An experimental approach to study the binding properties of vitamin E (α-tocopherol) during hairless mouse skin permeation

被引:9
作者
Lee, ARC
Tojo, K
机构
[1] Duksung Womens Univ, Coll Pharm, Dobong Ku, Seoul 132714, South Korea
[2] Kyushu Inst Technol, Fac Comp Sci & Syst Engn, Iizuka, Fukuoka 820, Japan
关键词
skin permeation; vitamin E (alpha-tocopherol); binding; skin reservoir; differential scanning calorimetry;
D O I
10.1248/cpb.49.659
中图分类号
R914 [药物化学];
学科分类号
100701 [药物化学];
摘要
An experimental approach to study the binding properties of vitamin E has been developed. Total vitamin E solubility in the skin was determined by a partition study, followed by in vitro skin permeation studies with whole skin and stripped skin. The amount of freely diffusable vitamin E in the diffusion process was determined from the permeation profiles of whole skin and stripped skin by employing a bi-layer model. The concentrations of vitamin E in the stratum corneum and viable dermis were determined separately. By subtracting this amount from the total concentration of vitamin E in the skin, as determined by the solubility study, the amount of bound vitamin E was determined. After skin permeation reached a steady state, the donor solution was removed and the permeation study continued (desorption study). During the entire period of the desorption experiment, the amount of vitamin E in the receptor solution hardly increased and remained constant. After the desorption experiment, vitamin E still remaining in the skin was determined by extracting with tissue solubilizer, SOLABLE, and is considered as the amount of vitamin E strongly bound in the skin, The concentrations of bound vitamin E determined by permeation and desorption studies coincided relatively well. To further investigate skin binding of vitamin E, a differential scanning calorimetry study was performed. Vitamin E-treated stratum corneum showed phase transitions at 76 and 85 degreesC, associated with lipid transitions. The thermal transitions associated with the lipid transition suggested interactions of vitamin E with lipid components of the skin. During skin permeation, vitamin E forms a very strong reservoir in the skin tissue and this amount of vitamin E, about 30%, exists as a bound-form with the lipid components of the stratum corneum.
引用
收藏
页码:659 / 663
页数:5
相关论文
共 23 条
[1]
Barber D A, 1994, Am Pharm, VNS34, P26
[2]
BIOCHEMICAL MODES OF ACTION OF VITAMIN-E AND SELENIUM - HYPOTHESIS [J].
DIPLOCK, AT ;
LUCY, JA .
FEBS LETTERS, 1973, 29 (03) :205-210
[3]
DIPLOCK AT, 1977, FEBS LETT, V82, P341, DOI 10.1016/0014-5793(77)80616-9
[4]
KNUTSON K, 1985, Journal of Controlled Release, V2, P67, DOI 10.1016/0168-3659(85)90034-3
[5]
EFFECTS OF LONG-TERM HYDRATION LEADING TO THE DEVELOPMENT OF POLAR CHANNELS IN HAIRLESS MOUSE STRATUM-CORNEUM [J].
LAMBERT, WJ ;
HIGUCHI, WI ;
KNUTSON, K ;
KRILL, SL .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1989, 78 (11) :925-928
[6]
DOSE-DEPENDENT ENHANCEMENT EFFECTS OF AZONE ON SKIN PERMEABILITY [J].
LAMBERT, WJ ;
HIGUCHI, WI ;
KNUTSON, K ;
KRILL, SL .
PHARMACEUTICAL RESEARCH, 1989, 6 (09) :798-803
[7]
Lee ARC, 1996, J SOC COSMET CHEM, V47, P85
[8]
LEE ARC, 1990, THESIS RUTGERS U
[9]
MISELNICKY SR, 1988, J SOC COSMET CHEM, V39, P169
[10]
POTTS RO, 1986, J SOC COSMET CHEM, V37, P9