Exploring the structure-permeation relationship of topical tricyclic antidepressants used for skin analgesia

doi:10.1016/j.ijpharm.2017.03.048

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標題:	Exploring the structure-permeation relationship of topical tricyclic antidepressants used for skin analgesia
作者:	Liu, Kuo-Sheng Huang, Tse-Hung Aljuffali, Ibrahim A. Chen, En-Li Wang, Jhi-Joung Fang, Jia-You
貢獻者:	Chia Nan Univ Pharm & Sci, Dept Pharm Chang Gung Mem Hosp, Dept Tradit Chinese Med Chang Gung Univ, Sch Tradit Chinese Med Natl Taipei Univ Nursing & Hlth Sci, Sch Nursing King Saud Univ, Dept Pharmaceut, Coll Pharm Chang Gung Univ, Grad Inst Nat Prod, Pharmaceut Lab Chi Mei Med Ctr, Dept Med Res Chang Gung Univ, Hlth Aging Res Ctr, Chinese Herbal Med Res Team Chang Gung Mem Hosp, Dept Anesthesiol Chang Gung Univ Sci & Technol, Res Ctr Ind Human Ecol Chang Gung Univ Sci & Technol, Res Ctr Chinese Herbal Med
關鍵字:	Tricyclic antidepressant Propamine Analgesia Cutaneous absorption Structure-permeation relationship
日期:	2017-05-15
上傳時間:	2018-11-30 15:52:26 (UTC+8)
出版者:	Elsevier Science Bv
摘要:	The purpose of this study was to evaluate the skin permeation of tricyclic antidepressants (TCAs) with propamine moiety to select candidates for the development of topical analgesics to treat cutaneous pain. We sought to establish the structure-permeation relationship (SPR) of topical TCAs. The lipophilicity, melting point, and aqueous solubility were determined to develop the physicochemical characterization. The TCA permeation into pig and nude mouse skins was estimated using Franz diffusion cell. TCAs and lidocaine were comparatively examined for cutaneous analgesia by pinprick assay. Cutaneous tolerance to TCAs was assessed using nude mouse skin. The skin deposition increased following the increase of lipophilicity after excluding the effect of solubility, with clomipramine exhibiting the highest skin retention. A contrary result was observed for TCA penetration into the receptor. Of the permeants tested, clomipramine demonstrated the best skin-targeting ability. Nortriptyline and clomipramine demonstrated selective uptake into the hair follicles, exhibiting a 2.5-fold higher follicular accumulation than desipramine. Replacement of nitrogen with carbon in the seven-member ring increased skin absorption. The tertiary amine TCAs demonstrated higher absorption than the secondary amine TCAs. The position of the double bond also affected skin transport. Topical clomipramine had a longer duration of analgesic action than lidocaine (240 min versus 60 min). Exploring the SPR revealed that clomipramine could be an analgesic candidate drug for future development. (C) 2017 Elsevier B.V. All rights reserved.
關聯:	International Journal of Pharmaceutics, v.523, n.1, pp.386-397
显示于类别:	[藥學系(所)] 期刊論文

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