MUCOADHESIVE MICROSPHERES OF METOPROLOL SUCCINATE FORMULATION AND IN VITRO EVALUATION STUDIES

Tarakaramarao Challa

Abstract


The design and formulation of mucoadhesive microspheres seem to be a potential candidate as an oral controlled drug delivery system in prolonging the drug retention in GIT, and increasing the bioavailability of drug.Objective: The present research has been a satisfactory attempt to formulate a mucoadhesive micro particulate system of controlled release of metoprolol succinate. Methods: The investigation has indicated that Emulsification internal gelation technique can be successfully employed to metoprolol Succinate loadedalginate microspheres. The biocompatible polymers like sodium alginate, HPMC K4M, chitosan and PVP K30 can be used to formulate a muco adhesive micro particulate system. Results: The scanning electron micrpscopy (SEM) analysis of the microspheres revealed that sodium alginate-HPMC K4M and sodium alginate-chitosan microspheres were smooth, spherical and slightly aggregated particles when compared with the microspheres of sodium alginate-PVP K30 which were porous, rough, grossly, discrete spherical. As the polymer concentration was increased the % drug loading decreased and % entrapment efficiency was increased due to increase in the viscosity of the solution. The mucoadhesive microspheres of drug with sodium alginate-chitosan were less adhesive to mucus when compared to sodium alginate-HPMC K4M and sodium alginate- PVP K30 which showed greater adhesive strength. The formulations F1 to F9 were best fitted into first order kinetic model and the drug release from the formulation was by non-fickcian (anomalous) diffusion mechanism. Conclusion: The selected formulations F3, F6 and F9 microspheres were stable and compatible at the selected temperature and humidity in storage for 60 days. From the stability studies it was found that there was no significant change in the drug entrapment, release characteristics and in-vitro adhesive behavior of the microspheres.

Key words: Microsphere, Mucoadhesives, SEM, Drug Entrapment and Stability.


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