Spray drying formulation of albendazole microspheres by experimental design. In vitro–in vivo studies

Abstract

Both an experimental design and optimization techniques were carried out for the development of chitosan–pectin–carboxymethylcellulose microspheres to improve the oral absorption of albendazole as a model drug. The effect of three different factors (chitosan, pectin and carboxy methyl cellulose concentrations) was studied on five responses: yield, morphology, dissolution rate at 30 and 60 min, and encapsulation efficiency of the microspheres. During the screening phase, the factors were evaluated in order to identify those which exert a significant effect. Simultaneous multiple response optimizations were then used to find out experimental conditions where the system shows the most adequate results. The optimal conditions were found to be: chitosan concentration, 1.00% w/v, pectin concentration 0.10% w/v and carboxymethylcellulose concentration 0.20% w/v. The bioavailability of the loaded drug in the optimized microspheres was evaluated in Wistar rats which showed an area under curve (AUC) almost 10 times higher than the pure drug.

• Albendazole
• biomaterials
• microspheres
• oral drug release
• spray drying

Acknowledgements

We would like to thank Marcela Culasso, María Robson, Mariana de Sanctis and Geraldine Raimundo for their assistance in the correction of the language.

Declaration of interest

The authors report no conflicts of interest. The authors alone are responsible for the content and writing of this article.

A.G. and G.P. are grateful to CONICET for a Doctoral and a Post-Doctoral Fellowship. The University of Rosario, CONICET (Consejo Nacional de Investigaciones Científicas y Técnicas, Project No. PIP 112-201001-00194) and ANPCyT (Agencia Nacional de Promoción Científica y Tecnológica, Project No. PICT 2006-1126) are gratefully acknowledged for financial support.