Souto E B, Müller R H, Gohla S
Department of Pharmaceutical Technology, Biotechnology and Quality Management, The Free University of Berlin, Berlin, Germany.
J Microencapsul. 2005 Sep;22(6):581-92. doi: 10.1080/02652040500162378.
This study describes the development, preparation and characterization of solid lipid nanoparticles (SLN) containing the novel anti-ageing substance alpha-lipoic acid. Lipoic acid is chemically labile, i.e. the degradation products possess an unpleasant odour. Therefore, the active was encapsulated in SLN. A lipid with low melting point (Softisan 601) was selected for preparation of active-loaded SLN after screening the solubility of alpha-lipoic acid in physicochemically different lipids. An entrapment efficiency of 90% (UV analysis) was obtained for all developed formulations using Miranol Ultra C32 as emulsifying agent. Particle size stability was monitored during 3 months storing the samples at 20 degrees C and at 4 degrees C. Results of DSC analysis confirm that these systems are characterized by a solid-like behaviour, although with a very low crystallinity index.
本研究描述了含有新型抗衰老物质α-硫辛酸的固体脂质纳米粒（SLN）的开发、制备及特性。硫辛酸在化学上不稳定，即其降解产物具有难闻的气味。因此，将该活性成分包封于固体脂质纳米粒中。在筛选了α-硫辛酸在物理化学性质不同的脂质中的溶解度后，选择了一种低熔点脂质（Softisan 601）来制备负载活性成分的固体脂质纳米粒。使用Miranol Ultra C32作为乳化剂，所有开发的制剂的包封率均达到90%（紫外分析）。在20℃和4℃下储存样品3个月期间监测了粒径稳定性。差示扫描量热法（DSC）分析结果证实，这些体系具有类似固体的行为特征，尽管结晶度指数非常低。
