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尼氟酸结肠靶向小球的制备与体外释药评价
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篇名: 尼氟酸结肠靶向小球的制备与体外释药评价
TITLE:
摘要: 目的:制备尼氟酸结肠靶向小球,并进行体外释药评价。方法:将尼氟酸包载于D-α-维生素E聚乙二醇1000琥珀酸酯(TPGS1000 )中形成纳米胶束,考察尼氟酸纳米胶束的包封率、载药量、粒径、Zeta电位和多分散系数(PDI)。再采用锐孔-凝固法将纳米胶束包裹于低酯果胶中形成尼氟酸结肠靶向小球,观察尼氟酸结肠靶向小球的外观形态,计算其粒径和跨距。比较尼氟酸纳米胶束和尼氟酸结肠靶向小球依次在人工胃液(2 h)、人工小肠液(3 h)和人工结肠液(3 h)中的释药情况。结果:尼氟酸纳米胶束包封率为(93.42±2.33)%、载药量为(8.54±0.36)%(n=3),粒径为(25.8±0.6) nm、Zeta电位为(-18.73±0.23) mV(n=20),PDI为0.25。尼氟酸结肠靶向小球外形圆整,表面纹理粗糙,其粒径为(1.33±0.14) mm(n=3),跨距为0.26。尼氟酸纳米胶束在前5 h内的累积释放度已超过60%,而尼氟酸结肠靶向小球在前5 h内的累积释放度<30%,二者8 h内的累积释放度均>80%。结论:该制备方法简单可行,成功制得具有良好的结肠靶向性能的尼氟酸小球。
ABSTRACT: OBJECTIVE: To prepare Niflumic acid colon-targeted delivery beads, and to evaluate in vitro drug release. METHODS: Niflumic acid-loaded nanomicelles were prepared with D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS1000) as carrier material. Entrapment efficiency, drug-loading amount, particle size, Zeta potential and polydispersity coefficient (PDI) of Niflumic acid-loaded nanomicelles was investigated. The nanomicelles were encapsulated into pectin by using piercing-solidifying method to form Niflumic acid colon-targeted delivery beads. The morphology of Niflumic acid colon-targeted delivery beads was observed, and particle size and span was calculated. The drug release of Niflumic acid-loaded nanomicelles and Niflumic acid colon-targeted delivery beads in artificial gastric juice (2 h), artificial intestinal fluid (3 h) and artificial colon fluid (3 h) were compared. RESULTS: The encapsulation efficiency of Niflumic acid-loaded nanomicelles was (93.42±2.33)%, drug-loading amount was (8.54±0.36)%; particle size was (25.8±0.6) nm (n=3); Zeta potential was (-18.73±0.23) mV (n=20); PDI was 0.25. Niflumic acid colon-targeted delivery beads were round in appearance and rough in texture; the particle size was (1.33±0.14) mm (n=3) and span was 0.26. Accumulative release rate of Niflumic acid-loaded nanomicelles was more than 60% within first 5 h. Accumulative release rate of Niflumic acid colon-targeted delivery beads was lower than 30% within first 5 h, and accumulative release rate were both higher than 80% in 8 h. CONCLUSIONS: The preparation method is simple and reliable.  Niflumic acid colon-targeted delivery beads are prepared successfully.
期刊: 2018年第29卷第15期
编辑: 鄢雪梨,黄仁杰,肖健
AUTHORS: YAN Xueli,HUANG Renjie,XIAO Jian
关键字: 尼氟酸;纳米胶束;D-α-维生素E聚乙二醇1000琥珀酸酯;结肠靶向小球;制备;体外释药
KEYWORDS: Niflumic acid; Nanomicelles; D-α-tocopheryl polyethylene glycol 1000 succinate; Colon-targeted delivery beads; Preparation; in vitro drug release
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