Bioavailability of Intravenous Formulations of P-Boronophenylalanine in Dog and Rat

LaHann, T. R.; Lü, Donghao; Daniell, G.W.Bampfylde; Sills, C.; Kraft, Susan L.; Gavin, Patrick R.; Bauer, William F.

doi:10.1007/978-1-4615-2978-1_118

Cited by 11 publications

(4 citation statements)

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“…The allometric equation for BSH clearance was CLB~H (L h-') = 0 . 129 W (kg)o'68 (4) Considering the similarities in the exponents, these two equations may be easily combined. Rewriting (3) to adjust the units,…”

Section: Discussionmentioning

confidence: 99%

Interspecies pharmacokinetic scaling of BSH in mice, rats, rabbits, and humans

Mehta

Lü

1995

Biopharm & Drug Disp

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Sodium mercaptoundecahydrododecaborate or BSH is an important compound for boron neutron capture therapy (BNCT). The total clearance and steady state volume of distribution of BSH in humans and in laboratory animals were analyzed as a function of species body weight using the allometric equation for interspecies scaling. Significant linear relationships were obtained between log CLt (Lh-1) and log W (kg) (r = 0.972; p = 0.028) as well as log VSS (L) and log W (kg) (r = 0.999; p = 0.0005). The corresponding allometric equations were CLt = 0.127 W0.68 and VSS = 1.557 W0.87, respectively. BSH clearance in various species was shown to be a constant fraction (0.26) of creatinine clearance, the relationship being independent of body weight. Thus BSH clearance in various species occurred at similar pace when measured by a physiological parameter (creatinine clearance) rather than chronological time. Interspecies scale-up of plasma concentration-time data for the four species using a complex Dedrick plot resulted in similar profiles. Our results indicate that the BSH data obtained in laboratory animals could be utilized to generate preliminary estimates of the pharmacokinetic parameters in humans. These parameters can serve as guidelines for better planning of clinical studies.

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Section: Discussionmentioning

confidence: 99%

Interspecies pharmacokinetic scaling of BSH in mice, rats, rabbits, and humans

Mehta

Lü

1995

Biopharm & Drug Disp

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“…BPA ( l ‐enantiomer, >98% 10 B enriched; Boron Biologicals, Inc., Raleigh, NC, USA) containing 4.9% 10 B by weight was used as the boron delivery agent. Solutions of the BPA‐fructose complex were prepared in keeping with the procedures published previously (32). Hamsters in group 4 were administered BPA as an i.p.…”

Section: Tumor Induction and In Vivo Bnctmentioning

confidence: 99%

Insight into the mechanisms underlying tumor response to boron neutron capture therapy in the hamster cheek pouch oral cancer model

Aromando

Heber

Trivillin

et al. 2009

J Oral Pathology Medicine

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“…For BNCT to be successful, the boron concentration in the tumor is required to be at least 20 μg of 10 B/g of tissue .…”

Section: Introductionmentioning

confidence: 99%

Combined Cryogenic Transmission Electron Microscopy and Electron Spin Resonance Studies of Egg Phosphatidylcholine Liposomes Loaded with a Carboranyl Compound Intended for Boron Neutron Capture Therapy

et al. 2003

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The lactosyl carborane [1,2-dicarba-closo-dodecarboran(12)-1-ylmethyl](β-d-galactopyranosyl)-(1→4)-β-gluco-pyranoside (LCOB) is an amphipilic boron-containing compound intended for boron neutron capture therapy. In this study cryogenic transmission electron microscopy was used to investigate the effects of LCOB on the structure and properties of extruded egg phosphatidylcholine liposomes. The results showed that LCOB concentrations up to at least x LCOB = 0.25 could be included in the preparations without any noticeable effects on the liposomal size or structure. Inclusion of LCOB concentrations corresponding to x LCOB = 0.44 or more gave, however, rise to significant changes in the liposome size distribution and the overall sample structure. In fresh samples no signs of phospholipid solubilization were detected until the molar fraction of LCOB reached 0.82. At this concentration the boronated compound induced, however, formation of open liposomes and threadlike micelles and, furthermore, with time the sample displayed a macroscopic phase separation. More details on the molecular interaction between LCOB and the liposome membranes were obtained by electron spin resonance spectroscopy. Two different n-doxyl stearic acid spin probes were used to measure the dynamics and the degree of order in the mixed systems. The results indicated that LCOB insertion into the phospholipid bilayer increased the packing order in the vicinity of the water/hydrocarbon interface whereas the inner hydrophobic region of the bilayer was unaffected.

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Bioavailability of Intravenous Formulations of P-Boronophenylalanine in Dog and Rat

Cited by 11 publications

References 1 publication

Interspecies pharmacokinetic scaling of BSH in mice, rats, rabbits, and humans

Interspecies pharmacokinetic scaling of BSH in mice, rats, rabbits, and humans

Insight into the mechanisms underlying tumor response to boron neutron capture therapy in the hamster cheek pouch oral cancer model

Combined Cryogenic Transmission Electron Microscopy and Electron Spin Resonance Studies of Egg Phosphatidylcholine Liposomes Loaded with a Carboranyl Compound Intended for Boron Neutron Capture Therapy

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