Essential properties of drug-targeting delivery systems.

How, if at all, can drug delivery help to create ideal drugs? After four decades of trying, an effective site-specific drug-delivery system has not yet been developed. This review draws attention to the pharmacokinetic conditions that must be met to achieve a successful performance by site-selective drug-carrier delivery systems. In a drug-carrier approach, a drug is attached to a macromolecular carrier via a chemically labile linker. The carrier transports the drug to its site of action and releases it at the target site. For this simple approach to work, several fundamental conditions (nonspecific interactions, target site access, drug release and drug suitability) must be satisfied. The importance of these essential requirements, not always recognized in the development of drug-delivery systems, is discussed and illustrated by recent examples selected from the literature.