Preparation and In- vitro Evaluation of Baclofen as an Oral Microsponge Tablets

Abstract

Baclofen (BFN) is a skeletal muscle relaxant used for the treatment of spastic muscle disorder; BFN suffers from short plasma half-life and narrow absorption window. The aim of the present study was to formulate floating effervescent microsponge tablets of BFN for controlling drug release and thereby decrease the side effects of the drug. The microsponges of BFN were prepared by non-aqueous emulsion solvent diffusion method (oil in oil emulsion method). The effects of drug: polymer ratio, stirring time and type of Eudragit polymer on the physical characteristics of microsponges were investigated. The prepared microsponges were characterized for production yield (PY), loading efficiency (LD), particle size, surface morphology, and in vitro drug release. The selected microsponge formula was incorporated into the floating effervescent gastro-retentive tablets. The prepared floating microsponge tablets were evaluated for their hardness, friability, swelling in addition to in vitro drug release. The results showed that the microsponge formula with Eudragit RS100 had optimum physical properties with PY % equal to 97 %, and LD % equal to 81% and controlled drug release (75% of drug release in 8 hr.) when compared with other formulas and pure BFN. Therefore, the non-aqueous emulsion solvent diffusion method is a promising method to produce baclofen microsponges.