Development and Evaluation of Topical Gabapentin Formulations
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 t...
Main Authors: | , , , |
---|---|
Format: | Article |
Language: | English |
Published: |
MDPI AG
2017-08-01
|
Series: | Pharmaceutics |
Subjects: | |
Online Access: | https://www.mdpi.com/1999-4923/9/3/31 |
id |
doaj-c920605f54f64e2db70efbacd5d670eb |
---|---|
record_format |
Article |
spelling |
doaj-c920605f54f64e2db70efbacd5d670eb2020-11-25T02:28:58ZengMDPI AGPharmaceutics1999-49232017-08-01933110.3390/pharmaceutics9030031pharmaceutics9030031Development and Evaluation of Topical Gabapentin FormulationsChristopher J. Martin0Natalie Alcock1Sarah Hiom2James C. Birchall3St Mary’s Pharmaceutical Unit, Cardiff and Vale UHB, Cardiff CF14 4HY, UKCardiff School of Pharmacy and Pharmaceutical Sciences, Redwood Building, King Edward VII Avenue, Cardiff University, Cardiff CF10 3NB, UKSt Mary’s Pharmaceutical Unit, Cardiff and Vale UHB, Cardiff CF14 4HY, UKCardiff School of Pharmacy and Pharmaceutical Sciences, Redwood Building, King Edward VII Avenue, Cardiff University, Cardiff CF10 3NB, UKTopical 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.https://www.mdpi.com/1999-4923/9/3/31gabapentintopicalCarbopol®Lipoderm®human skin |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
Christopher J. Martin Natalie Alcock Sarah Hiom James C. Birchall |
spellingShingle |
Christopher J. Martin Natalie Alcock Sarah Hiom James C. Birchall Development and Evaluation of Topical Gabapentin Formulations Pharmaceutics gabapentin topical Carbopol® Lipoderm® human skin |
author_facet |
Christopher J. Martin Natalie Alcock Sarah Hiom James C. Birchall |
author_sort |
Christopher J. Martin |
title |
Development and Evaluation of Topical Gabapentin Formulations |
title_short |
Development and Evaluation of Topical Gabapentin Formulations |
title_full |
Development and Evaluation of Topical Gabapentin Formulations |
title_fullStr |
Development and Evaluation of Topical Gabapentin Formulations |
title_full_unstemmed |
Development and Evaluation of Topical Gabapentin Formulations |
title_sort |
development and evaluation of topical gabapentin formulations |
publisher |
MDPI AG |
series |
Pharmaceutics |
issn |
1999-4923 |
publishDate |
2017-08-01 |
description |
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. |
topic |
gabapentin topical Carbopol® Lipoderm® human skin |
url |
https://www.mdpi.com/1999-4923/9/3/31 |
work_keys_str_mv |
AT christopherjmartin developmentandevaluationoftopicalgabapentinformulations AT nataliealcock developmentandevaluationoftopicalgabapentinformulations AT sarahhiom developmentandevaluationoftopicalgabapentinformulations AT jamescbirchall developmentandevaluationoftopicalgabapentinformulations |
_version_ |
1724835261119987712 |