ISSN:
1573-904X
Keywords:
transdermal drug delivery
;
prediction of percutaneous absorption
;
permeability
;
maximum flux
;
sunscreens
Source:
Springer Online Journal Archives 1860-2000
Topics:
Chemistry and Pharmacology
Notes:
Abstract Purpose. The goal of this study was to quantify the transdermally absorbed amounts of the sunscreens octyl dimethyl p-aminobenzoic acid, oxybenzone, 4-isopropyl-dibenzoylmethane, 3-(4-methylben-zylidene)-camphor, isoamyl-4-methoxycinnamate, the repellent and plasticizer dibutyl phthalate, the antioxidant 3.5-di-t-butyl-4-hydroxyanisol, and the antimicrobial compounds butyl-4-hydroxybenzoate, biphenyl-2-ol, and 2,4,4′-tri-chlor-2′-hydroxydiphenylether (tri-closane). Permeabilities P B and maximum fluxes J max should be correlated with relevant physicochemical properties. Methods. Saturated solutions of the above-mentioned compounds in a propylene glycol/water mixture were applied to the skin using glass chambers which were fixed to the upper arms of volunteers. Maximum fluxes were calculated from concentration decreases in the vehicle. Results. A linear relationship between the logarithms of permeabilities P B of the penetrants (0.02–0.28 cm h−l) and the corresponding octanol/vehicle partition coefficients PC Oct/v (166–186,208) was found. Consequently, the influence of aqueous boundary layers could be neglected. However, the slope of the resulting straight line of 0.38 is considerably smaller than unity indicating that PC Oct/v does not represent the lipophilicity of the stratum corneum adequately. Maximum fluxes range from 0.5 to 130 µg cm−2 h−1. A general equation for the calculation of J max was derived based on experimental data taking into account the PC Oct/v and the solubilities c sV of the respective penetrants in the vehicle.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1023/A:1016286026462
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