Transdermal delivery of cyclosporin-A using electroporation

被引:56
|
作者
Wang, S [1 ]
Kara, M [1 ]
Krishman, TR [1 ]
机构
[1] Mem Univ Newfoundland, Sch Pharm, St John, NF A1B 3V6, Canada
关键词
electroporation; ethanol; transdermal delivery; cyclosporin A;
D O I
10.1016/S0168-3659(97)00117-X
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Topical delivery of cyclosporin A (CSA) is desirable for treating psoriasis, but it is hindered by the barrier property of stratum corneum, and the physicochemical properties of CSA. Attempts to deliver CSA from a solution prepared in 40% ethanol (EtOH) in phosphate buffered saline (PBS) using iontophoresis did not result in any significant increase in drug delivery, compared to passive. However, the use of electroporation pulses as a physical penetration enhancer enabled delivery of a significant amount of CSA. Single pulse electroporation study indicated that the amount of EtOH delivered across the skin increased as the applied electrode voltage (U-electrode) was increased. However, it did not translate into a proportional increase in the delivery of CSA and only a three to four times increase, compared to passive delivery, was seen with the single pulse electroporation. The drug contact duration had a varying effect in the efficiency of transdermal delivery of CSA. Four hour contact duration was chosen for the multiple pulse study. Use of multiple pulses (25 pulses, 10 ms each) at U-electrode 200 V resulted in a sixty-fold increase, compared to passive, in the delivery of CSA to the skin. Transdermally delivered CSA was mostly bound to the skin and only a small amount was seen to cross the full skin into the receiver compartment. In a study of solvent transport, the flux of water was up to three times larger than that of EtOH after electroporation. (C) 1998 Elsevier Science B.V.
引用
收藏
页码:61 / 70
页数:10
相关论文
共 50 条
  • [31] Surfactant-enhanced transdermal delivery by electroporation
    Murthy, SN
    Sen, A
    Hui, SW
    JOURNAL OF CONTROLLED RELEASE, 2004, 98 (02) : 307 - 315
  • [32] Lecithin vesicular carriers for transdermal delivery of cyclosporin A
    Guo, JX
    Ping, QN
    Sun, GQ
    Jiao, CH
    INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2000, 194 (02) : 201 - 207
  • [33] THE PREVENTION OF HEYMANN NEPHRITIS USING CYCLOSPORIN-A
    KIRSON, IJ
    MAKKER, SP
    KHER, KK
    CLINICAL RESEARCH, 1981, 29 (01): : A151 - A151
  • [34] INTESTINAL TRANSPLANTATION IN THE PIGLET USING CYCLOSPORIN-A
    RICOUR, C
    REVILLON, Y
    LAUFENBURGER, A
    GHNASSIA, D
    JOS, J
    FONTAINE, JL
    VAIMAN, M
    WEYNE, P
    ARNAUDBATTANDIER, F
    GALLIX, P
    GASTROENTEROLOGIE CLINIQUE ET BIOLOGIQUE, 1983, 7 : A39 - A39
  • [35] BIOSYNTHESIS OF CYCLOSPORIN-A
    ZOCHER, R
    MADRY, N
    PEETERS, H
    KLEINKAUF, H
    PHYTOCHEMISTRY, 1984, 23 (03) : 549 - 551
  • [36] Transdermal delivery of timolol and atenolol using electroporation and iontophoresis in combination:: A mechanistic approach
    Denet, AR
    Ucakar, B
    Préat, V
    PHARMACEUTICAL RESEARCH, 2003, 20 (12) : 1946 - 1951
  • [37] NEPHROTOXICITY OF CYCLOSPORIN-A
    HOWS, JM
    GORDONSMITH, EC
    LANCET, 1981, 2 (8251): : 876 - 877
  • [38] Transdermal Delivery of Timolol and Atenolol Using Electroporation and Iontophoresis in Combination: A Mechanistic Approach
    Anne-Rose Denet
    Bernard Ucakar
    Véronique Préat
    Pharmaceutical Research, 2003, 20 : 1946 - 1951
  • [39] PHARMACOLOGY OF CYCLOSPORIN-A
    BOREL, J
    WINTERS, D
    INTERNATIONAL JOURNAL OF IMMUNOPHARMACOLOGY, 1982, 4 (04): : 367 - 367
  • [40] CYCLOSPORIN-A AND THE MEDIA
    CALNE, RY
    MCMASTER, P
    EVANS, DB
    BRITISH MEDICAL JOURNAL, 1980, 280 (6206): : 43 - 43