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标题：In Vivo Immunomodulatory, Cumulative Skin Irritation, Sensitization and Effect of d-Limonene on Permeation of 6-Mercaptopurine through Transdermal Drug Delivery
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作者：N. S. Chandrashekar ; Shobha Rani Rajeev Hiremath
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2008
卷号：31
期号：4
页码：656-661
DOI：10.1248/bpb.31.656
出版社：The Pharmaceutical Society of Japan
摘要：Using skin as a port for systemic drug administration, transdermal drug delivery has expanded greatly over the last two decades. Our aim was to formulate the single layer drug-in-adhesive transdermal patch for 6-mercaptopurine (6-MP). In vitro permeation study was carried out using modified Franz diffusion cell with and without of different concentration of d -limonene in human cadaver skin. In vivo immunomodulatory was carried out in mice, cumulative skin irritation, sensitization and patch adherence study was done in both mice and human subjects. 6-MP flux increased from 43±12.2 μg/cm²h (control) to 162.8±32.2 μg/cm²h (6% w/v d -limonene) data was significant ( p <0.05), with decrease in the lag time to 35±9.3 min compared to control of 90 ±15.3 min. In vivo immunomodulatory effect was shown in the Balb/c mice with 100 μmol/kg/body wt of animal for 5d (one dose/d) of d -limonene. WBC count of 13469 cells/mm peak was observed on 12th day, bone marrow cells of 26.3×10⁶ cells/femur and α-esterase positive cells of 1259±328.4 cells/4000 bone marrow cells. Cumulative skin irritation, sensitisation and patch adherence in animals and human subjects showed no skin irritation and sensitization. Patch adhesion was greater than 90.0% respectively in both human subjects and mice. The percentage of human subjects with adhesive residue was significantly less with scores of zero. d -Limonene proved as good chemical enhancer by increasing in the skin permeability with shortened the lag time. It proved that therapeutic amount of 6-MP can be delivered through transdermal drug delivery.
关键词：transdermal;6-mercaptopurine;d-limonene;immunomodulatory