Graduate Institute of Biomedical Materials and Tissue Engineering, College of Oral Medicine, Taipei, Taiwan.
Int J Nanomedicine. 2013;8:3455-66. doi: 10.2147/IJN.S48465. Epub 2013 Sep 11.
The utilization of self-microemulsifying premicroemulsion systems (SMEPMS) as templates for preparing poorly water-soluble compounds in the nanosized range represents a promising strategy. Fenofibrate was formulated with n-butyl L-lactate, Tween 80, and a number of cosurfactants (ethanol, 1-propanol, and PEG 600), diluted with the water phase (either water or saccharide solution) and then subjected to a freeze-drying (FD) process to obtain SMEPMS nanosized particulates. Results demonstrated that the particle size after resuspension of these FD SMEPMS nanosized particulates in water was too large, so the addition of saccharide solutions (lactose, mannitol, glucose, sucrose, and trehalose) as the solid carrier to prevent particles from aggregating seemed to be necessary and workable due to steric hindrance and repulsion. However, instability of these resuspended FD nanosized particulates after 30-90 minutes still occurred, and the addition of 0.5% sodium lauryl sulfate in the resuspending medium was able to retard the aggregation and maintain the particle size within the nano-range. Evaluation by scanning electron microscopy and X-ray powder diffraction also confirmed the results. It was concluded that using an SMEPMS formulation with PEG 600 as the cosurfactant, and in the presence of a suitable saccharide as an anticaking agent and FD process were able to produce fenofibrate nanoparticles.
自微乳前药系统 (SMEPMS) 作为模板用于制备纳米级范围内难溶性化合物具有广阔的应用前景。本文采用丁酸乙酯、吐温 80 和一些助表面活性剂（乙醇、1-丙醇和 PEG600）来制备非诺贝特的自微乳前药系统纳米颗粒，用水或糖溶液稀释，然后进行冷冻干燥（FD），得到 SMEPMS 纳米颗粒。结果表明，将这些 FD SMEPMS 纳米颗粒重新混悬于水中后，粒径过大，因此需要添加糖溶液（乳糖、甘露醇、葡萄糖、蔗糖和海藻糖）作为固体载体来防止颗粒聚集，这可能是因为空间位阻和排斥作用。然而，重新混悬的 FD 纳米颗粒在 30-90 分钟后仍不稳定，在重新混悬介质中添加 0.5%的十二烷基硫酸钠可以延缓聚集并保持粒径在纳米范围内。扫描电子显微镜和 X 射线粉末衍射的评估结果也证实了这一点。研究结论表明，采用含有 PEG600 的 SMEPMS 配方，并添加适当的糖作为防结块剂和 FD 工艺，能够制备非诺贝特纳米颗粒。
