载阿霉素聚乳酸多孔微球的表征及释药性能

Synthesis,characterization and in vitro drug release performance of poly-L-lactide porous microspheres

以阿霉素(DOX)为小分子化学药物模型,采用吸附法对聚乳酸(poly-L-lactide,PLLA)多孔微球进行载药,采用场发射扫描电子显微镜(FE-SEM)、傅里叶变换红外光谱(FTIR)、X射线衍射(XRPD)及差示扫描量热(DSC)对DOX-PLLA复合微球的形貌粒径及空气动力学性能、药物及材料的理化性能、载药性能进行表征,并且研究了其载药量、包封率和体外释放性能。结果表明,不同载药量之间的PLLA多孔微球粒径并无显著差异,均具有良好的空气动力学性能,适合肺部可吸入给药的条件;化学组成未见明显改变,物理结构由结晶态变为无定形态;随载药量的增加(2.9%,4.0%,4.6%),包封率逐渐降低(56%,51%,44%);药物的体外释放与原料药相比具有一定的缓释效果,最长释放时间可达5天,表明DOX-PLLA复合微球有望作为缓释制剂用于肺部给药。

Used the doxorubicin（DOX）as small molecule drug model,the DOX-loaded poly-L-lactide（PLLA）porous microspheres（PMs）were designed by adsorption method. The particle size distribution,aerodynamic properties,surface morphology,physical and chemical properties of PLLA PMs,and its successive drug-loaded conjugates,were detremined by various characterization techniques such as field emission-scanning electron microscope（FE-SEM）,Fourier transform infrared spectrophotometry（FTIR）,X-ray powder diffraction（XRPD）and differential scanning calorimetry（DSC）,among others. Further,the drug loading,as well as encapsulation efficiencies and DOX-release performance in vitro,were also investigated. The PLLA PMs resulted in decreased encapsulation efficiencies（56%,51%,and 44%）with the increase in drug loading efficiencies（2.9%,4.0% and 4.6%）. DOX-loaded PLLA PMs exhibited sustained-release profiles,in which the effect lasted more than 5 days. These porous microspheres can be used as an efficient platform due to their excellent aerodynamic properties and sustained release effect,which will potentially play a significant role in pulmonary drug delivery.