Ian Wark Research Institute, University of South Australia, Mawson Lakes Campus, Mawson Lakes, South Australia, Australia, 5095.
Nanomedicine (Lond). 2014 Dec;9(18):2745-59. doi: 10.2217/nnm.14.37.
To investigate the role of self-emulsifying lipids and porous silica particles in enhancing supersaturated drug loading and biopharmaceutical performance of nanostructured silica-lipid hybrid (SLH) systems.
MATERIALS & METHODS: Two lovastatin (LOV)-SLHs were engineered from self-emulsifying lipid (Gelucire(®) 44/14; Gattefossé, Lyon, France) and Aerosil(®) 380 (SLH-A; Evonik Industries, Essen, Germany) or Syloid(®) 244FP silica (SLH-S; Grace Davison Discovery Sciences, Rowville, Australia).
RESULTS & DISCUSSION: The LOV-SLHs encapsulated LOV at 10% w/w, which is ≥3-fold higher than typical lipid formulations in the absence of porous silica. The LOV-SLHs retained self-emulsifying lipid-associated solubilization benefits and improved drug solubilization by twofold in simulated intestinal condition. SLH-S, with larger surface area (299 m(2)/g), was superior to SLH-A (184 m(2)/g) in optimizing oral bioavailability, suggesting a critical role of the silica geometry. Bioavailability of SLH-S was 2.8- and 1.3-fold higher than pure drug and drug suspension in Gelucire 44/14, respectively.
In conclusion, SLHs profit from advantages associated with both self-emulsifying lipids and porous silica, and provide potentially improved therapy against coronary artery disease.
研究自乳化脂质和多孔硅颗粒在提高纳米结构硅脂质混合（SLH）系统的超饱和药物负载和生物药剂学性能中的作用。
两种洛伐他汀（LOV）-SLH 是由自乳化脂质（Gelucire（®）44/14；Gattefossé，里昂，法国）和 Aerosil（®）380（SLH-A；Evonik Industries，埃森，德国）或 Syloid（®）244FP 硅（SLH-S；Grace Davison Discovery Sciences，罗威尔，澳大利亚）制成的。
LOV-SLH 封装 LOV 的浓度为 10%（w/w），是不存在多孔硅时典型脂质制剂的 3 倍以上。LOV-SLH 保留了自乳化脂质相关的增溶益处，并在模拟肠道条件下将药物溶解度提高了两倍。表面积更大（299 m（2）/g）的 SLH-S 比 SLH-A（184 m（2）/g）更能优化口服生物利用度，表明硅的几何形状起着关键作用。SLH-S 的生物利用度分别比纯药物和药物混悬液在 Gelucire 44/14 中的生物利用度高 2.8 倍和 1.3 倍。
总之，SLH 受益于自乳化脂质和多孔硅的优势，为治疗冠状动脉疾病提供了潜在的改善方法。
