Miswan Zulaika, Lukman Siti Khadijah, Abd Majid Fadzilah Adibah, Loke Mun Fai, Saidin Syafiqah, Hermawan Hendra
Faculty of Biosciences and Medical Engineering, Universiti Teknologi Malaysia, 81310 Johor Bahru, Malaysia.
Faculty of Biosciences and Medical Engineering, Universiti Teknologi Malaysia, 81310 Johor Bahru, Malaysia; Department of Mining, Metallurgical and Materials Engineering & CHU de Québec Research Center, Laval University, Quebec City, G1V 0A6, Canada.
Int J Pharm. 2016 Dec 30;515(1-2):460-466. doi: 10.1016/j.ijpharm.2016.10.056. Epub 2016 Oct 26.
Active ingredients of ginsenoside, Rg1 and Re, are able to inhibit the proliferation of vascular smooth muscle cells and promote the growth of vascular endothelial cells. These capabilities are of interest for developing a novel drug-eluting stent to potentially solve the current problem of late-stent thrombosis and poor endotheliazation. Therefore, this study was aimed to incorporate ginsenoside into degradable coating of poly(lactic-co-glycolic acid) (PLGA). Drug mixture composed of ginseng extract and 10% to 50% of PLGA (xPLGA/g) was coated on electropolished stainless steel 316L substrate by using a dip coating technique. The coating was characterized principally by using attenuated total reflectance-Fourier transform infrared spectroscopy, scanning electron microscopy and contact angle analysis, while the drug release profile of ginsenosides Rg1 and Re was determined by using mass spectrometry at a one month immersion period. Full and homogenous coating coverage with acceptable wettability was found on the 30PLGA/g specimen. All specimens underwent initial burst release dependent on their composition. The 30PLGA/g and 50PLGA/g specimens demonstrated a controlled drug release profile having a combination of diffusion- and swelling-controlled mechanisms of PLGA. The study suggests that the 30PLGA/g coated specimen expresses an optimum composition which is seen as practicable for developing a controlled release drug-eluting stent.
人参皂苷的活性成分Rg1和Re能够抑制血管平滑肌细胞的增殖,并促进血管内皮细胞的生长。这些特性对于开发一种新型药物洗脱支架以潜在解决当前晚期支架血栓形成和内皮化不良的问题具有重要意义。因此,本研究旨在将人参皂苷掺入聚乳酸-乙醇酸共聚物(PLGA)的可降解涂层中。通过浸涂技术将由人参提取物和10%至50%的PLGA(xPLGA/g)组成的药物混合物涂覆在电解抛光的316L不锈钢基底上。主要通过衰减全反射傅里叶变换红外光谱、扫描电子显微镜和接触角分析对涂层进行表征,同时在浸泡一个月期间使用质谱法测定人参皂苷Rg1和Re的药物释放曲线。在30PLGA/g样品上发现了具有可接受润湿性的完全且均匀的涂层覆盖。所有样品都经历了取决于其组成的初始突释。30PLGA/g和50PLGA/g样品表现出具有PLGA扩散和溶胀控制机制相结合的控释药物释放曲线。该研究表明,30PLGA/g涂层样品表现出一种最佳组成,这对于开发控释药物洗脱支架而言被认为是可行的。