Taste masking of enalapril maleate by microencapsulation in Eudragit EPO® microparticles.

Abstract

Microencapsulation is one of the most commonly used taste masking techniques. It can be accomplished by various methods, including coacervation, solvent evaporation, extrusion and spray-drying. Enalapril maleate, a bitter-tasting ACE-inhibitor, is available worldwide in conventional tablet formulations and as oral solution in the USA. The purpose of this study was to develop enalapril-loaded microparticles using spray-drying and to test their taste masking potential. Eudragit EPO® was used as a taste masking polymer for the preparation of a drugpolymer suspension. The suspension was then spray-dried under the following conditions: inlet temperature 65 °C, outlet temperature 30 °C, aspiration 100% and pump rate 10%. The drug-to-polymer ratio was varied and seven different microparticle models were developed. The yield of spray-dried particles ranged from of 51.3 to 85.4%, drug loading varied from 7.75 to 24.69% and encapsulation efficiency ranged from 58.5 to 95.7%. The particle size varied between 5.00 μm and 17.47 μm and the moisture content varied between 7.1% and 10.3%. In vitro taste assessment revealed minimal or no ENA release in artificial saliva. In vivo studies (with experimental animals and healthy volunteers) were used to evaluate the taste masking potential of spray-dried microparticles of enalapril maleate and Eudragit EPO®.