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Eur J Pharm Biopharm. 2016 Aug;105:59-68. doi: 10.1016/j.ejpb.2016.05.025. Epub 2016 May 31.

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

Author information

1
Department of Pharmacy, Chia Nan University of Pharmacy and Science, Tainan, Taiwan.
2
Department of Physical Therapy, China Medical University, Taichung, Taiwan; Department of Medical Research, Chi Mei Medical Center, Tainan, Taiwan.
3
Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.
4
Pharmaceutics Laboratory, Graduate Institute of Natural Products, Chang Gung University, Kweishan, Taoyuan, Taiwan.
5
Department of Medical Research, Chi Mei Medical Center, Tainan, Taiwan. Electronic address: 400002@mail.chimei.org.tw.
6
Pharmaceutics Laboratory, Graduate Institute of Natural Products, Chang Gung University, Kweishan, Taoyuan, Taiwan; Chinese Herbal Medicine Research Team, Healthy Aging Research Center, Chang Gung University, Kweishan, Taoyuan, Taiwan; Department of Anesthesiology, Chang Gung Memorial Hospital, Kweishan, Taoyuan, Taiwan; Research Center for Industry of Human Ecology, Chang Gung University of Science and Technology, Kweishan, Taoyuan, Taiwan. Electronic address: fajy@mail.cgu.edu.tw.

Abstract

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 (0.34nmol/mg) was less than that of promazine (0.80nmol/mg) and doxepin (0.74nmol/mg). Mesoridazine had a prolonged duration of pain relief (165min) compared to promazine (83min) and doxepin (17min). 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 7days.

KEYWORDS:

Mesoridazine; Neuropathic pain; Skin; Topical delivery; Tricyclic depressant

PMID:
27260201
DOI:
10.1016/j.ejpb.2016.05.025
[Indexed for MEDLINE]

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