Formulation and evaluation of baclofen liposome vesicles using lecithin / Formulación y evaluación de vesículas de liposomas de baclofeno usando lecitina

ABSTRACT

INTRODUCTION: The main aim of present study was to prepare and characterize liposomal formulation of baclofen to improve the effectiveness of the topically applied formulation. METHOD: For the preparation of liposomes, different ratio of lecithin, cholesterol and ethanol were taken but ratio of drug and stearic acid were kept constant and prepared by ethanol injection method. Liposomes were characterized for vesicle size, vesicle shape, entrapment efficiency, in vitro studies, stability studies and in vivo studies. RESULTS: The average particle size of formulated liposome was in the range of 3.98 ± 0.45-4.24 ± 0.65 mim and small unilamellar vesicles with spherical in shape observed. Entrapment efficiency of optimized formulation was 58.67 ± 0.81 %. The maximum % cumulative drug release behaviours were 67.66 ± 5.32 % after 10 h. formulation stored in 4 ± 2 °C temperature shows better stability (64.19 ± 0.26) compared to elevated temperature. Swiss albino mice were used for the in vivo study and exhibit muscle relaxant activity in terms of no. of falls from rota rod apparatus (p value = 0.001). CONCLUSIONS: Baclofen loaded liposomal formulation have shown skeletal muscle relaxant activity in mice suggesting delivery of baclofen from liposomes in the therapeutic range