Mechanism of drug release from double-walled PDLLA(PLGA) microspheres.

Mechanism of drug release from double-walled PDLLA(PLGA) microspheres.
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DOI:
10.1016/j.biomaterials.2013.02.015
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发表时间:
2013-05
期刊:
影响因子:
14
通讯作者:
Pack, Daniel W.
Pack, Daniel W.
中科院分区:
工程技术1区
文献类型:
--
作者:
Xu, Qingxing;Chin, Shi En;Wang, Chi-Hwa;Pack, Daniel W.

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研究了两种双壁微球制剂的药物释放和降解行为,所述双壁微球制剂由多柔比星负载的聚(D,L-乳酸-共-乙醇酸)(PLGA)核(~46 kDa)和聚(D,L-乳酸)(PDLLA)壳层(~55和116 kDa)包围。据推测,不同分子量的壳层可以调节外涂层的侵蚀,并限制在不同时间尺度上水渗透到载药内核中的发生,从而控制药物从微球中的释放。对于两种微球制剂,观察到药物释放曲线相似。监测微球的降解约9周,并使用扫描电子显微镜、激光扫描共聚焦显微镜和凝胶渗透色谱法进行分析。有趣的是,尽管形成壳层的PDLLA分子量不同,但两种微球制剂在相似的时间尺度上表现出PDLLA的本体侵蚀的发生。双壁微球的壳层作为一个有效的扩散屏障,在最初的滞后期,并控制独立的壳层的分子量的亲水性药物的释放速率。
The drug release and degradation behavior of two double-walled microsphere formulations consisting of a doxorubicin loaded poly(D,L-lactic-co-glycolic acid) (PLGA) core (~46 kDa) surrounded by a poly(D,L-lactic acid) (PDLLA) shell layer (~55 and 116 kDa) were examined. It was postulated that different molecular weights of the shell layer could modulate the erosion of the outer coating and limit the occurrence of water penetration into the inner drug-loaded core on various time scales, and therefore control the drug release from the microspheres. For both microsphere formulations, the drug release profiles were observed to be similar. The degradation of the microspheres was monitored for a period of about nine weeks and analyzed using scanning electron microscopy, laser scanning confocal microscopy, and gel permeation chromatography. Interestingly, both microsphere formulations exhibited occurrence of bulk erosion of PDLLA on a similar time scale despite different PDLLA molecular weights forming the shell layer. The shell layer of the double-walled microspheres served as an effective diffusion barrier during the initial lag phase period and controlled the release rate of the hydrophilic drug independent of the molecular weight of the shell layer.
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