Development and evaluation of floating microspheres of Pioglitazone hydrochloride using ethyl cellulose 

By Satish V. Shirolkar, Mukund.G. Tawar, Nishant. S. Gandhi, Nilesh B Deore.  

ABSTRACT

Various approaches have been used to retain the dosage form in the stomach as a way of increasing the gastric residence time (GRT), including floatation systems; high-density systems; mucoadhesive systems; magnetic systems; unfoldable, extendible, or swellable systems; and superporous hydrogel systems. The aim of this study was to prepare and evaluate floating microspheres of Pioglitazone hydrochloride for the prolongation of gastric residence time. The microspheres were prepared by emulsion solvent diffusion-evaporation method using ethyl cellulose and HPMC K100M. A full factorial design was applied to optimize the formulation. Preliminary studies revealed that the concentration of polymer and stirring speed significantly affected the characteristics of floating microspheres. The optimum batch of microsphere exhibited smooth surfaces with good flow and packing properties, prolonged sustained drug release, remained buoyant for more than 10 hrs, high entrapment efficiency upto 97%w/w. Scanning electron microscopy confirmed the hollow structure with particle size in the order of 190 µm. The studies revealed that increase in concentration of hydrophillic polymer (HPMC) increased the drug release from the floating mcirospheres. The results of 32 full factorial design revealed that the concentration of ethylcellulose 10 cps (X1) and stirring speed (X2) significantly affected drug entrapment efficiency, percentage release after 8 h and particle size of microspheres.  

Key words: - Pioglitazone hydrochloride, ethyl cellulose, solvent diffusion evaporation, floating microspheres, factorial design.

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