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吡非尼酮药物缓释载体PTMAc-PEG-PTMAc水凝胶制备与体外实验
Authors
余敏斌
全大萍
+5 more
吴开力
彭蔚
杨扬帆
林羡钗
王涛
Publication date
1 January 2019
Publisher
Editorial Office of Journal of Sun Yat-sen University
Abstract
【目的】以PTMAc-PEG-PTMAc三嵌段(PPP)水凝胶为吡非尼酮(PFD)药物缓释载体,评价其药物缓释性能。观察PFD载药水凝胶对人眼Tenon′s囊成纤维细胞(HTF)增殖抑制作用。【方法】制备PPP水凝胶;研究其溶胀率及其影响因素;光学显微镜观察水凝胶(载药与空载)中人眼Tenon′s囊成纤维细胞(HTF)的形态学改变;直接接触法进行PPP载药水凝胶进行体外释药实验。通过测定浓度、计算累积药物释放量,绘制出两种水凝胶体外药物释放曲线。CCK-8法检测不同浓度不同时间点水凝胶材料对细胞活力的影响及载药水凝胶体外抑制HTF增殖。【结果】PPP水凝胶成胶稳定。扫描电镜显示水凝胶呈现三维立体网孔状结构。水凝胶具有溶胀特性。溶胀率随水凝胶材料浓度增加而减少。在体外释药试验显示在前4d有明显的药物突释,此后缓慢释药直至第14天达到平衡。增加载药浓度,减少凝胶体积将明显增加药物累积缓释量;显微镜观察PPP水凝胶有抑制HTF细胞黏附作用;PPP水凝胶与HTF相互作用24、48、72、96h观察细胞活力分别为85.7%、93.0%、82.0%、81.6%,水凝胶不同方位HTF细胞形态不尽相同;水凝胶对细胞有抑制细胞黏附作用。两组不同载药浓度(1mg/mL和2mg/mL)载药水凝胶在24、48、72、96h这4个时间点细胞增殖抑制率分别为25.8%、21.8%、55.4%、25.6%;44.6%、35.9%、55.5%、31.4%。而1mg/mLPFD溶液在24、48、72、96h这4个时间点细胞增殖抑制率分别为28.9%、29.7%,7.8%、7.7%。【结论】PPP水凝胶具备良好药物缓释性能,载吡非尼酮水凝胶能明显抑制HTF增殖且较含等量药物溶液长效
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Last time updated on 16/10/2024