| Autor: |
Michiru Nagao, Masataka Tajima, Erika Sugiyama, Ryosuke Shinouchi, Keita Shibata, Masayuki Yoshikawa, Takushi Yamamoto, Vilasinee Hirunpanich Sato, Koji Nobe, Hitoshi Sato |
| Jazyk: |
angličtina |
| Rok vydání: |
2022 |
| Předmět: |
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| Zdroj: |
Pharmacology Research & Perspectives, Vol 10, Iss 2, Pp n/a-n/a (2022) |
| Druh dokumentu: |
article |
| ISSN: |
2052-1707 |
| DOI: |
10.1002/prp2.919 |
| Popis: |
Abstract In clinical practice, pregabalin is orally administered for neuropathic pain, but causes severe central nervous system side effects, such as dizziness, which results in dose limitation or discontinuation. To reduce the central side effects of pregabalin, we developed four pregabalin preparations for transdermal application: 0.4% aqueous solution, pluronic lecithin organogel (PLO gel), hydrophilic cream, and lipophilic cream. Transdermal permeabilities of pregabalin among the four formulations were compared in vitro using hairless mouse skin. The longitudinal distribution of pregabalin within the skin was analyzed using mass spectrometric (MS) imaging. Furthermore, the in vivo analgesic effects of the formulations were evaluated using the von Frey filament test in a mouse model of diabetic neuropathy (DN). The PLO gel showed the highest permeability of pregabalin, followed by the aqueous solution, and no permeation was observed in the two cream formulations. The MS imaging analysis showed that pregabalin was distributed up to the dermis in the PLO gel 1 h after application, while the aqueous solution was distributed near the epidermis. A significant analgesic effect (p |
| Databáze: |
Directory of Open Access Journals |
| Externí odkaz: |
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