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
[31]   Synergistic effects of chemical enhancers and therapeutic ultrasound on transdermal drug delivery [J].
Johnson, ME ;
Mitragotri, S ;
Patel, A ;
Blankschtein, D ;
Langer, R .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1996, 85 (07) :670-679
[32]   PERMEATION OF STEROIDS THROUGH HUMAN SKIN [J].
JOHNSON, ME ;
BLANKSCHTEIN, D ;
LANGER, R .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1995, 84 (09) :1144-1146
[33]  
KAI T, 1993, BIOL PHARM BULL, V16, P284
[34]   Physicochemical high throughput screening: Parallel artificial membrane permeation assay in the description of passive absorption processes [J].
Kansy, M ;
Senner, F ;
Gubernator, K .
JOURNAL OF MEDICINAL CHEMISTRY, 1998, 41 (07) :1007-1010
[35]   Discovery of transdermal penetration enhancers by high-throughput screening [J].
Karande, P ;
Jain, A ;
Mitragotri, S .
NATURE BIOTECHNOLOGY, 2004, 22 (02) :192-197
[36]   High throughput screening of transdermal formulations [J].
Karande, P ;
Mitragotri, S .
PHARMACEUTICAL RESEARCH, 2002, 19 (05) :655-660
[37]   DIFFUSION LAYER EFFECTS ON PERMEATION OF PHENYLBUTAZONE THROUGH POLYDIMETHYLSILOXANE [J].
LOVERING, EG ;
BLACK, DB .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1974, 63 (09) :1399-1402
[38]  
Maitani Y, 1996, CHEM PHARM BULL, V44, P403
[39]  
MATSUZAKI K, 1993, CHEM PHARM BULL, V41, P575
[40]   MECHANISTIC STUDY OF ULTRASONICALLY-ENHANCED TRANSDERMAL DRUG-DELIVERY [J].
MITRAGOTRI, S ;
EDWARDS, DA ;
BLANKSCHTEIN, D ;
LANGER, R .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1995, 84 (06) :697-706