Formulation and Characterization of Gabapentin-Loaded Bigel For Transpinal Delivery to Brain

Abstract

In this research, the focus was on the design and evaluation of novel two-phase systems known as bigels (BGs) for the transpinal (TS) drug delivery of gabapentin. BGs combine the advantages of hydrogels and organogels while mitigating the drawbacks of individual gels. The formulation involved preparing hydrogels and organogels using carbopol 940 in varying concentrations, which were later combined in a 1:1 ratio to produce BGs. The Fourier-transform infrared spectroscopy (FTIR) analysis indicated the interaction between the drug and polymer was nil. The formulated BG formulations underwent comprehensive characterization, including assessments of physical appearance, pH, viscosity, swelling index, spreadability, drug content, in-vitro release, ex-vivo permeation, skin irritation, and antiepileptic activity. Formulation B5 emerged as the optimized formulation based on various evaluation parameters. Skin irritation studies demonstrated compatibility with the skin, showing no adverse reactions. In antiepileptic activity, rats receiving gabapentin BG via the TS route exhibited a significant reduction in convulsion duration compared to control groups that received BG without the drug or free drug solution orally. Conclusively, the study suggests that the developed BGs containing gabapentin, when applied through the TS route on the back of the neck, hold promise for reaching the brain effectively. This method presents a potential avenue for enhanced drug delivery in the control of epilepsy.