Background: Long-term survival and curve can not he achieved in patien
ts with unresectable metastatic liver cancer. In this study, to improv
e the antitumor activity of oily anticancer agents, which enable targe
ted cancer chemotherapy, various concentrations of vinblastine dissolv
ed in Lipiodol ultrafluid (vinblastin/Lipiodol U) or Lipiodal F, which
has three times the viscosity of Lipiodol ultrafluid, were used. Mate
rials and Methods: Rabbits bearing VX2 tumors measuring I to 2 cm in d
iameter in the liver received arterial injections of 0.2 ml of these d
rugs, and antitumor activity were examined. Results: Complete necrosis
of the tumor was observed in three of nine rabbits received vinblasti
ne/Lipiodol U at 2.5 mg/ml. Complete necrosis of the tumor was observe
d in all eleven rabbits which received vinblastine/Lipiodol U at 5 mg/
ml. At concentrations of 7.5 and 10 mg/ml, the necrotic area spread fr
om the tumor to the liver parenchyma surrounding the tumor. The antitu
mor activity of vinblastine dissolved in Lipiodol F was increased comp
ared with that of vinblastine dissolved in Lipiodol ultrafluid. Conclu
sions: The antitumor activity of a kind of the oily anticancer agents,
vinblastine/Lipiodol increased with increasing amounts of vinblastine
dissolved in Lipiodol ultrafluid and with the increasing viscosity of
the carrier, Lipiodol.