Formulation and evaluation of ergotamine tartrate Lyophilized nasal insert

Abstract

Lyophilized nasal inserts represent an alternative route for the administration of drugs. The aim of this study is to prepare a firm single dose unit of nasal insert containing ergotamine tartrate which allows easy administration in the nasal cavity and prevent first pass metabolism leading to increased bioavailability. The insert was prepared by applying freeze drying technique using 2% w/w of different polymers.The prepared inserts were evaluated for appearance, bioadhesion potential, water uptake, in vitro drug release and imaged by scanning electron microscopy.The results showed that the prepared nasal inserts have a smooth surface and a spongy-like appearance. No interaction occurred between the drug and different polymers as revealed in DSC and FT-IR. Higher viscosity of the polymer causes a greater degree of water uptake and high bioadhesion potential; this in turn reduces the drug release, as the diffusional path length of drug becomes longer. The study revealed an inverse relationship between water uptake, bioadhesion potential and in vitro drug release. The order of drug release from different inserts is HPMC E5 > PVP K90 > Sodium aliginate > Carrageenan > NaCMC > Xanthan Gum > Chitosan.