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Pharmaceutics 2017, 9(3), 31; https://doi.org/10.3390/pharmaceutics9030031

Development and Evaluation of Topical Gabapentin Formulations

1
St Mary’s Pharmaceutical Unit, Cardiff and Vale UHB, Cardiff CF14 4HY, UK
2
Cardiff School of Pharmacy and Pharmaceutical Sciences, Redwood Building, King Edward VII Avenue, Cardiff University, Cardiff CF10 3NB, UK
*
Author to whom correspondence should be addressed.
Received: 23 June 2017 / Revised: 17 August 2017 / Accepted: 22 August 2017 / Published: 30 August 2017
(This article belongs to the Special Issue Penetration Enhancement of Topical Formulations)
View Full-Text   |   Download PDF [1975 KB, uploaded 30 August 2017]   |  

Abstract

Topical delivery of gabapentin is desirable to treat peripheral neuropathic pain conditions whilst avoiding systemic side effects. To date, reports of topical gabapentin delivery in vitro have been variable and dependent on the skin model employed, primarily involving rodent and porcine models. In this study a variety of topical gabapentin formulations were investigated, including Carbopol® hydrogels containing various permeation enhancers, and a range of proprietary bases including a compounded Lipoderm® formulation; furthermore microneedle facilitated delivery was used as a positive control. Critically, permeation of gabapentin across a human epidermal membrane in vitro was assessed using Franz-type diffusion cells. Subsequently this data was contextualised within the wider scope of the literature. Although reports of topical gabapentin delivery have been shown to vary, largely dependent upon the skin model used, this study demonstrated that 6% (w/w) gabapentin 0.75% (w/w) Carbopol® hydrogels containing 5% (w/w) DMSO or 70% (w/w) ethanol and a compounded 10% (w/w) gabapentin Lipoderm® formulation were able to facilitate permeation of the molecule across human skin. Further pre-clinical and clinical studies are required to investigate the topical delivery performance and pharmacodynamic actions of prospective formulations. View Full-Text
Keywords: gabapentin; topical; Carbopol®; Lipoderm®; human skin gabapentin; topical; Carbopol®; Lipoderm®; human skin
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).
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Martin, C.J.; Alcock, N.; Hiom, S.; Birchall, J.C. Development and Evaluation of Topical Gabapentin Formulations. Pharmaceutics 2017, 9, 31.

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