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Titolo:
Effect of barrier disruption by acetone treatment on the permeability of compounds with various lipophilicities: Implications for the permeability ofcompromised skin
Autore:
Tsai, JC; Sheu, HM; Hung, PL; Cheng, CL;
Indirizzi:
Natl Cheng Kung Univ, Coll Med, Inst Clin Pharm, Tainan 70101, Taiwan NatlCheng Kung Univ Tainan Taiwan 70101 lin Pharm, Tainan 70101, Taiwan Natl Cheng Kung Univ, Coll Med, Dept Dermatol, Tainan 70101, Taiwan Natl Cheng Kung Univ Tainan Taiwan 70101 Dermatol, Tainan 70101, Taiwan Chia Nan Univ, Dept Pharm, Tainan, Taiwan Chia Nan Univ Tainan TaiwanChia Nan Univ, Dept Pharm, Tainan, Taiwan
Titolo Testata:
JOURNAL OF PHARMACEUTICAL SCIENCES
fascicolo: 9, volume: 90, anno: 2001,
pagine: 1242 - 1254
SICI:
0022-3549(200109)90:9<1242:EOBDBA>2.0.ZU;2-H
Fonte:
ISI
Lingua:
ENG
Soggetto:
CORNEUM LIPID ABNORMALITIES; TRANSEPIDERMAL WATER-LOSS; HUMAN STRATUM-CORNEUM; PERCUTANEOUS-ABSORPTION; EPIDERMAL BARRIER; DERMATITIS; DISORDERS; HYDROCORTISONE; NEWBORN; INFANTS;
Keywords:
barrier disruption; skin permeability; compound lipophilicity; transepidermal water loss; acetone treatment;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
33
Recensione:
Indirizzi per estratti:
Indirizzo: Tsai, JC Natl Cheng Kung Univ, Coll Med, Inst Clin Pharm, Tainan 70101, Taiwan Natl Cheng Kung Univ Tainan Taiwan 70101 , Tainan 70101, Taiwan
Citazione:
J.C. Tsai et al., "Effect of barrier disruption by acetone treatment on the permeability of compounds with various lipophilicities: Implications for the permeability ofcompromised skin", J PHARM SCI, 90(9), 2001, pp. 1242-1254

Abstract

The permeability of compromised skin barrier was investigated in vitro using acetone-disrupted hairless mouse skin as a model membrane. The effect ofcompound lipophilicity was studied using sucrose, caffeine, hydrocortisone, estradiol, and progesterone as model compounds. The results demonstrated that permeability barrier disruption by acetone treatment significantly enhanced the permeability of the skin to both hydrophilic and amphipathic compounds, including sucrose, caffeine and hydrocortisone. This effect was moreprominent with caffeine and hydrocortisone at different transepidermal water loss (TEWL) levels. Acetone treatment, however, didn't appear to alter the percutaneous penetration of highly lipophilic compounds, such as estradiol and progesterone. The characteristics of skin permeability were described by parabolic relationships between log P-WS (permeability coefficient of whole skin) and log K-O/W (octanol/water partition coefficient) at different degrees of permeability barrier disruption. The optimal log K-O/W of compounds for skin penetration appeared to decrease with an increase in TEWL levels. The maximal permeability achieved was similar through skin displayingdifferent TEWL levels. In an attempt to explore the underlying mechanisms for the changes in skin permeability, the stratum corneum/ normal saline partition coefficients of water, caffeine, and hydrocortisone either decreased or remained unaffected with an increase in TEWL. Electron microscopic examinations have revealed reductions in stratum corneum lipid content and alterations in intercellular membrane structures as a result of acetone treatment, whereas negligible changes in the number of horny layers were observedby safranin staining of the stratum corneum. We have concluded that the enhancement in skin permeability to both hydrophilic and amphipathic compounds by acetone treatment arose mainly because of the increase in stratum corneum diffusivity at higher TEWL levels. The results imply the possibility ofusing both TEWL and drug lipophilicity to predict alterations in skin permeability and hence the dose adjustment of topically applied medication for patients with impaired skin barrier function. (C) 2001 Wiley-Liss, Inc. andthe American Pharmaceutical Association.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 04/04/20 alle ore 15:30:22