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Development and Evaluation of Topical Gabapentin Formulations
Christopher J Martin1, Natalie Alcock2, Sarah Hiom3
1St Mary's Pharmaceutical Unit, Cardiff and Vale UHB, Cardiff CF14 4HY, UK. C.J.Martin@bath.ac.uk.
Pharmaceutics
|September 5, 2017
Summary
Topical gabapentin formulations show promise for peripheral neuropathic pain relief. Specific hydrogel and Lipoderm® formulations effectively permeated human skin in vitro, warranting further clinical investigation.
Area of Science:
- Pharmacology
- Dermatology
- Drug Delivery
Background:
- Topical gabapentin aims to treat peripheral neuropathic pain while minimizing systemic side effects.
- Previous in vitro studies on topical gabapentin delivery yielded variable results, often dependent on the specific skin model used (e.g., rodent, porcine).
Purpose of the Study:
- To investigate the in vitro permeation of gabapentin across human skin from various topical formulations.
- To evaluate the efficacy of different bases and enhancers in facilitating gabapentin skin penetration.
Main Methods:
- Gabapentin permeation was assessed in vitro using Franz-type diffusion cells with human epidermal membranes.
- Formulations included Carbopol® hydrogels with enhancers (DMSO, ethanol) and a compounded Lipoderm® base.
- Microneedle delivery served as a positive control.
Main Results:
- Specific formulations demonstrated successful gabapentin permeation through human skin.
- A 6% gabapentin Carbopol® hydrogel with 5% DMSO or 70% ethanol, and a 10% gabapentin Lipoderm® formulation were effective.
- Results were contextualized with existing literature, highlighting the impact of skin models.
Conclusions:
- Certain topical gabapentin formulations, including specific hydrogels and a Lipoderm® base, can permeate human skin in vitro.
- Further pre-clinical and clinical studies are necessary to confirm the efficacy and safety of these topical delivery systems for neuropathic pain.
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