Physicochemical aspects of percutaneous penetration and its enhancement.
Guy RH; Hadgraft J
Departments of Pharmacy and Pharmaceutical Chemistry, Schools of Pharmacy and Medicine, University of California, San Francisco, California, 1987 Dec; :1-31
The relationship between permeation and penetrant physicochemical properties was examined in a brief review of simple Fickian transport as it pertains to the skin. The goal was to establish a conceptual framework for the prospective assessment and optimization of transdermal transport. Both the physicochemical significance and the major deductions from these two approaches were shown to be in general agreement, particularly the prediction of the effect of penetrant oil/water partition coefficient on transdermal flux, which was consistent with the two methods. Similar dependencies on penetrant physical chemistry were demonstrated by both diffusional and kinetic assessments of skin penetration enhancement. Requirements for successful promotion of a lipophilic drug transdermal flux were quite different from those needed for a hydrophilic penetrant. Evidence for different absorption paths across the stratum corneum was also considered and the impact of penetrant size on transport was addressed. According to the authors, currently held ideas concerning the existence of a putative polar route through the stratum corneum and the dependence of flux on molecular weight should be given further study in light of the findings of this project.
NIOSH-Grant; Dermatitis; Skin-exposure; Skin-absorption; Tissue-distribution
Pharmacy University of California 926 Medical Sciences Building San Francisco, Calif 94143
Final Grant Report
NTIS Accession No.
Departments of Pharmacy and Pharmaceutical Chemistry, Schools of Pharmacy and Medicine, University of California, San Francisco, California
University of California San Francisco, San Francisco, California