In vitro percutaneous absorption of boron as boric acid, borax, and disodium octaborate tetrahydrate in human skin: a summary.
Literature from the first half of this century reports concern for toxicity from topical use of boric acid, but assessment of percutaneous absorption has been impaired by lack of analytical sensitivity. Analytical methods in this study included inductively coupled plasma-mass spectrometry which now allows quantitation of percutaneous absorption of 10B in 10B-enriched boric acid, borax and disodium octaborate tetrahydrate (DOT) in biological matrices. In vitro human skin percent doses of boric acid absorbed were 1.2 for a 0.05% solution, 0.28 for a 0.5% solution, and 0.70 for a 5.0% solution. These absorption amounts translated into flux values of, respectively, 0.25, 0.58, and 14.58 microg/cm2/h, and permeability constants (Kp) of 5.0 x 10(-4), 1.2 x 10(-4), and 2.9 x 10(-4) cm/h for the 0.05%, 0.5%, and 5.0% solutions. The above in vitro doses were at infinite, 1000 microL/cm2 volume. At 2 microL/cm2 (the in vivo dosing volume), flux decreased some 200-fold to 0.07 microg/cm2/h and Kp of 1.4 x 10(-6) cm/h, while percent dose absorbed was 1.75%. Borax dosed at 5.0%/1000 microL/cm2 had 0.41 percent dose absorbed, flux at 8.5 microg/cm2/h, and Kp was 1.7 x 10(-4) cm/h. Disodium octaborate tetrahydrate (DOT) dosed at 10%/1000 microL/cm2 was 0.19 percent dose absorbed, flux at 7.9 microg/cm2/h, and Kp was 0.8 x 10(-4) cm/h. These in vitro results from infinite doses (1000 microL/cm2) were a 1000-fold greater than those obtained in the companion in vivo study. The results from the finite (2 microL/cm2) dosing were closer (10-fold difference) to the in vivo results. General application of infinite dose percutaneous absorption values for risk assessment is questioned by these results.
Department of Dermatology, University of California, San Francisco, USA.
R C
RC
Wester
T
T
Hartway
H I
HI
Maibach
M J
MJ
Schell
D J
DJ
Northington
B D
BD
Culver
P L
PL
Strong
D000328:Adult; D000368:Aged; D000704:Analysis of Variance; D001881:Borates / Q000493:pharmacokinetics*; D001888:Boric Acids / Q000493:pharmacokinetics*; D001895:Boron / Q000493:pharmacokinetics*; D015194:Diffusion Chambers, Culture / Q000295:instrumentation / Q000379:methods; D005260:Female; D006801:Humans; D066298:In Vitro Techniques; D007306:Insecticides / Q000493:pharmacokinetics*; D007554:Isotopes; D008297:Male; D013058:Mass Spectrometry; D008875:Middle Aged; D012680:Sensitivity and Specificity; D012869:Skin Absorption
D001881:Borates; D001888:Boric Acids; D007306:Insecticides; D007554:Isotopes; C018851:borax; D001895:Boron; C032688:boric acid; C077054:disodium octaborate tetrahydrate