ABSTRACT
INTRODUCTION As the pharmaceutical industry continues to develop improved techniques for chemical synthesis, high throughput screening, and computer modeling software, medicinal chemists are able to produce new molecular entities with elevated therapeutic potential quickly and effectively. Often, these drugmolecules show great potential for improved therapeutic outcomes; however, these present a variety of challenges to the formulating scientist. Increased lipophilicity and molecular weight and a corresponding decrease in solubility in physiological media are major hurdles that reduce the overall bioavailability of many of these drugs. It is widely accepted that 40% of new drugs developed exhibit poor dissolution and low solubility in aqueous media, leading to reduced therapeutic effect or bioavailability. Bioavailability can be broken down, most simply, into a combination of two characteristics of the therapeutic molecule: solubility and permeability. Indeed, bioavailability has been demonstrated to be amuchmore complicated concept, as described byWuandBenet (1), involving potential drug instability, elimination criteria, active transport, andvarious organmetabolisms. These additional concerns add to a need for production and formulation methods to improve basic principles of drug delivery-solubility and permeability.
