Formulation and In-vitro Characterization of floating microcapsules as gastroretentive drug delivery system containing Itopride hydrochloride by W/O/O multiple emulsion solvent diffusion technique

Abstract

Itopride hydrochloride loaded floating microcapsules were prepared by W/O/O multiple emulsion solvent diffusion method using ethyl cellulose and eudragit RSPO 100 as drug release rate controlling polymers. Drug containing aqueous phase was emulsified in ACN: DCM primary organic phase. This W/O primary emulsion was further emulsified in continuous phase (light liquid paraffin) containing emulsifying agent (span 80).Formulated microcapsules were harvested by filtration and subsequent washing with petroleum ether. Further microcapsules were evaluated for flow properties, %product yield, particle size, %EE, buoyancy, in-vitro drug release, SEM, FTIR and DSC analysis.Floating microcapsules were prepared with varying proportions of EC and eudragit RSPO 100. Microcapsules containing drug: EC: Eudragit RSPO 100 (Formulation F5) in proportion of 1:2:1shows desired properties. All formulations show good to excellent flow properties. F5 formulation shows 91.41± 2.84% production yield, mean particle size was29.39± 5.45µm, %buoyancy 88.27±1.75%, EE 98.53±0.349%. Cumulative % drug release from microcapsules of F5 formulation was 98.99± 1.90% in 24hours and following Korsmeyer–Peppas kinetic model for drug release with R2 value 0.9805. SEM analysis revealed formation of spherical microcapsules with rough surface indicates encapsulation of drug within polymer coat. FTIR and DSC analysis shows no interaction between drug and polymers used in formulation.Formulated multiple unit floating gastroretentive microcapsules of Itopride hydrochloride have potential to delivered drug in upper part of GIT for extended period of time, thereby reducing dosing frequency, enhance bioavailability and improved patient compliance.