Preparation, characterization and anticoagulation of curcumin-eluting controlled biodegradable coating stents
Preparation, characterization and anticoagulation of curcumin-eluting controlled biodegradable coating stents
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DOI：
10.1016/j.jconrel.2006.08.023
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发表时间：
2006-11-10
影响因子：
10.8
通讯作者：
Huang, N.
中科院分区：
文献类型：
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作者：
Pan, Ch. J.;Tang, J. J.;Huang, N.
姜黄素在许多方面具有药理活性，具有抗凝血、抗增殖、抗炎等特性，可用于制造药物洗脱支架，以治疗支架植入后的支架内再狭窄。本文研究了以生物可降解聚合物PLGA（聚乳酸-共羟基乙酸）为药物载体，采用超声喷涂法在316L不锈钢支架表面均匀制备姜黄素洗脱型PLGA涂层。研究了三种剂量——低剂量（类似于每个支架140 μ g或115 μ g/cm(2)）、中等剂量（类似于每个支架280 μ g或230 μ g/cm(2)）和高剂量（类似于每个支架490 μ g或408 μ g/cm(2)）。通过光学显微镜（OM）和扫描电镜（SEM）对支架涂层的膨胀前和膨胀后形貌进行了检测，表明涂层不仅非常光滑均匀，而且能够承受支架在膨胀过程中施加的压缩和拉伸应变而不产生裂纹。原子力显微镜（AFM）图像显示，仅plga和中剂量姜黄素洗脱支架的形貌显示平均粗糙度低于1 nm；支架表面未见药物颗粒，说明采用超声雾化喷雾的方法可以在分子水平上将姜黄素与PLGA混合。利用傅里叶变换红外光谱（FTIR）和x射线电子能谱（XPS）对膜的结构进行了表征，结果表明姜黄素与药物之间没有发生化学反应。姜黄素洗脱支架体外释药测试结果表明，所研究的姜黄素洗脱支架均呈现近似线性的缓释曲线，在测量期内无明显的爆裂释药。通过静态血小板粘附和APTT （activated partial thromboplastin time）试验研究姜黄素洗脱支架的体外抗凝行为，发现姜黄素洗脱支架的抗凝性能优于不锈钢支架和纯plga涂层支架。随着给药剂量的增加，姜黄素支架的抗凝性能明显改善。(c) 2006 Elsevier B.V.版权所有
Curcumin is pharmaceutically active in many ways, having properties including anticoagulation, anti-proliferation, anti-inflammatory, and may be used to fabricate drug-eluting stents to treat in-stent restenosis after stent implantation. Here we describe our investigations of curcumin-eluting PLGA coatings formed using the biodegradable polymer PLGA (polylactic acid-co-glycolic acid) as drug carrier and uniformly fabricated on the surface of 316L stainless steel stents by an ultrasonic spray method. Three doses were explored - low dose (similar to 140 mu g per stent or 115 mu g/cm(2)) moderate dose (similar to 280 mu g per stent or 230 mu g/cm(2)), and high dose (similar to 490 mu g per stent or 408 mu g/cm(2)). Pre- and post-expansion morphologies of the stent coating were examined by optical microscopy (OM) and scanning electron microscopy (SEM), indicating that the coating not only was very smooth and uniform but also had the ability to withstand the compressive and tensile strains imparted without cracking from the stent during the expansion process. Atomic force microscopy (AFM) images indicated the topography of the PLGA-only and moderate dose curcumin-eluting stent that showed an average roughness below 1 nm; no drug particles could be seen on the stent surface, indicating that curcumin can be mixed with PLGA at the molecular level using an ultrasonic atomization spray method. The structure of the coating films was characterized by Fourier Transform Infrared (FTIR) spectroscopy and X-ray electron spectroscopy (XPS), with results suggesting that there was no chemical reaction between curcumin and the drug. The results of in vitro measurements of drug release from curcumin-eluting stents showed that all the curcumin-eluting stents studied exhibited a nearly linear sustained-release profile with no significant burst releases within the measurement period. The in vitro anticoagulation behavior of curcumin-eluting stents was investigated by static platelet adhesion and APTT (activated partial thromboplastin time) tests, revealing that the anticoagulation properties of curcumin-eluting stents are superior to those for stainless steel stents and PLGA-only-coated stents. The anticoagulation behavior of curcumin stents improved significantly as the drug dose was increased. (c) 2006 Elsevier B.V. All rights reserved.