ArticlePharmacology research & perspectives2022
Evaluation of in vitro transdermal permeation, mass spectrometric imaging, and in vivo analgesic effects of pregabalin using a pluronic lecithin organogel formulation in mice.
Article in Pharmacology research & perspectives, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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7 citing papers in PubMed, 7 citations in OpenAlex.
- Effect of an experimental pregabalin gel on dental sensitivity and color change after bleaching with 35% hydrogen peroxide: a randomized clinical trial.Clinical oral investigations · 2025Trial
- Promising Glaucoma Medication: A Comprehensive Translational Evaluation.Pharmaceutics · 2026Article
- Pregabalin acts on NaPain reports · 2026Article
- Assessment of the effect of experimental gel of pregabalin associated with 35% hydrogen peroxide bleaching on bovine dental enamel: an in vitro study.Odontology · 2025Article
- Characterization and Evaluation of the Cytotoxicity of Pregabalin Gels for Oral Application.Pharmaceuticals (Basel, Switzerland) · 2024Article
- Recent Progress in Gels for Neuropathic Pain.Gels (Basel, Switzerland) · 2023Review
- Evaluation of in vitro transdermal permeation, mass spectrometric imaging, and in vivo analgesic effects of pregabalin using a pluronic lecithin organogel formulation in mice.Pharmacology research & perspectives · 2022Article
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Authors and funding
10 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
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 < .05) was observed 1.5 h after PLO gel application in the DN model mice, but the aqueous solution had no effect. This study indicated for the first time that pregabalin penetrated beyond the skin epidermis up to the dermis, from the PLO gel formulation, and that the application of this formulation exhibited an in vivo analgesic effect in the mouse model of DN.
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