The results of fundamental and applied studies of blood-brain barrier had been conducted by authors during the last 10 years are summarized in the publication. The molecular anatomy of barrier microvessels, as well as promising markers of BBB and other proteins involved in barrier functions are discussed. Via in vitro experiments with endothelial cells of cerebral microvessels we characterized the basic conditions required for adequate BBB modeling. The in vivo data of BBB permeability for macromolecules in normal and different pathological process is including radiation injury, hyperosmotic shock, and nervous tissue ischemia are properly described. A particular attention was focused upon the experimental studies of the permeability and functional reorganization of barrier endothelium during tumor neoangiogenesis. We detected a dramatically increased permeability of neoplastic microvessels both for horseradish peroxidase/serum albumin and labeled monoclonal antibodies. The increased tumor permeability for IgG and the overexpression of target antigens in tumor tissue and peritumoral zone make possible the targeted delivery of diagnostics and therapeutic agents into the tumor by means of monoclonal antibodies.

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