A brief overview of the general, retrometabolic drug design principles, inc
luding soft drug and chemical delivery system design, is presented. Selecte
d recent developments within these fields are also summarized, including re
sults related to the design of soft bufuralol and amiodarone analogues, to
the airway activity of loteprednol etabonate, a soft corticosteroid, and to
the brain targeted delivery of some neuropeptides.