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

doi:10.16085/j.issn.1000-6613.2017-1852

Abstract

Abstract: 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.

Key words: doxorubicin, porous microspheres, poly-L-lactide, in vitro release, pulmonary drug delivery

摘要： 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。

关键词: 阿霉素, 多孔微球, 聚乳酸, 体外释放, 肺部给药

CLC Number:

R318

HONG Yazhen, ZHU Lihui. Synthesis,characterization and in vitro drug release performance of poly-L-lactide porous microspheres[J]. Chemical Industry and Engineering Progress, 2018, 37(03): 1130-1136.

洪雅真, 朱利会. 载阿霉素聚乳酸多孔微球的表征及释药性能[J]. 化工进展, 2018, 37(03): 1130-1136.

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