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Analgesic Efficacy and Transdermal Penetration of Topical Gabapentin Creams: Finding an Optimal Dose and Pre-treatment Time

Author(s):  Heustess Allie,Spigener Shuler,Sweitzer Sarah,Romero-Sandoval Alfonso,Asbill Scott

Issue:  Mar/Apr 2015 – Volume 19, Number 2
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Abstract:  Many patients with chronic neuropathic pain continue to suffer despite traditional pharmacotherapy. As a result, pharmacists commonly compound gabapentin into creams, gels, and ointments as an alternative treatment option. In this study, various concentrations (1%, 5%, and 10%) of topical gabapentin compounded in Lipoderm were applied at various pre-treatment times (30 minutes, 1 hour, and 4 hours) to investigate what gabapentin concentration and pre-treatment time best attenuates formalin-induced nociceptive behaviors in a rodent model. A 30-minute pre-treatment with 5% gabapentin demonstrated maximum attenuation of nociceptive behaviors in this in vivo preclinical pain model. Nociceptive behaviors unexpectedly increased when gabapentin concentration or pre-treatment time was increased, suggesting both antinociceptive and pronociceptive effects of transdermal gabapentin administration. Gabapentin permeation into the skin and deeper tissues of the hindpaw was measured following the in vivo study. Skin and deep tissue permeation of gabapentin was both dose and time-dependent. Maximum deep tissue permeation occurred within 30 minutes of topical application. Skin concentrations increased with a longer 1-hour pre-treatment. Minimal skin and deeper tissue levels were found following a 4-hour pre-treatment. These results suggest that topical gabapentin may be antinociceptive in a rodent formalin model at specific doses and pre-treatment intervals.

Related Keywords: Allie Heustess, Shuler Spigener, Sarah Sweitzer, PhD, Alfonso Romero-Sandoval, PhD, Scott Asbill, PhD, gabapentin, chronic pain, neuropathic pain, neuropathy, topical analgesics, topical preparation, transdermal delivery, skin permeation, transdermal penetration, formalin pain model, dose-dependent pain relief, analgesia, voltage-dependent calcium channel blocker, alpha-2-delta subunit inhibitor, pain-related behavior, antinociception



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