The role of solid nanoparticle technology in the parenteral delivery of poorly water-soluble drugs

Water insolubility has always been a key obstacle in pharmaceutical formulation, affecting formulation stability and drug bioavailability. Approaches for achieving complete dissolution often have disadvantages associated with the large quantities of required excipients. Small-particle suspensions (200 nm-2 mum), consisting essentially of pure drug, require only a minimum amount of surface-active agent for stabilization. Such suspensions may be formulated for rapid dissolution, thus achieving pharmacokinetic properties similar to those of a solution, or drug insolubility may be leveraged to afford prolonged in vivo release. In both situations, higher dosing may be possible than with a drug solution. This may afford enhanced efficacy at reduced excipient concentrations with potentially less toxicity. We present a brief introduction to the pharmaceutical technology of pure submicron drug particles in relationship to other dosage forms, and study examples are presented to underscore the potential benefits of this approach in parenteral delivery. (C) 2004 Elsevier B.V. All rights reserved.