Formulation, evaluation and 3² full factorial design-based optimization of ondansetron hydrochloride incorporated taste masked microspheres

Abstract

Context: Masking the bitter taste of Ondansetron hydrochloride (ONS) may improve palatability, acceptance and compliance of ONS products.

Objective: ONS-loaded, taste-masked microspheres were prepared with a polycationic pH-sensitive polymer and 3² full factorial design (FFD) was applied to optimize microsphere batches.

Materials and methods: Solvent evaporation, in acetone--methanol/liquid paraffin system, was used to prepare taste-masked ONS microspheres. The effect of varying drug/polymer (D/P) ratios on microspheres characteristics were studied by 3² FFD. Desirability function was used to search the optimum formulation. Microspheres were evaluated by FTIR, XRD and DSC to examine interaction and effect of microencapsulation process. In vitro taste assessment approach based on bitterness threshold and drug release was used to assess bitterness scores.

Results: Prepared ONS microspheres were spherical and surface was wrinkled. ONS was molecularly dispersed in microspheres without any incompatibility with EE100. In hydrochloric acid buffer pH 1.2, ONS released completely from microsphere in just 10 min. Contrary to this, ONS release at initial 5 min from taste-masked microspheres was less than the bitterness threshold.

Conclusion: Full factorial design and in vitro taste assessment approach, coupled together, was successfully applied to develop and optimize batches of ONS incorporated taste-masked microspheres.

• Desirability
• Eudragit E100
• response surface
• solvent evaporation
• taste assessment

Acknowledgements

We highly acknowledge Tirupati Medicare Ltd. (H.P., India), and Evonik Degussa India Pvt, Ltd, (Mumbai, India) for providing gift samples of ONS and EE100, respectively.