Physical chemical considerations of lipid-based oral drug delivery--solid lipid nanoparticles.

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. Copyright 2004 Begell House, Inc.