Establishment of Evaluation Method for Function of Drug Targeting Systems and Systematization of their Physicochemical Character-Function Relationship

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Recently, drug targeting approaches have attracted great interest for optimization of drug delivery. The use of drug carriers is one of the most promising ways to accomplish the drug targeting. Great efforts have been made to develop carrier systems, however, most approaches are done through trial and error or based on only experiences. The purposes of this tesearch project were as follows. First, to establish the evaluation method for targeting systems. Second, to systematize the pharmacokinetic characteristics of drug carriers. Third, to establish the methodology for drug targeting. In order to study at whole body, organ, and cellular levels, in vivo distribution experiments, organ perfusion experiments, and in vitro experiments using cultured cells were carried out. Through these experiments, we have clarified the relationship between the pharmacokinetic characteristics of macromolecular and microparticulate carriers and their physicochemical properties, such as size and charge. Based on the findings, we have developed some targeting delivery systems of superoxide dismutase (antioxidant enzyme) and vitamin K5 (blood coagulant).