To stay competitive in today’s challenging business environment, drug delivery technologies are needed that offer positive differentiation over first-generation commercial products [1, 2]. In formulations intended for oral administration, poorly water-soluble API’s, classified according to the Biopharmaceutical Classification System as Class II (BCS class II), may suffer from an inadequate, or highly variable, rate and/or extent of drug absorption (sometimes as a function of food in the stomach, i.e., fed/fasted variability).
The scientific and patent literature is replete with examples of where reducing the particle size of an active pharmaceutical ingredient (API) results in increased bioavailability [3-5]. Importantly, however, particle size reduction of API’s will also significantly increase the specific surface area and so further enhance the rate and extent of drug absorption such that the bioavailability requirements of the drug are met [6, 7]. Any increase in efficacy can reduce the potential toxicity (because less drug substance is needed). There is also a growing body of evidence that, specifically with nanoparticulate materials, it is the surface area and not particle size that is the defining metric that controls toxicological interaction [8-10].
The creation of API’s that are “nano-size” offers additional advantages that are not attainable with typical micronized drug products. A recent article, by Morigi, et al , discusses the financial drivers responsible for the intense interest and tremendous patent activity in nanotechnology-based drug delivery and targeting. The commercial success of this approach is attributed to the improved biological performance and compliance, which in turn may give rise to patentable technologies – a key metric for investors.
In this article, we will differentiate from the typical technical reviews and give a historic perspective of nanotechnology and then discuss some of the challenges involved in translating nanotechnology from the bench to pharmaceutical market.