Systemically injected porphyrins and other tetrapyrrolic compounds associate with serum proteins. Highly hydrophobic photosensitizers are mainly associated with lipoproteins and are deposited in intracellular loci of the neoplastic tissue. Hydrophilic photosensitizers are preferentially bound by serum albumin that releases the dye in the vascular stroma of the tumor. As a consequence the type of photosensitizer carrier determines different mechanisms of PDT-induced tumor necrosis. Low-density lipoproteins (LDL) may increase the selectivity of tumor targeting by releasing the bound dye to the neoplastic cells by a receptor-mediated endocytotic mechanism.