Formulation, Development and Evaluation of Nasal In situ Gel of Pregabalin

Abstract

The objective of the present work is to formulate, develop and evaluate nasal in situ gel of Pregabalin to provide better therapy for Epilepsy. Pregabalin is BCS class I drug. It is 3rd generation anticonvulsant used in epilepsy in which faster action is required. Nasal route has faster action than oral route, also convenient to unconscious patient. Pregabalin loaded in situ gel, for the treatment of epilepsy to avoid side effects and first pass metabolism associated with conventional treatment and increase bioavailability. Pregabalin was loaded into different polymeric solutions of Polycarbophil and HPMC K4M. The drug was characterized for various parameters like UV-Spectroscopy, FTIR Spectroscopy and DSC study. Excipients were screened for selection of mucoadhesive and gelling polymer. Then the drug was formulated as in situ gel. The experiment was subjected to 32 full factorial design, the concentration of Polycarbophil (X1) and HPMC K4M (X2) were selected as independent variables with % drug release and muco-adhesive strength as dependent variables. The kinetic study was carried out for 30 days. Polycarbophil was selected as mucoadhesive and gelling polymer. The values for X1 and X2 were 0.3922% and 0.5263% relating the % drug release and mucoadhesive strength values were 78.20% CDR at 240 min. and 960 dynes/cm2 respectively for checkpoint batch following zero order and Higuchi kinetic. The formulation was found to be stable for 30 days. The present research will be helpful in order to improve the efficacy and tolerability of the antiepileptic drug therapy. So alternative administration strategy has been investigated which deliver nasally administered medication directly to brain effectively. The intranasal in situ gelling system is a promising novel drug delivery system for an antiepileptic drug Pregabalin which could enhance nasal residence time with increased viscosity and mucoadhesive character and provided better release profile of drug for treating epileptic conditions.