HINDERED DIFFUSION OF POLAR-MOLECULES THROUGH AND EFFECTIVE PORE RADII ESTIMATES OF INTACT AND ETHANOL-TREATED HUMAN EPIDERMAL MEMBRANE

被引:132
作者
PECK, KD
GHANEM, AH
HIGUCHI, WI
机构
[1] Department of Pharmaceutics and Pharmaceutical Chemistry, University of Utah, Salt Lake City, Utah
关键词
HUMAN EPIDERMAL MEMBRANE; SKIN PERMEABILITY; TRANSDERMAL DELIVERY; PERMEATION ENHANCERS; HINDERED DIFFUSION; STRATUM CORNEUM;
D O I
10.1023/A:1018998529283
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
The in vitro passive transport of urea, mannitol, sucrose and raffinose across intact and ethanol treated human epidermal membrane was investigated. The intent of this study was to characterize the barrier properties and permeation pathways of these membranes for polar permeants under passive conditions. Based upon the relative permeabilities of these four solutes and hindered diffusion theory, the experimental data was adequately modeled for both membrane systems according to permeation through a porous membrane. Effective pore radii estimates for intact human epidermal membrane fell between 15 Angstrom to 25 Angstrom while similar estimates fell compactly between 15 Angstrom to 20 Angstrom for ethanol treated human epidermal membrane. Similarities between the relative permeabilities of human epidermal membrane for the four permeants studied and the relative permeabilities of these same permeants through ethanol pretreated human epidermal membrane indicate that significant similarities exist between the permeation pathways for both membrane systems. The results of this study have important implications for transdermal drug delivery in general and more specifically for strategies of designing effective chemical permeation enhancement systems.
引用
收藏
页码:1306 / 1314
页数:9
相关论文
共 30 条
[1]   ETHER WATER PARTITIONING AND PERMEABILITY THROUGH NUDE-MOUSE SKIN INVITRO .2. HYDROCORTISONE 21-NORMAL-ALKYL ESTERS, ALKANOLS AND HYDROPHILIC COMPOUNDS [J].
ACKERMANN, C ;
FLYNN, GL ;
SMITH, WM .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1987, 36 (01) :67-71
[2]  
BECK RE, 1972, BIOCHIM BIOPHYS ACTA, V255, P272
[3]   THE INFLUENCE OF PEPTIDE STRUCTURE ON TRANSPORT ACROSS CACO-2 CELLS [J].
CONRADI, RA ;
HILGERS, AR ;
HO, NFH ;
BURTON, PS .
PHARMACEUTICAL RESEARCH, 1991, 8 (12) :1453-1460
[4]   THE ROUTES OF PENETRATION OF IONS AND 5-FLUOROURACIL ACROSS HUMAN SKIN AND THE MECHANISMS OF ACTION OF TERPENE SKIN PENETRATION ENHANCERS [J].
CORNWELL, PA ;
BARRY, BW .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1993, 94 (1-3) :189-194
[5]   HINDERED TRANSPORT OF LARGE MOLECULES IN LIQUID-FILLED PORES [J].
DEEN, WM .
AICHE JOURNAL, 1987, 33 (09) :1409-1425
[6]   EFFECTS OF MOLECULAR-SIZE AND CONFIGURATION ON DIFFUSION IN MICROPOROUS MEMBRANES [J].
DEEN, WM ;
BOHRER, MP ;
EPSTEIN, NB .
AICHE JOURNAL, 1981, 27 (06) :952-959
[7]   *MOLEKULARE THEORIE DER MIKROREIBUNG [J].
GIERER, A ;
WIRTZ, K .
ZEITSCHRIFT FUR NATURFORSCHUNG SECTION A-A JOURNAL OF PHYSICAL SCIENCES, 1953, 8 (09) :532-538
[8]   STRATUM-CORNEUM LIPID PHASE-TRANSITIONS AND WATER BARRIER PROPERTIES [J].
GOLDEN, GM ;
GUZEK, DB ;
KENNEDY, AH ;
MCKIE, JE ;
POTTS, RO .
BIOCHEMISTRY, 1987, 26 (08) :2382-2388
[9]   EFFECT OF VEHICLE ON THE SKIN PERMEABILITY OF DRUGS - POLYETHYLENE-GLYCOL 400-WATER AND ETHANOL-WATER BINARY SOLVENTS [J].
HATANAKA, T ;
SHIMOYAMA, M ;
SUGIBAYASHI, K ;
MORIMOTO, Y .
JOURNAL OF CONTROLLED RELEASE, 1993, 23 (03) :247-260
[10]   STUDIES ON THE EFFECTS OF APPLIED VOLTAGE AND DURATION ON HUMAN EPIDERMAL MEMBRANE ALTERATION/RECOVERY AND THE RESULTANT EFFECTS UPON IONTOPHORESIS [J].
INADA, H ;
GHANEM, AH ;
HIGUCHI, WI .
PHARMACEUTICAL RESEARCH, 1994, 11 (05) :687-697