Development of Rizatriptan Benzoate Microspheres for Nose to Brain Delivery

Abstract

The purpose of present work was to develop mucoadhesive microspheres for nasal delivery. This would avoid the first pass effect and thereby significantly improve the bioavailability of rizatriptan benzoate. Ethyl cellulose 45 cps was selected as synthetic mucoadhesive polymer due to its non-toxic nature and potential for sustained release. Microspheres were prepared by two methods. First method was emulsion solvent diffusion method. T he Prepared microsphere were evaluated for % entrapment efficiency and it was less than 20% with this method. So, attempt was made to encapsulate RIZA with sufficiently high entrapment efficiency by w/o/o double emulsion solvent diffusion method using a non-aqueous processing medium. Various preliminary trials were taken to optimize process and formulation parameters. The prepared microspheres were evaluated with respect to particle size, entrapment efficiency, % drug loading, % practical yield, in-vitro drug release, drug permeation. All the formulations showed good entrapment efficiency. Best batch showed entrapment more than 85% and released drug up to 8 h.