Bunjes Heike, Steiniger Frank, Richter Walter
Department of Pharmaceutical Technology, Institute of Pharmacy, Friedrich Schiller University Jena, Lessingstrasse 8, 07743 Jena, Germany.
Langmuir. 2007 Mar 27;23(7):4005-11. doi: 10.1021/la062904p. Epub 2007 Feb 23.
Colloidal suspensions of triglycerides are under investigation as potential drug carrier systems. The properties of the matrix lipids are altered in the nanoparticles compared to those of the bulk material. For instance, the metastable alpha-modification of the triglycerides usually transforms into the stable beta-polymorph quite rapidly in the colloidal particles. Recently, it was observed that the alpha-modification can be preserved for a considerable period of time in tristearin nanoparticles when the particles are stabilized with a blend of saturated long-chain phospholipids and the bile salt sodium glycocholate [Bunjes, H.; Koch, M. H. J. J. Controlled Release 2005, 107, 229-243]. As triglyceride nanoparticles in the alpha-modification may offer some advantages over those in the beta-form with regard to drug delivery applications, the structure of the corresponding dispersions was investigated in more detail with differential scanning calorimetry, X-ray diffraction, and electron microscopy. The electron microscopic investigations confirmed a platelet-like, layered structure for particles in the beta-modification and revealed a spheroidal shape with concentric layers for larger particles in the alpha-form. For the first time, not only was information on the internal structure of solid triglyceride nanoparticles obtained from freeze-fracture electron micrographs but also details were observed by cryoelectron microscopy.
甘油三酯的胶体悬浮液作为潜在的药物载体系统正在研究中。与块状材料相比,纳米颗粒中基质脂质的性质发生了改变。例如,甘油三酯的亚稳α-晶型在胶体颗粒中通常会相当迅速地转变为稳定的β-多晶型。最近观察到,当颗粒用饱和长链磷脂和胆盐甘氨胆酸钠的混合物稳定时,α-晶型可以在硬脂酸甘油酯纳米颗粒中保留相当长的一段时间[Bunjes, H.; Koch, M. H. J. 控制释放杂志2005, 107, 229 - 243]。由于在药物递送应用方面,α-晶型的甘油三酯纳米颗粒可能比β-晶型的具有一些优势,因此用差示扫描量热法、X射线衍射和电子显微镜对相应分散体的结构进行了更详细的研究。电子显微镜研究证实了β-晶型颗粒的片状层状结构,并揭示了α-晶型较大颗粒的具有同心层的球状形状。首次不仅从冷冻断裂电子显微照片获得了固体甘油三酯纳米颗粒内部结构的信息,而且通过低温电子显微镜观察到了细节。