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FORMULATION AND IN VITRO EVALUATION OF SUSTAINED RELEASE MICROPARTICLES OF LOXOPROFEN SODIUM
Sherbaz Bilal, Pharm-D, Qaiser Iqbal, PhD* and Syed Umer Jan, PhD
Background: Loxoprofen sodium is an essential NSAID which is 2-arylpropionoc acid derivative. It owns a very short half-life and principally used for treating osteoarthritis & rheumatoid arthritis. So far there is no loxoprofen sodium‘s modified release dosage form available and is commercialized as tablets and transdermal patches only. Objective: The aim of this study was to develop and characterize the sustained and prolonged release microparticles of loxoprofen sodium by utilizing HPMC as a bio-polymer. Methods: Coacervation-phase separation technique was used in this study. The prepared microparticles went through in-vitro evaluation to observe the outcome of various parameters (polymer to drug ratio, stirring speed, and stirring time) on the physiochemical behaviors of prepared micro particles. Prepared microparticles exhibited excellent encapsulation efficiency and percentage yield, i.e. up to 91.71% & 88.94% respectively. Micrometrics examination showed the evidence of good flow characteristics of microparticles. By using USP defined dissolution apparatus at pH 6.8 for 12 hours at 37 ± 0.5°C dissolution studies for the prepared formulations were performed. The accumulative drug release was retarded with the increase in drug to polymer ratio during observation. Most of the prepared batches were in pursuit of higuchi model of release trough Fickian diffusion model. The optimal batch F6 was selected for further assessment FTIR, SEM and XRD. Results and Discussion: FTIR results showed no interaction between polymer and drug. XRD proved the stability of the product. Scanning electron micrographs depict that the particles had, heterogeneous, irregular and porous surface. Mean diameter was calculated as 200 ?m. Thus the microparticles were prepared successfully using best polymer and technique.[Full Text Article]