A NUMERICAL APPROACH TO STUDY THE EFFECT OF BINDING ON THE IONTOPHORETIC TRANSPORT OF A SERIES OF AMINO-ACIDS

被引:31
作者
WEARLEY, LL [1 ]
TOJO, K [1 ]
CHIEN, YW [1 ]
机构
[1] RUTGERS STATE UNIV,COLL PHARM,CONTROLLED DRUG DELIVERY RES CTR,PISCATAWAY,NJ 08855
关键词
D O I
10.1002/jps.2600791110
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The objective of this investigation was to quantitate the effect of binding on the iontophoretic transport of a series of amino acids. The diffusivity and concentration in the stratum corneum and viable skin were estimated from the passive permeation profiles through whole and stripped skin. Using these parameters and the Langmuir binding parameters from equilibrium binding studies, the passive permeation and desorption profiles were simulated using a bilayer skin permeation model. The parameters were adjusted until convergence with experimental data was achieved. Then the iontophoretic profiles were simulated, using the parameters from the simulated passive permeation studies, an estimate of convective flow from the flux of tritiated water, and measurement of the potential across the skin. The overall effect of binding on the iontophoretic profiles was found to dampen the effect of the iontophoresis treatment; the profiles appear flatter, and the transition to passive diffusion less distinct compared to profiles which do not include the binding parameters. It also appears that the degree of skin hydration has a substantial effect on the shape of the iontophoretic profile, such that approximately 50% of the enhancement in the iontophoretic profile of freshly excised skin continues after treatment. Copyright © 1990 Wiley‐Liss, Inc., A Wiley Company
引用
收藏
页码:992 / 998
页数:7
相关论文
共 12 条
[1]  
BEHL CR, 1980, J INVEST DERMATOL, V75, P346, DOI 10.1111/1523-1747.ep12531118
[2]   INFLUENCE OF CONSTANT CURRENT IONTOPHORESIS ON THE IMPEDANCE AND PASSIVE NA+ PERMEABILITY OF EXCISED NUDE-MOUSE SKIN [J].
BURNETTE, RR ;
BAGNIEFSKI, TM .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1988, 77 (06) :492-497
[3]   SCOPOLAMINE PERMEATION THROUGH HUMAN-SKIN INVITRO [J].
CHANDRASEKARAN, SK ;
MICHAELS, AS ;
CAMPBELL, PS ;
SHAW, JE .
AICHE JOURNAL, 1976, 22 (05) :828-832
[4]  
HILLE B, 1984, IONIC CHANNELS EXCIT, P157
[5]  
ROBERTS J, 1967, ORGANIC CHEM, P483
[7]   DRUG PERMEATION ACROSS THE SKIN - EFFECT OF PENETRANT HYDROPHILICITY [J].
TOJO, K ;
CHIANG, CC ;
CHIEN, YW .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1987, 76 (02) :123-126
[8]  
TOJO K, 1989, P INT S CONTROL REL, V16, P452
[9]  
WANG J, 1982, THESIS U IOWA IOWA C, P269
[10]   IONTOPHORESIS-FACILITATED TRANSDERMAL DELIVERY OF VERAPAMIL .2. FACTORS AFFECTING THE REVERSIBILITY OF SKIN PERMEABILITY [J].
WEARLEY, L ;
LIU, JC ;
CHIEN, YW .
JOURNAL OF CONTROLLED RELEASE, 1989, 9 (03) :231-242