Biodistribution of BPA and BSH after single, repeated and simultaneous administrations for neutron-capture therapy of cancer.
The effect of administration mode of L-BPA and BSH on the biodistribution in the melanoma-bearing hamsters was investigated. In single intravenous (i.v.) administration, BSH (100 mg BSH/kg) showed no significant retention of (10)B in all the tissues, including tumors, while long-term retention of (10)B in the tumor, muscle and brain was observed with L-BPA (500 mg BPA/kg). The dose escalation of L-BPA and the simultaneous single administration of L-BPA and BSH were not so effective at increasing boron accumulation in tumor after bolus i.v. injection. The boron concentration in tumor was 41 microg B/g after single bolus i.v. injection even at the dose of 1000 mg BPA/kg. In contrast, two sequential bolus i.v. injections of l-BPA with the dose of 500 mg BPA/kg each was found to be effective at increasing (10)B accumulation in the tumor; the maximum (10)B concentration in the tumor reached 52 microg B/g at 3 h after the second i.v. injection.
Ichikawa
H
H
Faculty of Pharmaceutical Sciences and Cooperative Research Center of Life Sciences, Kobe Gakuin University, 1-1-3 Minatojima, Chuo-ku, Kobe 650-8586, Japan. ichikawa@pharm.kobegakuin.ac.jp
Taniguchi
E
E
Fujimoto
T
T
Fukumori
Y
Y
D000818:Animals; D001894:Borohydrides / Q000008:administration & dosage* / Q000493:pharmacokinetics* / Q000627:therapeutic use; D001895:Boron / Q000493:pharmacokinetics; D001896:Boron Compounds / Q000008:administration & dosage* / Q000493:pharmacokinetics* / Q000627:therapeutic use; D016754:Boron Neutron Capture Therapy / Q000379:methods*; D006224:Cricetinae; D005260:Female; D007554:Isotopes / Q000493:pharmacokinetics; D008546:Melanoma, Experimental / Q000378:metabolism* / Q000532:radiotherapy*; D008647:Mesocricetus; D010649:Phenylalanine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000627:therapeutic use; D011838:Radiation-Sensitizing Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics* / Q000627:therapeutic use; D013438:Sulfhydryl Compounds / Q000008:administration & dosage* / Q000493:pharmacokinetics* / Q000627:therapeutic use; D014018:Tissue Distribution
D001894:Borohydrides; D001896:Boron Compounds; D007554:Isotopes; D011838:Radiation-Sensitizing Agents; D013438:Sulfhydryl Compounds; C014651:mercaptoundecahydrododecaborate; D010649:Phenylalanine; D001895:Boron; C033685:4-boronophenylalanine