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首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >Coating of indomethacin-loaded embolic microspheres for a successful embolization therapy
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Coating of indomethacin-loaded embolic microspheres for a successful embolization therapy

机译：吲哚美辛栓塞微球的包衣成功栓塞治疗

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Indomethacin-loaded dietheylaminoethyl trisacryl~R microspheres (DEAE-MS), originally designed for therapeutic embolization, were encapsulated using two methods: coacervation and solvent evaporation/extraction. This encapsulation was achieved using a biocompatible polymer, the PLGA 50:50, and aimed to control the release of the anti-inflammatory non-steroidal drug (AINSD) in the occluded vessel. PLGA degradation study showed that it had an erosion half-life of ～35 days. Scanning electron microscopy (SEM) photographs showed that microcapsules (MC) prepared by coacervation had a wrinkled surface while those prepared using solvent-removal process showed non-porous, smooth surface, those of originally DEAE-MS showed a macro-porous, rough surface. The mean diameters were 61 μm for naked DEAE-MS vs. 71 μm and 65 μm for MC prepared by coacervation and solvent evaporation/extraction method, respectively. In vitro release study of indomethacin adsorbed onto MS indicated that drug release from MC was controlled by a diffusion process. Indomethacin diffusivity from MC was much lower than its free diffusivity from MS (mean 14.5 and 10.5 times lower for formulations prepared by coacervation and solvent evaporation/extraction method, respectively). This indicates that efficient indomethacin concentrations could be maintained over much longer time-periods in the embolized region, which is assumed to be beneficial in inhibiting normally occurring inflammatory reaction and the subsequent revascularization; responsible for treatment failure when definitive occlusion is required.
机译：最初设计用于治疗性栓塞的吲哚美辛负载的二甲基氨基乙基三丙烯酸R微球（DEAE-MS）采用凝聚和溶剂蒸发/萃取两种方法进行封装。这种封装是使用生物相容性聚合物PLGA 50:50实现的，其目的是控制抗炎非甾体药物（AINSD）在闭塞血管中的释放。 PLGA降解研究表明其腐蚀半衰期约为35天。扫描电子显微镜（SEM）照片显示，凝聚法制备的微囊（MC）表面起皱，而脱溶剂法制备的微囊表面无孔，表面光滑，原始DEAE-MS的微囊表面大孔，表面粗糙。裸露的DEAE-MS的平均直径分别为61μm，而通过凝聚和溶剂蒸发/萃取法制备的MC的平均直径分别为71μm和65μm。吲哚美辛吸附在MS上的体外释放研究表明，MC释放的药物受扩散过程控制。吲哚美辛从MC的扩散率远低于其从MS的自由扩散率（对于通过凝聚和溶剂蒸发/萃取法制备的制剂而言，分别低14.5和10.5倍）。这表明在栓塞区域中可以在更长的时间内保持有效的消炎痛浓度，这被认为对抑制正常发生的炎症反应和随后的血管重建是有益的。当需要确定性闭塞时，应对治疗失败负责。

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