化工进展 ›› 2018, Vol. 37 ›› Issue (03): 1130-1136.DOI: 10.16085/j.issn.1000-6613.2017-1852

• 生物与医药化工 • 上一篇    下一篇

载阿霉素聚乳酸多孔微球的表征及释药性能

洪雅真1,2, 朱利会1,2   

  1. 1 华侨大学化工学院, 福建 厦门 361021;
    2 华侨大学生物材料与组织工程研究所, 福建 厦门 361021
  • 收稿日期:2017-09-04 修回日期:2017-11-09 出版日期:2018-03-05 发布日期:2018-03-05
  • 通讯作者: 洪雅真(1988-),女,硕士,研究实习员,研究方向为生物材料。

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

HONG Yazhen1,2, ZHU Lihui1,2   

  1. 1 College of Chemical Engineering, Huaqiao University, Xiamen 361021, Fujian, China;
    2 Institute of Biomaterials and Tissue Engineering, Huaqiao University, Xiamen 361021, Fujian, China
  • Received:2017-09-04 Revised:2017-11-09 Online:2018-03-05 Published:2018-03-05

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

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

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