Literature DB >> 1924136

Quantitative evaluation of ethanol effects on diffusion and metabolism of beta-estradiol in hairless mouse skin.

P Liu1, W I Higuchi, W Q Song, T Kurihara-Bergstrom, W R Good.   

Abstract

The influence of low levels of ethanol on the simultaneous diffusion and metabolism of beta-estradiol (E2 beta) in hairless mouse skin was quantitatively evaluated. A wide range of diffusion/metabolism experiments was conducted with full-thickness skin, stripped skin, and dermis at the various ethanol levels. The experiments were carried out in a two-chamber diffusion-cell system where ethanol was present in both the donor and the receiver chambers at equal concentrations. Analysis of the experimental data with several enzyme distribution models further showed that the best model was that for which the enzyme activity resided totally in the epidermis and near the basal layer of the epidermis. The ethanol effects were separated and quantified in terms of the diffusion and metabolism parameters. Aqueous ethanol, even at low concentrations (greater than or equal to 25%), was found to have two important effects on E2 beta transport: ethanol functions as an inhibitor of the enzymatic conversion of E2 beta to estrone (E1) in the viable epidermis, and ethanol is able to enhance the transport of permeants across the lipoidal pathway of the stratum corneum.

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Year:  1991        PMID: 1924136     DOI: 10.1023/a:1015847311266

Source DB:  PubMed          Journal:  Pharm Res        ISSN: 0724-8741            Impact factor:   4.200


  6 in total

1.  17 -Hydroxysteroid dehydrogenase of rat skin. Substrate specificity and inhibitors.

Authors:  B P Davis; E Rampini; S L Hsia
Journal:  J Biol Chem       Date:  1972-03-10       Impact factor: 5.157

2.  Dose-related effects of a single dose of ethanol on the metabolism in rat liver of some aromatic and chlorinated hydrocarbons.

Authors:  A Sato; T Nakajima; Y Koyama
Journal:  Toxicol Appl Pharmacol       Date:  1981-08       Impact factor: 4.219

3.  Permeation of hairless mouse skin I: Experimental methods and comparison with human epidermal permeation by alkanols.

Authors:  H Durrheim; G L Flynn; W I Higuchi; C R Behl
Journal:  J Pharm Sci       Date:  1980-07       Impact factor: 3.534

4.  Inhibition of drug metabolism by acute ethanol intoxication. A hepatic microsomal mechanism.

Authors:  E Rubin; H Gang; P S Misra; C S Lieber
Journal:  Am J Med       Date:  1970-12       Impact factor: 4.965

Review 5.  Drug kinetics and alcohol ingestion.

Authors:  E M Sellers; M R Holloway
Journal:  Clin Pharmacokinet       Date:  1978 Nov-Dec       Impact factor: 6.447

6.  Physical model evaluation of topical prodrug delivery-simultaneous transport and bioconversion of vidarabine-5'-valerate II: Parameter determinations.

Authors:  C D Yu; J L Fox; N F Ho; W I Higuchi
Journal:  J Pharm Sci       Date:  1979-11       Impact factor: 3.534

  6 in total
  8 in total

1.  Cotransport of estradiol and ethanol through human skin in vitro: understanding the permeant/enhancer flux relationship.

Authors:  P Liu; T Kurihara-Bergstrom; W R Good
Journal:  Pharm Res       Date:  1991-07       Impact factor: 4.200

2.  Analysis of simultaneous transport and metabolism of ethyl nicotinate in hairless rat skin.

Authors:  K Sugibayashi; T Hayashi; T Hatanaka; M Ogihara; Y Morimoto
Journal:  Pharm Res       Date:  1996-06       Impact factor: 4.200

3.  Vitamin D3-based conjugates for topical treatment of psoriasis: synthesis, antiproliferative activity, and cutaneous penetration studies.

Authors:  Shimon Ben-Shabat; Rachel Benisty; Uri Wormser; Amnon C Sintov
Journal:  Pharm Res       Date:  2005-01       Impact factor: 4.200

4.  Diffusion and metabolism of prednisolone farnesylate in viable skin of the hairless mouse.

Authors:  K Tojo; K Yamada; T Hikima
Journal:  Pharm Res       Date:  1994-03       Impact factor: 4.200

5.  Binding of prednisolone and its ester prodrugs in the skin.

Authors:  T Hikima; K Tojo
Journal:  Pharm Res       Date:  1997-02       Impact factor: 4.200

Review 6.  Pharmacokinetic characterisation of transdermal delivery systems.

Authors:  B Berner; V A John
Journal:  Clin Pharmacokinet       Date:  1994-02       Impact factor: 6.447

7.  Biotransformation of estradiol in the human keratinocyte cell line HaCaT: metabolism kinetics and the inhibitory effect of ethanol.

Authors:  R Altenburger; T Kissel
Journal:  Pharm Res       Date:  1998-11       Impact factor: 4.200

8.  Structure Enhancement Relationship of Chemical Penetration Enhancers in Drug Transport across the Stratum Corneum.

Authors:  Doungdaw Chantasart; S Kevin Li
Journal:  Pharmaceutics       Date:  2012-01-17       Impact factor: 6.321

  8 in total

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