Polymers effect on estradiol partition coefficient between powdered human stratum corneum and water.
Macromolecules have gained interest as drug entities unto themselves and as transport facilitators to alter initial phases of percutaneous absorption. Two macromolecular polymers (MW 2081 and 2565) were designed to hold cosmetics and drugs to the skin surface by altering initial chemical and skin partitioning. The effect of these polymers on the partition coefficient (PC) of estradiol with powdered human stratum corneum (PHSC) and water was determined. There was no statistically significant effect on the PC when the concentration of estradiol was increased 100-fold (0.028-2.8 microg/mL), when the incubation time was increased from 0 to 24 h, or when PHSC was delipidized. The addition of a liphophilic polymer had no effect on the PC; however, the hydrophilic polymer showed a significant polymer concentration-dependent increase (p < 0.01) in log PC for estradiol concentrations. Thus, a macromolecular chemical has the potential to alter the partitioning of chemical into the outer layers of skin, the first step in percutaneous absorption.
Wester
Ronald C
RC
Dermatology Department, University of California, San Francisco, California 94143-0989, USA. rcwgx@itsa.ucsf.edu
Hui
Xiaoying
X
Hewitt
Philip G
PG
Hostynek
Jurij
J
Krauser
Scott
S
Chan
Thomas
T
Maibach
Howard I
HI
D004337:Drug Carriers; D004817:Epidermis / Q000187:drug effects* / Q000502:physiology; D004958:Estradiol / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D011108:Polymers / Q000737:chemistry* / Q000494:pharmacology; D011208:Powders; D014867:Water / Q000737:chemistry*
D004337:Drug Carriers; D011108:Polymers; D011208:Powders; D014867:Water; D004958:Estradiol