Jores Katja, Mehnert Wolfgang, Drechsler Markus, Bunjes Heike, Johann Christoph, Mäder Karsten
Institute of Pharmacy, Department of Pharmaceutical Technology, Free University of Berlin, Kelchstr. 31, 12169 Berlin, Germany.
J Control Release. 2004 Mar 5;95(2):217-27. doi: 10.1016/j.jconrel.2003.11.012.
Recently, colloidal dispersions made from mixtures of solid and liquid lipids were described to combine controlled release characteristics with higher drug loading capacities than solid lipid nanoparticles (SLN). It has been proposed that these nanostructured lipid carriers (NLC) are composed of oily droplets which solubilize the drug and which are embedded in a solid lipid matrix. The structures of SLN and NLC based on glyceryl behenate and medium chain triglycerides were characterized by photon correlation spectroscopy (PCS) and laser diffraction (LD), field-flow fractionation (FFF) with multi-angle light scattering detection (MALS), and cryo transmission electron microscopy (cryo TEM). PCS indicates that SLN and NLC differ from a nanoemulsion with respect to Brownian motion due to asymmetric particle shapes. Non-spherical particles, in case of SLN and NLC, lead to higher polydispersity indices compared to the nanoemulsion. In FFF, the nanodroplets elute much earlier than SLN- and NLC-platelets although their PCS and LD data show similar particle sizes. In TEM platelet (for SLN), oil loaded platelet ("nanospoons"; for NLC) and droplet (for nanoemulsion) structures were observed. In contrast to literature reports, the investigated SLN appear as thin platelets. NLC are found to be lipid platelets with oil spots sticking on the surface. Very short diffusion pathways in platelets, increased water-lipid interfaces and low drug incorporation in crystalline lipids are the drawback of SLN and NLC compared to conventional nanoemulsions.
最近,有人描述了由固体和液体脂质混合物制成的胶体分散体,它具有控释特性,且药物载量高于固体脂质纳米粒(SLN)。有人提出,这些纳米结构脂质载体(NLC)由油性液滴组成,这些液滴可溶解药物并嵌入固体脂质基质中。基于山嵛酸甘油酯和中链甘油三酯的SLN和NLC的结构通过光子相关光谱法(PCS)、激光衍射法(LD)、带多角度光散射检测(MALS)的场流分级法(FFF)以及冷冻透射电子显微镜法(冷冻TEM)进行了表征。PCS表明,由于颗粒形状不对称,SLN和NLC在布朗运动方面与纳米乳剂不同。对于SLN和NLC,非球形颗粒导致的多分散指数高于纳米乳剂。在FFF中,纳米液滴的洗脱时间比SLN和NLC血小板早得多,尽管它们的PCS和LD数据显示颗粒大小相似。在TEM中观察到了血小板结构(对于SLN)、载油血小板结构(“纳米勺”;对于NLC)和液滴结构(对于纳米乳剂)。与文献报道相反,所研究的SLN呈现为薄血小板状。发现NLC是表面附着有油斑的脂质血小板。与传统纳米乳剂相比,血小板中极短的扩散路径、增加的水-脂质界面以及结晶脂质中低的药物掺入量是SLN和NLC的缺点。