Parallel artificial membrane permeability assay: A new membrane for the fast prediction of passive human skin permeability

被引:154
作者
Ottaviani, Giorgio
Martel, Sophie
Carrupt, Pierre-Alain [1 ]
机构
[1] Univ Geneva, Sect Sci Pharmaceut, LCT Pharmacochim, CH-1211 Geneva 4, Switzerland
[2] Univ Lausanne, CH-1211 Geneva 4, Switzerland
关键词
D O I
10.1021/jm060230+
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
This work was devoted to the search for new artificial membranes allowing a rapid evaluation of passive human skin permeation of compounds with a parallel artificial membrane permeability assay ( PAMPA). Effective permeability coefficients ( P-e) determined for a set of compounds using the PAMPA technique with isopropyl myristate ( IPM) and silicone oil, alone or in mixture, were compared to the corresponding human skin permeability coefficient values ( K-p). A good correlation between Pe and Kp was found for compounds tested through a membrane consisting of 70% silicone and 30% IPM. Moreover, positive correlation between the membrane retention of compounds and stratum corneum/water partition coefficients ( P-SC) was established. These results showed that this new artificial membrane, defined as PAMPA-skin, is able to mimic the main barrier properties of human stratum corneum and can be used for the fast prediction of passive human skin permeability coefficients.
引用
收藏
页码:3948 / 3954
页数:7
相关论文
共 53 条
[1]   Human skin permeation and partition: General linear free-energy relationship analyses [J].
Abraham, MH ;
Martins, F .
JOURNAL OF PHARMACEUTICAL SCIENCES, 2004, 93 (06) :1508-1523
[2]   Drug absorption in vitro model:: filter-immobilized artificial membranes 2.: Studies of the permeability properties of lactones in Piper methysticum Forst [J].
Avdeef, A ;
Strafford, M ;
Block, E ;
Balogh, MP ;
Chambliss, W ;
Khan, I .
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2001, 14 (04) :271-280
[3]   PH-metric log P 11.: pKa determination of water-insoluble drugs in organic solvent-water mixtures [J].
Avdeef, A ;
Box, KJ ;
Comer, JEA ;
Gilges, M ;
Hadley, M ;
Hibbert, C ;
Patterson, W ;
Tam, KY .
JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS, 1999, 20 (04) :631-641
[4]  
Avdeef A., 2003, ABSORPTION DRUG DEV, DOI [10.1002/047145026X, DOI 10.1002/047145026X]
[5]  
Barry, 1983, DERMATOLOGICAL FORMU
[6]   PERMEATION OF ESTRONE, ESTRADIOL, ESTRIOL AND DEXAMETHASONE ACROSS CELLULOSE-ACETATE MEMBRANE [J].
BARRY, BW ;
BRACE, AR .
JOURNAL OF PHARMACY AND PHARMACOLOGY, 1977, 29 (07) :397-400
[7]   INFLUENCE OF NONIONIC SURFACTANTS ON PERMEATION OF HYDROCORTISONE, DEXAMETHASONE, TESTOSTERONE AND PROGESTERONE ACROSS CELLULOSE-ACETATE MEMBRANE [J].
BARRY, BW ;
ELEINI, DID .
JOURNAL OF PHARMACY AND PHARMACOLOGY, 1976, 28 (03) :219-227
[8]  
Bouchard G, 2002, CHEM-EUR J, V8, P3478, DOI 10.1002/1521-3765(20020802)8:15<3478::AID-CHEM3478>3.0.CO
[9]  
2-U
[10]  
Brain KR, 2002, DRUGS PHARM SCI, V119, P197