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。
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.