Selective targeting of anti-cancer drug and simultaneous image enhancement in solid tumors by arterially administered lipid contrast medium

Abstract

Twenty‐four patients with various solid tumors including metastatic liver cancer and cancer of the lung, gallbladder, and pancreas were treated with a lipophilic macromolecular drug, copoly(styrene‐maleic acid) conjugated neocarzinostatin (SMANCS). The drug was dissolved in a lipid contrast medium Lipiodol and administered by catheterizing the respective feeding arteries under x‐ray monitoring. The advantages of this therapy include: (1) selective deposition of Lipiodol with the anti‐cancer drug in the target tumor, (2) a pronounced and long‐lasting anti‐cancer effect, (3) enhanced visulization of the tumor on x‐ray examinations for a prolonged period which also facilitated the long‐term follow‐up, (4) semiquantitative evaluation of the dosage regimen by x‐ray examination before further administration, (5) general applicability due to procedural simplicity, and (6) little side effect. Since the amount of Lipiodol and SMANCS used per administration for a patient (1.0–5.0 ml; 1.0–5.0 mg) was far less that the anticipated toxicity (LD₅₀ of Lipiodol = 95 ml/60 kg, dog, intravenously; and that of SMANCS = 3.4 mg/kg, mouse, IV), no deleterious effects to such critical organs as the brain, heart, lung, liver, or kidneys were observed upon radiologic and general clinical examination.