Design and Evaluation of Imatinib Mesylate Loaded Microspheres for Stomach Specific Drug Delivery

Aims: The aim of the present work was to design and evaluate the Imatinib mesylate microspheres using natural and semi synthetic polymers for stomach specific drug delivery.
Study Design: Design and Evaluation of Imatinib Mesylate loaded microspheres
Place and Duration of the Study: The study was carried out in Department of Pharmaceutics, JKKMMRF’s Annai JKK Sampoorani Ammal College of Pharmacy, between November 2012 and July 2013.
Methodology: The microspheres were prepared using Sodium alginate as a polymer by Emulsification Ionic Gelation Technique. Copolymers of natural origin namely Guar gum, Karaya gum, Chitosan and semi synthetic origin namely Hydroxy propoylmethyl cellulose K4M, K15M, K100M are used as mucoadhesive polymers. The prepared microspheres were evaluated for their percentage yield, entrapment efficiency, degree of swelling, particle size, surface morphology and in-vitro mucoadhesion, drug release studies. Drug release kinetics was determined from drug release data. Selected formulations are subjected to stability studies under varying conditions of temperature and humidity.
Results: The production yields of microspheres were found to be between 76.74 to 88.18%. Percentage drug entrapment efficiency of Imatinib mesylate microspheres was ranged from 65.51 to 88.78%. Particle size of the prepared microspheres was in the size range of 440-810µm. SEM analysis revealed that all the prepared microspheres were discrete, spherical in shape. The in-vitro mucoadhesive study demonstrated that Hydroxy propoylmethyl cellulose adhered to the mucus to a greater extent than other polymers. The in-vitro release study shows that, retarded release with increase in percentage of polymers. The release of drug from the microspheres followed Krosmeyer Peppas kinetics. After the stability studies, the formulations remained stable at the end of storage period.
Conclusion: Based on the results, it was concluded that, the formulations with natural polymers were found to be best than semi synthetic polymers for the oral delivery of Imatinib mesylate.