Background: :
Epilepsy is a genuine neurological turmoil that effects around 50 million individuals around the
world. Practically 30% of epileptic patients experience the ill effects of pharmaco-obstruction, which is related with social
seclusion, subordinate conduct, low marriage rates, joblessness, mental issues and diminished personal satisfaction. At
present accessible antiepileptic drugs have a restricted viability, and their negative properties limit their utilization and
cause challenges in patient administration. Gabapentin 1-(aminomethyl)cyclohexane acetic acid, Gbp , (trade name
Neurontin), a structural analog of γ-aminobutyric acid (GABA), BCS class 3 drug with having permeability issues.
Objective:
This work was an attempt to formulate and characterize a new approach to treat epilepsy by targeting to
Phospholipase A2 Enzyme through Nanostructured Lipid Carrier.
Methods:
Docking studied carried out using Accelrys Discovery studio 4.1 Client and gabapentin and
phosphotidylcholine were conjugated through chemical conjugation. Nanostructured lipid carrier (NLC) was
prepared using hot homogenization technique.
Results:
The libdock score of Gabapentin- Phosphotidylcholine conjugate (192.535) were found to be more than
Gabapentin (77.1084) and Phosphotidylcholine (150.212). For the optimized formulation the particle size (50.08), zeta
potential (-1.48), PDI (0.472) and entrapment efficiency (77.8) was observed. The NLC was studies for in-vitro drug
release studies and release kinetics. Finally found that the drug release from the NLC followed Higuchi release kinetic and
the mode of drug release from the NLC was found to be Non- Fickian diffusion.
Conclusion:
The formulated Nanostructured lipid carrier of Gabapentin-Phosphotidylcholine conjugate may be able to
use to prevent seizure.
TRPA1 Agonist Cinnamaldehyde Decreases Adipogenesis in 3T3-L1 Cells More Potently than the Non-agonist Structural Analog Cinnamyl Isobutyrate
