Evaluation of a novel sodium borocaptate-containing unnatural amino acid as a boron delivery agent for neutron capture therapy of the F98 rat glioma

Table 1 Summary of Boron biodistribution in F98 glioma bearing rats

				Boron concentrations ± SD(μg¹⁰B/g)									Ratios^b
Agent	Route	Time^a(h)	n	Blood			Brain			Tumor			T/Bl	T/Br
ACBC-BSH	CED^c ^200μl/24h	1	3	3.3	±	2.2	1.5	±	1.3	21.1	±	3.3	6.4	14.2
		6	3	1.3	±	0.0	0.4	±	0.3	17.8	±	10.1	13.7	42.4
		24	3	0.5	±	0.1	0.0	±	0.0	0.0	±	0.1	0.1	1.4
	i.v.^d	1	4	6.3	±	1.7	0.2	±	0.0	2.7	±	0.5	0.4	14.9
	i.v.^d	6	3	7.0	±	3.4	0.3	±	0.1	6.0	±	1.7	0.9	18.6
BPA	CED^e ^200μl/24h	1	3	0.5	±	0.3	0.1	±	0.1	10.1	±	4.1	23	125.2
		6	2	2.0	±	0.9	0.7	±	0.1	8.9	±	3.7	4.4	13.7
		24	3	0.4	±	0.3	0.0	±	0.0	0.1	±	0.2	0.4	7
	i.v.^f	1	3	8.5	±	0.3	3.0	±	0.6	19.7	±	1.4	2.3	6.7
	i.v.^f	6	3	4.1	±	1.3	3.1	±	1.3	14.4	±	3.4	3.6	4.7
BSH	CED^g ^200μl/24h	1	3	0.9	±	0.7	0.3	±	0.2	12.2	±	5.6	13.6	40.7
		6	3	1.8	±	0.5	0.3	±	0.5	15.8	±	7.7	8.8	52.7
		24	3	1.6	±	0.3	0.1	±	0.0	1.4	±	0.3	0.9	14.0
	i.v.^h	1	3	10.3	±	3.3	0.1	±	0.1	2.0	±	1.3	0.2	20.0
	i.v.^h	6	3	2.0	±	0.3	0.1	±	0.0	0.5	±	0.0	0.3	5.0

ACBC α-aminocyclobutane-1-carboxylic acid, CED convection-enhanced delivery, SD standard deviation, BPA p-boronphenylalanine, BSH dodecaboranethiol, iv intravenous
^aTime to euthanize rats after boron compound administration
^bT/Bl indicates the tumor to blood ratio and T/Br indicates the tumor to normal brain ratio
^cACBC-BSH was administered by long term CED in volume of 200 μl for 24 h at a dose of 1.2 mg¹⁰B/kg b.w
^dACBC-BSH was administered i.v. at a dose of 12 mg10B/kg b.w
^eBPA was administered by long term CED in volume of 200 μl for 24 h at a dose of 1.2 mg¹⁰B/kg b.w
^fBPA was administered i.v. at a dose of 12 mg¹⁰B/kg b.w (= 250 mgBPA/kg b.w)
^gBSH was administered by long term CED in volume of 200 μl for 24 h at a dose of 1.2 mg¹⁰B/kg b.wl
^hBSH was administered i.v. at a dose of 12 mg¹⁰B/kg b.w

ISSN: 1748-717X