]瑞士巴塞尔大学药学院 [3]北京放射医学研究所,北京100850

出　　处：《Journal of Chinese Pharmaceutical Sciences》2011年第4期390-396,共7页中国药学（英文版）

基　　金：National Basic Research Program of China (973 Program No 2009CB930300);National Integrity Innovational Technology Platform of New Drug and Research and Development (Grant No 2009ZX09310-001)

摘　　要：To increase the solubility and adsorption of budesonide（BUD）,budesonide-loaded solid lipid nanoparticles（BUD-SLNs） were prepared and characterized in this study.Glycerin monostearate（GMS）was selected to be the matrix lipid material after calculation the differences of partial solubility parameters.An emulsification-ultrasound diffusion method was employed and formula was optimized in the BUD-SLNs preparation.The entrapment efficiency（ee%）of BUD-SLNs was（97.77±2.60）%, and the mean particle size was 147.3 nm（PDI=0.228）.Uniform and sphere particles were observed under TEM.The in vitro release of BUD-SLNs could be well explained by the biphasic release dynamics equation.The spectrums of DSC and X-ray diffraction indicated that BUD molecules were dispersed mainly into the lipids to form homogeneous matrix structure.Our results provide fundamental data for the application of SLNs in pulmonary delivery system.为改善布地奈德的溶解度和吸收,制备并评价了布地奈德固体脂质纳米粒(BUD-SLNs)。通过计算部分溶解度参数选择了单硬脂酸甘油酯作为脂材。经处方优化采用乳化-超声分散的方法制备的BUD-SLNs,包封率为(97.77±2.60)%;平均粒径是147.3nm,粒径分布均匀(PDI=0.228)。透射电镜下可见圆整颗粒。差热分析和X射线衍射实验的结果表明BUD以分子形式分散在SLNs中,体外释放结果表明BUD-SLNs符合双相动力学方程,属于均相骨架结构。研究结果为BUD-SLNs在肺部给药奠定了基础。

关 键 词：BUDESONIDE Solid lipid nanoparticles Pulmonary drug delivery PREPARATION CHARACTERIZATION 

分 类 号：R943[医药卫生—药剂学]