Department of Pharmaceutics, College of Pharmacy, Shandong University, Jinan, PR China.
J Microencapsul. 2010 May;27(3):234-41. doi: 10.3109/02652040903079526.
In order to improve drug entrapment efficiency and loading capacity, nanostructured lipid carriers consisting of solid lipid and liquid lipid as a new type of colloidal drug delivery system were prepared. The dispersions of oridonin-loaded solid lipid nanoparticles and nanostructured lipid carriers were successfully prepared by the emulsion-evaporation and low temperature-solidification technique using monostearin as the solid lipid, caprylic/capric triglycerides as the liquid lipid and oridonin as the model drug. Their physicochemical properties of oridonin-loaded nanostructured lipid carriers and release behaviours were investigated and compared with those of solid lipid nanoparticles. As a result, the mean particle size was approximately 200 nm with narrow polydispersity index lower than 0.4 for all developed formulations. Zeta potential values were in the range -35 mV approximately -50 mV, providing good physical stability of all formulations. The differential scanning calorimetry and X-ray diffraction analysis results demonstrated lipid nanoparticles exhibited crystal order disturbance and thus left more space to accommodate drug molecules. The improved drug entrapment efficiency and loading capacity were observed for nanostructured lipid carriers and they enhanced with increasing the caprylic/capric triglycerides content. In vitro drug release experiments exhibited biphasic drug release patterns with burst release initially and prolonged release afterwards. These results indicated that nanostructured lipid carriers could potentially be exploited as a delivery system with improved drug entrapment efficiency and controlled drug release.
为了提高药物包封效率和载药量，采用固态脂质和液态脂质作为新型胶体药物传递系统的纳米结构脂质载体被制备。通过乳化蒸发和低温固化技术，以单硬脂酸甘油酯作为固态脂质、辛酸/癸酸三酸甘油酯作为液态脂质和冬凌草甲素作为模型药物，成功制备了冬凌草甲素固体脂质纳米粒和纳米结构脂质载体的分散体。考察并比较了载冬凌草甲素的纳米结构脂质载体的理化性质和释放行为与固体脂质纳米粒的差异。结果表明，所有制剂的平均粒径约为 200nm，多分散指数均低于 0.4。Zeta 电位值在-35mV 至-50mV 范围内，为所有制剂提供了良好的物理稳定性。差示扫描量热法和 X 射线衍射分析结果表明，脂质纳米粒表现出晶体有序性的紊乱，从而为药物分子提供了更多的容纳空间。纳米结构脂质载体的药物包封效率和载药量得到提高，且随着辛酸/癸酸三酸甘油酯含量的增加而增加。体外药物释放实验显示出双相药物释放模式，初始突释，随后持续释放。这些结果表明，纳米结构脂质载体有望作为一种药物包封效率提高和药物释放控制的新型给药系统。
