Synthesis of a nickel tetracarboranylphenylporphyrin for boron neutron-capture therapy: Biodistribution and toxicity in tumor-bearing mice

✍ Scribed by Michiko Miura; Peggy L. Micca; Craig D. Fisher; John C. Heinrichs; Jason A. Donaldson; Gerald C. Finkel; Daniel N. Slatkin

• Publisher: John Wiley and Sons
• Year: 1996
• Tongue: French
• Weight: 646 KB
• Volume: 68
• Category: Article
• ISSN: 0020-7136
• DOI: 10.1002/(sici)1097-0215(19960927)68:1<114::aid-ijc20>3.0.co;2-a

✦ Synopsis

Nickel-2,3,7,8,I2,I3,I7,I&uctaacetic acid-5,10, I5,20-tetra-[3cahmmyl-methoxyphe@rporphyrin octamethylester (NITCP) was given in a Cremophor EL, a polyethowylated castor oil, and propylene glycol emulsion to B A W c mice bearing transplanted S.C. KHJJ mammary carcinomas. A total dose of 244 pg NiTCP/ gram body weight (gbw) (54 pg B/gbw) was given in 6 i.p. injections over a 32 hr period. Observations of behavior and changes in body weight and chemical and hematological blood tests indicated little or no toxicity from NiTCP over a period of 6-90 hr after injections. Boron concentrations near tumor margins were 160-180 pg B/g at 41-90 hr after the last injection. Tumormormal brain boron concentration ratios reached approx. I 0 I and tumocblood ratios reached approx. 250 I after 4 days. There was no evidence of thromboqtopenia or other potentially impottant toxicities. Our findings place NiTCP among the leading candidates for pre-clinical experiments aimed toward improvement upon the compounds being tested for boron neutron-capture therapy of glioblastoma multifme.