Imaging the prodrug-to-drug transformation of a 5-fluorouracil derivative in skin by confocal Raman microscopy.
Imaging the prodrug-to-drug transformation of a 5-fluorouracil derivative in skin by confocal Raman microscopy.
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DOI：
10.1038/sj.jid.5700690
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发表时间：
2007-05
期刊：
影响因子：
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通讯作者：
Guojin Zhang;D. Moore;K. Sloan;C. Flach;R. Mendelsohn
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文献类型：
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作者：
Guojin Zhang;D. Moore;K. Sloan;C. Flach;R. Mendelsohn
经皮药物递送的广泛采用受到表皮最外层角质层（SC）的屏障性质的限制。已经开发了多种方法来克服该屏障，包括使用活性治疗剂的前药形式来增强透皮递送。一旦进入表皮，前分子通过内源性酶或简单的化学水解转化为活性药物。目前研究选择的前药，1-乙氧羰基-5-氟尿嘧啶，已知可增强5-氟尿嘧啶（一种重要的全身性抗肿瘤药物）的透皮递送。使用共焦拉曼显微镜对猪皮活检处理的前药，我们能够成像的空间分布的前药和药物在SC和活的表皮，从而提供有关渗透和代谢的信息。这种方法可以很容易地扩展到各种皮肤病学过程。
The widespread adoption of transdermal drug delivery has been limited by the barrier properties of the outermost layer of the epidermis, the stratum corneum (SC). A variety of approaches have been developed to overcome the barrier, including the use of a prodrug form of an active therapeutic agent to enhance transdermal delivery. Once in the epidermis, the pro-molecule is converted to the active drug by endogenous enzymes or simple chemical hydrolysis. The prodrug selected for the current studies, 1-ethyloxycarbonyl-5-fluorouracil, is known to enhance transdermal delivery of 5-fluorouracil, an important systemic antitumor drug. Using confocal Raman microscopy on pigskin biopsies treated with prodrug, we are able to image the spatial distribution of both prodrug and drug in the SC and viable epidermis, thereby providing information about permeation and metabolism. This approach may readily be extended to a variety of dermatological processes.