In vitro evaluation of a series of N-dodecanoyl-L-amino acid methyl esters as dermal penetration enhancers

Timothy K. Fincher, Sun D. Yoo, Mark R. Player, J. Walter Sowell, Bozena Michniak-Kohn

Research output: Contribution to journalArticle

18 Citations (Scopus)

Abstract

A series of N-dodecanoyl-L-amino acid methyl esters (1-10) and n-pentyl N-acetylprolinate (11) were evaluated for dermal enhancement properties using an in vitro diffusion cell technique. Methods of synthesis of these compounds were described. Enhancers were applied 1 h prior to drug treatment. Hydrocortisone was used as the model drug and was applied to excised hairless mouse skin as a saturated suspension in propylene glycol. Enhancement ratios (ER) were determined for permeability coefficient, 24 h diffusion cell receptor concentration (Q24), and 24 h full-thickness skin steroid content. Controls received no enhancer pretreatment of the skin. N-Dodecanoyl-L- proline (10) showed the highest Q24 value for total steroid (ER 13.7) while N-dodecanoyl-L-phenylalanine (5) showed the highest total steroid skin retention (ER 16.5).

Original languageEnglish (US)
Pages (from-to)920-923
Number of pages4
JournalJournal of Pharmaceutical Sciences
Volume85
Issue number9
DOIs
StatePublished - Jan 1 1996
Externally publishedYes

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Esters
Amino Acids
Skin
Steroids
Hairless Mouse
Propylene Glycol
Phenylalanine
Proline
Pharmaceutical Preparations
Hydrocortisone
Permeability
Suspensions
In Vitro Techniques

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science

Cite this

Fincher, Timothy K. ; Yoo, Sun D. ; Player, Mark R. ; Sowell, J. Walter ; Michniak-Kohn, Bozena. / In vitro evaluation of a series of N-dodecanoyl-L-amino acid methyl esters as dermal penetration enhancers. In: Journal of Pharmaceutical Sciences. 1996 ; Vol. 85, No. 9. pp. 920-923.
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abstract = "A series of N-dodecanoyl-L-amino acid methyl esters (1-10) and n-pentyl N-acetylprolinate (11) were evaluated for dermal enhancement properties using an in vitro diffusion cell technique. Methods of synthesis of these compounds were described. Enhancers were applied 1 h prior to drug treatment. Hydrocortisone was used as the model drug and was applied to excised hairless mouse skin as a saturated suspension in propylene glycol. Enhancement ratios (ER) were determined for permeability coefficient, 24 h diffusion cell receptor concentration (Q24), and 24 h full-thickness skin steroid content. Controls received no enhancer pretreatment of the skin. N-Dodecanoyl-L- proline (10) showed the highest Q24 value for total steroid (ER 13.7) while N-dodecanoyl-L-phenylalanine (5) showed the highest total steroid skin retention (ER 16.5).",
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In vitro evaluation of a series of N-dodecanoyl-L-amino acid methyl esters as dermal penetration enhancers. / Fincher, Timothy K.; Yoo, Sun D.; Player, Mark R.; Sowell, J. Walter; Michniak-Kohn, Bozena.

In: Journal of Pharmaceutical Sciences, Vol. 85, No. 9, 01.01.1996, p. 920-923.

Research output: Contribution to journalArticle

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