Intranasal delivery of gabapentin loaded optimized nanoemulsion for augmented permeation

Abstract

ObjectiveThe study made an attempt to develop and optimize gabapentin loaded mucoadhesive nanoemulsion for the direct nose to brain delivery for better management of convulsion. MethodThe nanocarrier was screened based on maximum drug solubility and capmul assisted improved permeation across the blood brain barrier for rapid relief. The optimized formulations (response surface methodology) comprising of Capmul MCM C8, Smix and constant amount of the drug were characterized for particles size and size distribution, zeta potential, morphology, pH, viscosity, percent transmittance, residence time, stability, drug content, in vitro and ex vivo permeation parameters using goat nasal mucosa. Nasal cilio toxicity study was conducted using fresh goat nasal mucosal tissue. ResultsThe optimized formulation (M130) had a particle size of 16.72 nm, zeta potential of −4.59 mV, percent transmittance of 99.99%, viscosity of 164.8 mPa s−1, residence time of 5 s and drug content of ˃ 97–99.8%. The mucoadhesive carbopol (0.5% and 0.7% w/v) addition increased zeta potential and globular size (<90 nm) which still is suitable for enhanced permeability through the nasal mucosa. Stability data suggests no significant variation in size and transparency over explored time. The toxicity of the developed nano-emulsion was also determined against the nasal mucosal lining. In vitro drug release and ex vivo permeation of M130 and RoG were found substantially high and sustained as compared to pure drug solution. Toxicity assessment corroborated no cilio-toxicity of gabapentin loaded mucoadhesive nanoemulsion with improved efficacy through intranasal administration.