The effect of solvents and hydrophilic additive on stable coating and controllable sirolimus release system for drug-eluting stent
The effect of solvents and hydrophilic additive on stable coating and controllable sirolimus release system for drug-eluting stent
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DOI：
10.1016/j.msec.2017.04.024
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发表时间：
2017-09-01
影响因子：
7.9
通讯作者：
Han, Dong Keun
中科院分区：
文献类型：
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作者：
Kim, Seong Min;Park, Sung-Bin;Han, Dong Keun
多种药物洗脱支架（DES）已被研发出来，用于预防支架植入后的再狭窄。然而，为了实现有效的临床治疗，DES仍需提高聚合物载药涂层的稳定性以及对药物释放的控制。在本研究中，通过使用超声喷涂系统，在钴铬（Co - Cr）合金表面涂覆可生物降解的聚（D,L - 丙交酯）（PDLLA）以及与亲水性普朗尼克F127添加剂混合的西罗莫司（SRL），以获得稳定的涂层表面并控制SRL的释放。研究了PDLLA/SRL涂层在生理溶液中的降解情况。发现添加F127可减少PDLLA的降解，并在60天内提高涂层的稳定性。还研究了氯仿和四氢呋喃（THF）等有机溶剂对涂层均匀性的影响。结果表明，与氯仿相比，THF能产生非常光滑且均匀的涂层。根据有机溶剂类型和亲水性添加剂的不同，体外药物释放模式为DES中可控药物释放设计提供了可能性。发现无论使用何种有机溶剂，使用F127时药物释放都是持续的。此外，与氯仿相比，THF能够实现更快且可控的释放曲线。利用超小角中子散射研究了SRL分子在不同有机溶剂中的结构。此外，SRL的结构在氯仿中具有浓度依赖性，在高浓度下性质紧密，但在THF中与浓度无关。这些结果有力地证明了涂层稳定性和药物释放模式可因有机溶剂、添加剂和涂层策略等各种参数的物理化学性质而改变。（C）2017爱思唯尔B.V.保留所有权利。
Various drug-eluting stents (DESs) have been developed to prevent restenosis after stent implantation. However, DES still needs to improve the drug-in-polymer coating stability and control of drug release for effective clinical treatment. In this study, the cobalt-chromium (Co-Cr) alloy surface was coated with biodegradable poly(D,L-lactide) (PDLLA) and sirolimus (SRL) mixed with hydrophilic Pluronic F127 additive by using ultrasonic spray coating system in order to achieve a stable coating surface and control SRL release. The degradation of PDLLA/SRL coating was studied under physiological solution. It was found that adding F127 reduced the degradation of PDLLA and improved the coating stability during 60 days. The effects of organic solvent such as chloroform and tetrahydrofuran (THF) on the coating uniformity were also examined. It was revealed that THF produced a very smooth and uniform coating compared to chloroform. The patterns of in vitro drug release according to the type of organic solvent and hydrophilic additive proposed the possibility of controllable drug release design in DES. It was found that using F127 the drug release was sustained regardless of the organic solvent used. In addition, THF was able to get faster and controlled release profile when compared to chloroform. The structure of SRL molecules in different organic solvents was investigated using ultra-small angle neutron scattering. Furthermore, the structure of SRL is concentration-dependent in chloroform with tight nature under high concentration, but concentration-independent in THE These results strongly demonstrated that coating stability and drug release patterns can be changed by physicochemical properties of various parameters such as organic solvents, additive, and coating strategy. (C) 2017 Elsevier B.V. All rights reserved.