Formulation and Evaluation of Gastroretentive Microballoons Containing Baclofen for a Floating Oral Controlled Drug Delivery System
The objective of the present study was to fabricate and evaluate a multiparticulate oral gastroretentive dosage
form of baclofen characterized by a central large cavity (hollow core) promoting unmitigated floatation with practical applications
to alleviate the signs and symptoms of spasticity and muscular rigidity. Solvent diffusion and evaporation procedure
were applied to prepare floating microspheres with a central large cavity using various combinations of ethylcellulose
(release retardant) and HPMC K4M (release modifier) dissolved in a mixture of dichloromethane and methanol (2:1).
The obtained microspheres (700-1000 µm) exhibit excellent floating ability (86±2.00%) and release characteristics with
entrapment efficiency of 95.2±0.32%. Microspheres fabricated with ethylcellulose to HPMC K4M in the ratio 8.5:1.5 released
98.67% of the entrapped drug in 12 h. Muscle relaxation caused by baclofen microspheres impairs the rotarod performance
for more than 12 h. Abdominal X-ray images showed that the gastroretention period of the floating barium sulfate-
labeled microspheres was no less than 10 h. The buoyant baclofen microspheres provide a promising gastroretentive
drug delivery system to deliver baclofen in spastic patients with a sustained release rate.
Keywords: Abdominal x-ray imaging, Baclofen, Central large cavity, Floating sustained release microspheres, Rotarod.
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