Bummer Paul M
University of Kentucky, College of Pharmacy, Lexington, Kentucky 40505, USA.
Crit Rev Ther Drug Carrier Syst. 2004;21(1):1-20.
Of all the methods employed by formulators when presented with the task of improving oral bioavailability, the use of lipid assemblies is perhaps the least understood. Nonetheless, lipid-based formulations, and in particular solid lipid nanoparticles (SLN), show great promise for enhancing the oral bioavailability of some of the most poorly absorbed compounds. The physical/chemical characteristics of lipid-based systems are highly complex because of the existence of a variety of lipid assembly morphologies, the morphology-dependent solubility of drug, the interconversion of assembly morphology as a function of time and chemical structure, and the simultaneous lipid digestion. The present work will center on recent studies of the relevant physicochemical characteristics of SLN, most notably solubility of the drug in the lipid matrix, location of the drug in the aggregate, drug release properties of the aggregate, and particle size stability. Strengths and weaknesses of the lipid assemblies, in particular solid lipid nanoparticles, in promoting drug delivery by the oral route for systemic or Peyer's patch uptake will be highlighted, and possible future research pathways will be suggested.
在配方设计师面临提高口服生物利用度的任务时所采用的所有方法中，脂质组装体的应用可能是最不为人所理解的。尽管如此，基于脂质的制剂，尤其是固体脂质纳米粒（SLN），在提高一些吸收最差的化合物的口服生物利用度方面显示出巨大的潜力。由于存在多种脂质组装形态、药物的形态依赖性溶解度、组装形态随时间和化学结构的相互转化以及同时发生的脂质消化，基于脂质的系统的物理/化学特性高度复杂。本工作将围绕固体脂质纳米粒相关物理化学特性的最新研究展开，最显著的是药物在脂质基质中的溶解度、药物在聚集体中的位置、聚集体的药物释放特性以及粒径稳定性。将突出脂质组装体，特别是固体脂质纳米粒，在促进口服途径药物递送以实现全身或派伊尔结摄取方面的优缺点，并提出未来可能的研究途径。
