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    Please use this identifier to cite or link to this item: http://ir.cnu.edu.tw/handle/310902800/31052


    標題: Topically applied mesoridazine exhibits the strongest cutaneous analgesia and minimized skin disruption among tricyclic antidepressants: The skin absorption assessment
    作者: Liu, Kuo-Sheng
    Chen, Yu-Wen
    Aljuffali, Ibrahim A.
    Chang, Chia-Wen
    Wang, Jhi-Joung
    Fang, Jia-You
    關鍵字: Tricyclic depressant
    Mesoridazine
    Skin
    Topical delivery
    Neuropathic pain
    日期: 2016-08
    上傳時間: 2018-01-18 11:40:39 (UTC+8)
    出版者: Elsevier Science Bv
    摘要: Tricyclic antidepressants (TCAs) are found to have an analgesic action for relieving cutaneous pain associated with neuropathies. The aim of this study was to assess cutaneous absorption and analgesia of topically applied TCAs. Percutaneous delivery was investigated using nude mouse and pig skin models at both infinite and saturated doses. We evaluated the cutaneous analgesia in nude mice using the pinprick scores. Among five antidepressants tested in the in vitro experiment, mesoridazine, promazine and doxepin showed a superior total absorption percentage. The drug with the lowest total absorption percentage was found to be fluphenazine (<7%) either at an infinite dose or at saturated solubility. The follicular pathway was important for mesoridazine and promazine delivery. Mesoridazine showed stronger skin analgesia than the other TCAs although the in vivo skin absorption of mesoridazine (0.34 nmol/mg) was less than that of promazine (0.80 nmol/mg) and doxepin (0.74 nmol/mg). Mesoridazine had a prolonged duration of pain relief (165 min) compared to promazine (83 min) and doxepin (17 min). The skin irritation test demonstrated an evident barrier function deterioration and cutaneous erythema by promazine and doxepin treatment, whereas mesoridazine caused no obvious adverse effect by topical application for up to 7 days. (C) 2016 Elsevier B.V. All rights reserved.
    關聯: European Journal of Pharmaceutics and Biopharmaceutics, v.105, pp.59-68
    Appears in Collections:[藥學系(所)] 期刊論文

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