Catalogo Articoli (Spogli Riviste)

OPAC HELP

Titolo:
Monohydroxylation and esterification as determinants of the effects of cis- and trans-9-octadecenoic acids on the permeation of hydrocortisone and 5-fluorouracil across hairless mouse skin in vitro
Autore:
Song, JF; Lau-Cam, CA; Kim, KH;
Indirizzi:
St Johns Univ, Coll Pharm & Allied Hlth Profess, Jamaica, NY 11439 USA St Johns Univ Jamaica NY USA 11439 ed Hlth Profess, Jamaica, NY 11439 USA
Titolo Testata:
INTERNATIONAL JOURNAL OF PHARMACEUTICS
fascicolo: 2, volume: 212, anno: 2001,
pagine: 153 - 160
SICI:
0378-5173(20010116)212:2<153:MAEADO>2.0.ZU;2-7
Fonte:
ISI
Lingua:
ENG
Soggetto:
PERCUTANEOUS-ABSORPTION ENHANCEMENT; REFLECTANCE INFRARED-SPECTROSCOPY; 2-LAYER DIFFUSION-MODEL; STRATUM-CORNEUM; FATTY-ACIDS; OLEIC-ACID; PENETRATION ENHANCEMENT; NONPOLAR ROUTES; IN-VIVO; INVITRO;
Keywords:
cis and trans 9-octadecenoic acids; monohydroxylation; esterification; hydrocortisone; 5-fluorouracil; skin permeation;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
28
Recensione:
Indirizzi per estratti:
Indirizzo: Kim, KH St Johns Univ, Coll Pharm & Allied Hlth Profess, Jamaica, NY 11439USA St Johns Univ Jamaica NY USA 11439 Profess, Jamaica, NY 11439 USA
Citazione:
J.F. Song et al., "Monohydroxylation and esterification as determinants of the effects of cis- and trans-9-octadecenoic acids on the permeation of hydrocortisone and 5-fluorouracil across hairless mouse skin in vitro", INT J PHARM, 212(2), 2001, pp. 153-160

Abstract

The effects of cis-9-octadecenoic acid (oleic acid) and of a group of chemically related cis- (ricinoleic acid) and trans- (ricinelaidic acid) 12-monohydroxylated derivatives and their corresponding ethyl and methyl esters on the skin permeation of model hydrophobic (hydrocortisone, log K = 1.61) and hydrophilic (5-fluorouracil, log K = - 0.89) drugs was investigated in vitro using excised hairless mouse skin. Drug solutions were prepared in propylene glycol, with and without the addition of a fatty acid to a level of 5%. Whereas the addition of oleic acid markedly enhanced the transdermal flux of both drugs relative to a sample in propylene glycol alone (hydrocortisone similar to 1800-fold; 5-fluorouracil similar to 330-fold), that of a cis- or trans-12-monohydroxylated analog of oleic acid resulted in only a small increase (1.4-2.7-fold for hydrocortisone; 4.4-6.6-fold for 5-fluorouracil). On the other hand, the methyl and ethyl eaters of cis- and trans-12-hydroxy-9-octadecenoic acid exerted a much greater enhancing effect (327-720-fold for hydrocortisone, 42-74-fold for 5-fluorouracil) than the corresponding parent fatty acids. Furthermore, whereas the ethyl esters were found to have a greater effect on the skin permeation of hydrocortisone than the methyl esters, the reverse was true with regards to 5-fluorouracil. Additionally, the esters of trans-12-hydroxy-9-octadecenoic acid promoted permeation to an extent comparable to that achieved with their cis-counterparts. (C)2001 Elsevier Science B.V. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 01/06/20 alle ore 01:55:17