Abstract
A major challenge confronting pharmaceutical chemists in the future will be the design of drug candidates having structural characteristics adequate to circumvent the biological barriers [e. g., intestinal mucosa, liver, blood-brain barrier (BBB)] that often prevent the clinical development of potentially useful drug candidates (Audus and Raub, 1993). Through rational drug design, medicinal chemists are capable of synthesizing very potent and very specific drug candidates (Morgan and Gainer, 1989; Greenlee, 1990; Huff, 1991; Doherty, 1992; Bondinell et al., 1994). These drug candidates are developed with molecular characteristics that permit optimal interaction with the specific macromolecules (e. g., receptors, enzymes) that mediate their pharmacological effects. However, rational drug design, as currently practiced in many pharmaceutical companies, does not necessarily ensure optimal delivery of the drug to its site of action. Optimal delivery can be achieved by incorporating the drug candidate into a delivery system (e. g., formulation strategies) and/or by designing the drug candidate to have the structural characteristics (rational drug design strategies) that will provide optimal transfer between the point of administration and the pharmacological target in the body (Lee, 1991).
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Borchardt, R.T., Smith, P.L., Wilson, G. (1996). General Principles in the Characterization and Use of Model Systems for Biopharmaceutical Studies. In: Borchardt, R.T., Smith, P.L., Wilson, G. (eds) Models for Assessing Drug Absorption and Metabolism. Pharmaceutical Biotechnology, vol 8. Springer, Boston, MA. https://doi.org/10.1007/978-1-4899-1863-5_1
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