Johnsson Markus, Barauskas Justas, Norlin Andreas, Tiberg Fredrik
Physical Chemistry 1, Lund University, P.O. Box 124, SE-221 00 Lund, Sweden.
J Nanosci Nanotechnol. 2006 Sep-Oct;6(9-10):3017-24. doi: 10.1166/jnn.2006.402.
Liquid crystalline nanoparticles (LCNP) formed through lipid self-assembly have a range of attractive properties as in vivo drug delivery carriers. In particular they offer: a wide solubilization spectrum, and consequently high drug payloads; effective encapsulation; stabilization and protection of sensitive drug substances. Here we present basic physicochemical features of non-lamellar LCNP systems with a focus on intravenous drug applications. This is exemplified by the formulation properties and in vivo behavior using the drug substance propofol; a well-known anesthetic agent currently used in clinical practice in the form of a stable emulsion. In order to appraise the drug delivery features of the LCNP system the current study was carried out with a marketed propofol emulsion product as reference. In this comparison the propofol-LCNP formulation shows several useful features including: higher drug-loading capacity, lower fat-load, excellent stability, modified pharmacokinetics, and an indication of increased effect duration.
通过脂质自组装形成的液晶纳米颗粒（LCNP）作为体内药物递送载体具有一系列吸引人的特性。特别是它们具有：广泛的增溶谱，因此药物载量高；有效的包封；敏感药物物质的稳定化和保护。在这里，我们介绍非层状LCNP系统的基本物理化学特征，重点是静脉内药物应用。以药物丙泊酚为例说明其制剂特性和体内行为；丙泊酚是一种目前在临床实践中以稳定乳剂形式使用的著名麻醉剂。为了评估LCNP系统的药物递送特性，本研究以市售的丙泊酚乳剂产品作为参考进行。在这种比较中，丙泊酚-LCNP制剂显示出几个有用的特性，包括：更高的载药能力、更低的脂肪负载、优异的稳定性、改变的药代动力学以及作用持续时间增加的迹象。
