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Tissue binding affects the kinetics of theophylline diffusion through the stratum corneum barrier layer of skin.

Authors
Frasch-HF; Barbero-AM; Hettick-JM; Nitsche-JM
Source
J Pharm Sci 2011 Jul; 100(7):2989-2995
NIOSHTIC No.
20038366
Abstract
New data sets on both (i) equilibrium theophylline (TH) partitioning/binding in stratum corneum and (ii) transient TH diffusion through human epidermis are explained by an extended partition-diffusion model with reversible binding. Data conform to a linear binding isotherm within the tested concentration range (0-2000 :g/mL) with an equilibrium ratio of bound-to-free solute of approximately 1.4. The permeability coefficient for TH is 4.86 10-5 cm/h, and the lag time is 20.1 h. Binding occurs as a slow process, significantly affecting the kinetics of dermal penetration.
Keywords
Skin-exposure; Skin-absorption; Dermatology; Exposure-assessment; Cell-function; Cellular-transport-mechanism; Author Keywords: transdermal; passive diffusion/transport; kinetics; protein binding; transient diffusion; lag time; reversible binding; permeable corneocytes; theophylline; keratin
Contact
H. Frederick Frasch, Health Effects Laboratory, National Institute for Occupational Safety and Health, Morgantown, West Virginia 26505
CODEN
JPMSAE
Publication Date
20110701
Document Type
Journal Article
Fiscal Year
2011
NTIS Accession No.
NTIS Price
Issue of Publication
7
ISSN
0022-3549
NIOSH Division
HELD
Source Name
Journal of Pharmaceutical Sciences
State
WV
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