背景：近年来将强的松龙应用于促进周围神经损伤后功能恢复取得了良好效果，但因半衰期短、局部应用血药浓度不稳定及较大的不良反应限制了其临床应用。目的：制备强的松龙纳米微球缓释膜并对其药物缓释特性进行检测。方法：采用反胶束乳化溶剂挥发法制备强的松龙纳米微球，对载药纳米微球的形态、粒径、载药量、包封率和体外释药行为等性质进行研究；同时将纳米微球与胶原、壳聚糖、大豆卵磷脂等膜材相结合，制得复合药膜，考察复合药膜的形貌、膜中材料的相互作用及药膜的体外释药行为。结果与结论：强的松龙纳米微球具有良好的微观结构，药物均匀分布于纳米微球中，纳米微球粒径均一，表面光滑，平均粒径500 nm，包封率达90%以上，体外缓释实验药物释放良好，存在一定的药物突释现象。观察球膜结合方法制得的复合膜，可见纳米微球均匀分散于复合膜中，复合膜微观结构良好，体外缓释实验见复合膜药物释放更加稳定，无明显药物突释现象出现，显示了良好的药物释放效果。表明通过反胶束乳化溶剂挥发法和球膜结合方法制备出的强的松龙缓释膜剂具有良好的药物缓释特性。%BACKGROUND:In recent years, the use of prednisolone has good achievements in functional recovery after peripheral nerve injury, but its short half-life, instable plasma concentrations and greater adverse reactions limit its clinical application. OBJECTIVE:To prepare prednisolone implantable films and to explore the sustained-release property of prednisolone implantable films. METHODS:Novel reverse micellar emulsion-solvent evaporation method was used to prepare nanoparticles which contains prednisolone, and we investigated the properties of prednisolone-loaded nanoparticles, including morphological form, diameter, drug loading, encapsulation efficiency, in vitro release properties. Then, composite film was prepared with the nanoparticles above and col agen, chitosan, soybean phosphatidylcholine. The properties of composite films, such as morphological form, the interaction among film materials, in vitro releasing curve, were investigated. RESULTS AND CONCLUSION:The prednisolone-loaded nanoparticles displayed favorable microstructure such as smooth surface, consistent diameters. The mean diameter of the nanoparticle was 500 nm and the max encapsulation efficiency of the nanoparticle was more than 90%. The nanoparticle displayed obvious sustained-release effect in vitro, but it exhibited a certain burst release phenomenon. We found that the nanoparticles were uniformly distributed inside and on the surface of the composite film;and the in vitro release rate of the film was slower and more stable than the nanoparticles. The composite film displayed favorable sustained-release effect with no burst release. From what we have il ustrated above, we can safely come to a conclusion that the prednisolone-loaded film possesses good sustained-release effects.
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