ABSTRACT
Recently, with the applications of genomics, high-throughput screening, robot ics, combinatorial chemistry, informatics, and miniaturization to the drug-discovery area, far more drug candidates than ever have been generated for development (Lip per 1999). However, as a result of the preferred pharmacological activity process of drug discovery, which attem pts to maximize the activity, biopharm aceutical proper ties of new drug candidates, including water solubility, tend to suffer (Yamashita and Furubayashi 1998). It is noteworthy that a com pound with great receptor affinity and selectivity, but with poor biopharmaceutical properties for formulation or delivery, is
rarely regarded as ineligible to enter development. This viewpoint has prevailed in industry despite the potential for a com pound’s poor biopharm aceutical properties to be a major delay on the developm ent timeline (Lipper 1999). Compounds optimized solely on the basis of receptor-based potency, depending on the nature of the recep tor, are usually hydrophobic or water insoluble. Therefore, more and more problems have recently been experienced in the early formulation development of drugs (Sweetana and Akers 1996; Corswant, Thoren, and Engstrom 1998; Pace et al. 1999). Water insolubility can postpone or completely halt new drug development and can prevent the m uch needed reformulation of currently marketed products (Pace et al. 1999).
