Influence of phloretin and 6-ketocholestanol on the skin permeation of sodium-fluorescein

被引:22
作者
Auner, BG
Valenta, C
Hadgraft, J
机构
[1] Univ Vienna, Inst Pharmaceut Technol & Biopharmaceut, A-1090 Vienna, Austria
[2] Univ Greenwich, Skin & Membrane Transfer Res Ctr, Chatham ME4 4TB, Kent, England
关键词
transdermal delivery; 6-ketocholestanol; phloretin; sodium-fluorescein; confocal laser scanning microscopy;
D O I
10.1016/S0168-3659(03)00124-X
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
In the present study. we investigated the feasibility of enhancing the transport of the model drug sodium-fluorescein across rat. porcine and human skin by treating it with phloretin and 6-ketocholestanol. Both 6-ketocholestanol and phloretin were incorporated into unilamellar liposomes and used as a skin pre-treatment. Afterwards standard diffusion experiments with Franz-type diffusion cells were performed. The results indicate a positive effect of 6-ketocholestanol on the sodium-fluorescein diffusion in all skin types, whereas phloretin had no significant influence compared to the control in human skin. In contrast to this. phloretin had a significant positive effect in rat as well as in porcine skin after 30 h of diffusion. In addition to the permeation studies, the human skin samples were analysed by confocal laser scanning microscopy for direct visualisation of the sodium-fluorescein. As expected the results of the diffusion experiments were confirmed by this microscopic method. (C) 2003 Elsevier Science B.V. All rights reserved.
引用
收藏
页码:321 / 328
页数:8
相关论文
共 20 条
[1]  
ANDO HY, 1984, J PHARM SCI, V73, P491
[2]  
[Anonymous], 1987, TRANSDERMAL DELIV DR
[3]   Influence of lipophilic counter-ions in combination with phloretin and 6-ketocholestanol on the skin permeation of 5-aminolevulinic acid [J].
Auner, BG ;
Valenta, C ;
Hadgraft, J .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2003, 255 (1-2) :109-116
[4]  
BARRY B W, 1987, Journal of Controlled Release, V6, P85, DOI 10.1016/0168-3659(87)90066-6
[5]   INTERACTION OF ELECTRIC DIPOLES WITH PHOSPHOLIPID HEAD GROUPS - A H-2 AND P-31 NMR-STUDY OF PHLORETIN AND PHLORETIN ANALOGS IN PHOSPHATIDYLCHOLINE MEMBRANES [J].
BECHINGER, B ;
SEELIG, J .
BIOCHEMISTRY, 1991, 30 (16) :3923-3929
[6]   Intramembrane molecular dipoles affect the membrane insertion and folding of a model amphiphilic peptide [J].
Cladera, J ;
O'Shea, P .
BIOPHYSICAL JOURNAL, 1998, 74 (05) :2434-2442
[7]   Influence of molecular dipoles on human skin permeability: Use of 6-ketocholestanol to enhance the transdermal delivery of bacitracin [J].
Cladera, J ;
O'Shea, P ;
Hadgraft, J ;
Valenta, C .
JOURNAL OF PHARMACEUTICAL SCIENCES, 2003, 92 (05) :1018-1027
[8]   VISUALIZATION OF IONTOPHORETIC PATHWAYS WITH CONFOCAL MICROSCOPY AND THE VIBRATING PROBE ELECTRODE [J].
CULLANDER, C ;
GUY, RH .
SOLID STATE IONICS, 1992, 53 :197-206
[9]   RELATION OF ELECTRICAL-PROPERTIES OF SKIN TO STRUCTURE AND PHYSIOLOGIC STATE [J].
EDELBERG, R .
JOURNAL OF INVESTIGATIVE DERMATOLOGY, 1977, 69 (03) :324-327
[10]   INTERNAL ELECTROSTATIC POTENTIALS IN BILAYERS - MEASURING AND CONTROLLING DIPOLE POTENTIALS IN LIPID VESICLES [J].
FRANKLIN, JC ;
CAFISO, DS .
BIOPHYSICAL JOURNAL, 1993, 65 (01) :289-299