Free hematoporphyrin administered intravenously to healthy rabbits (1-28 mg/kg body weight) is bound by the 3 major lipoprotein components of plasma (VLDL, LDL and HDL) with different efficiency. In vitro-prepared complexes of hematoporphyrin (Hp) with lipoprotein fractions isolated from mouse serum have been injected intracardiacally into mice affected by MS-2 fibrosarcoma (1 mg of Hp per kg body weight). LDL appear to allow a more specific delivery of the complexed Hp to the tumor tissue as compared with HDL, VLDL or free Hp. The different behavior of VLDL, LDL and HDL as carriers of Hp in vivo is also discussed.