Topically applied mesoridazine exhibits the strongest cutaneous analgesia and minimized skin disruption among tricyclic antidepressants: The skin absorption assessment

doi:10.1016/j.ejpb.2016.05.025

CNU IR > Pharmacy and Science > Dept. of Pharmacy > Periodical Articles > Item 310902800/31052

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题名:	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
贡献者:	Chia Nan Univ Pharm & Sci, Dept Pharm China Med Univ, Dept Phys Therapy Chi Mei Med Ctr, Dept Med Res King Saud Univ, Coll Pharm, Dept Pharmaceut Chang Gung Univ, Grad Inst Nat Prod 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
关键词:	Tricyclic depressant Mesoridazine Skin Topical delivery Neuropathic pain
日期:	2016-08
上传时间:	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
显示于类别:	[Dept. of Pharmacy] Periodical Articles

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