[Usefulness of local administration of methotrexate bound to activated carbon particles (MTX-CH)].
We developed a new dosage formulation, methotrexate bound to activated carbon particles (MTX-CH), and used it to reduce tumors via its long-acting effect at the administration sites. MTX-CH was injected locally into tumors on the back of BALB/c mice, 30 mg/mouse, as MTX and compared with mice treated with MTX aqueous solution, saline solution, activated carbon particles (CH-40) and non-treated mice. The MTX concentration at the administration sites was higher in the MTX-CH group than in the MTX aqueous solution group. A marked effect on the control of tumor growth by MTX-CH was noted after repeated administration (every 3 days, total 4 times) throughout the observation period. Although tumor size was not reduced, necrosis was microscopically observed around the site of MTX-CH administration. For the reasons mentioned above, MTX-CH is superior to MTX aqueous solution in terms of long-acting effect at the administration sites and the control of tumor growth.
Ito
T
T
Dept. of Digestive Surgery, Kyoto Prefectural University of Medicine.
Takagi
T
T
Shimomura
K
K
Takemura
M
M
Toma
A
A
Fujiyama
J
J
Sonoyama
Y
Y
Sakakura
C
C
Ootsuji
E
E
Hagiwara
A
A
Yamagishi
H
H
D000818:Animals; D000964:Antimetabolites, Antineoplastic / Q000008:administration & dosage* / Q000493:pharmacokinetics; D002244:Carbon; D003692:Delayed-Action Preparations; D008297:Male; D008727:Methotrexate / Q000008:administration & dosage* / Q000493:pharmacokinetics; D051379:Mice; D008807:Mice, Inbred BALB C; D009374:Neoplasms, Experimental / Q000188:drug therapy* / Q000378:metabolism
D000964:Antimetabolites, Antineoplastic; D003692:Delayed-Action Preparations; D002244:Carbon; D008727:Methotrexate