College of Chemistry, Chemical Engineering and Biotechnology, Donghua University, Shanghai 201620, PR China.
Int J Pharm. 2011 Apr 15;408(1-2):200-7. doi: 10.1016/j.ijpharm.2011.01.058. Epub 2011 Feb 1.
Eudragit® L 100-55 nanofibers loaded with diclofenac sodium (DS) were successfully prepared using an electrospinning process, and characterized for structural and pharmacodynamic properties. The influence of solvent and drug content on fiber formation and quality was also investigated. Fiber formation was successful using a solvent mixture 5:1 (v/v) ethanol:DMAc. XRD and DSC analysis of fibers confirm electron microscopic evidence that DS is evenly distributed in the nanofibers in an amorphous state. FTIR analysis indicates hydrogen bonding occurs between the drug and the polymer, which accounts for the molecular integration of the two components. In vitro dissolution tests verified that all the drug-loaded Eudragit® L 100-55 nanofibers had pH-dependent drug release profiles, with limited, less than 3%, release at pH 1.0, but a sustained and complete release at pH 6.8. This profile of properties indicates drug-loaded Eudragit® L 100-55 nanofibers have the potential to be developed as oral colon-targeted drug delivery systems.
载有双氯芬酸钠（DS）的 Eudragit® L 100-55 纳米纤维成功地通过静电纺丝工艺制备，并对其结构和药效性质进行了表征。还研究了溶剂和药物含量对纤维形成和质量的影响。使用 5:1（v/v）乙醇：DMAc 的溶剂混合物成功地形成了纤维。纤维的 XRD 和 DSC 分析证实了电子显微镜的证据，即 DS 以无定形状态均匀分布在纳米纤维中。FTIR 分析表明药物和聚合物之间发生氢键相互作用，这解释了两种成分的分子整合。体外溶解试验证实，所有载药的 Eudragit® L 100-55 纳米纤维在 pH 值依赖性药物释放曲线中，在 pH 值 1.0 时的药物释放量有限，小于 3%，但在 pH 值 6.8 时则持续且完全释放。这种性能特征表明，载药的 Eudragit® L 100-55 纳米纤维有可能被开发为口服结肠靶向药物传递系统。
