Abstract
Background:A novel drug delivery system for treating acute epileptic condition.Objective:To develop an intranasal mucoadhesive formulation of Lamotrigine (LTG) loaded insitu gel, for the treatment of epilepsy to avoid possible side effects and first pass metabolism associated with conventional treatment.Methods:Lamotrigine was loaded into different polymeric solutions of gellan and xanthan gum.Results:All formulations subjected to various evaluation studies were within their acceptable limits. The pH of formulation ranges between 5.8 ±.001 to 6.8 ±.005 indicating that no mucosal irritation is expected as pH was in acceptable range. Invitro drug release from the mucoadhesive insitu gel formulations showed immediate drug release pattern with a maximum drug release of 97.02 ±0.54% for optimized G5 formulation within 20min. Exvivo permeation studies of optimized formulation G5 and control formulation was estimated. Exvivo permeation studies of G5 insitu formulation done for a period of 12 h resulted in slow, sustained release and greater permeability significance(P <0.05) through nasal mucosa when compared to control. Histopathological studies showed that G5 formulation was safer for nasal administration without any irritation. The stability studies indicated that gels were stable over 45 days in refrigerated condition (4±2ºC).Conclusion:The intranasal insitu gelling system is a promising novel drug delivery system for an antiepileptic drug lamotrigine which could enhance nasal residence time with increased viscosity and mucoadhesive character and provided better release profile of drug for treating acute epileptic conditions.
Highlights
Epilepsy is a neurological disorder of brain characterized by sudden recurrent episodes of sensory disturbances with brief loss of consciousness and awareness, which lead to seizures
AEDs (Antiepileptic drugs) are the medications used in the treatment of epileptic seizure, some of them act by targeting the voltage gated Na+ and Ca+ channel while some act in stimulating GABA system
The reason for selecting intranasal insitu drug delivery is because of its large surface area for drug absorption, as it avoids first pass metabolism and it help in delivering drug to CNS thereby by passing BBB, there is rapid onset of pharmacological action and higher bioavailability of lipophilic drugs like lamotrigine
Summary
Epilepsy is a neurological disorder of brain characterized by sudden recurrent episodes of sensory disturbances with brief loss of consciousness and awareness, which lead to seizures. AEDs (Antiepileptic drugs) are the medications used in the treatment of epileptic seizure, some of them act by targeting the voltage gated Na+ (sodium) and Ca+ (calcium) channel while some act in stimulating GABA system. This article mainly helps in evaluating and developing an insitu gel loaded with lamotrigine. The reason for selecting intranasal insitu drug delivery is because of its large surface area for drug absorption, as it avoids first pass metabolism and it help in delivering drug to CNS thereby by passing BBB, there is rapid onset of pharmacological action and higher bioavailability of lipophilic drugs like lamotrigine. Intranasal insitu gel is developed for the purpose of immediate release of lamotrigine for treating acute epileptic condition, which is very essential in treating an emergency condition [3 - 24]. A novel drug delivery system for treating acute epileptic condition
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