Nano and Microparticulate Chitosan Based System for Formulation of Carvedilol Rapid Melt Tablet

Abstract

Purpose: In the present study rapid melt tablets (RMT’s) of carvedilol were prepared by using ionotropic-gelated chitosan nanoparticles using a spray-drying method. Carvedilol is beta-adrenergic antagonist and its oral bioavailability is about 25-35% because of first pass metabolism. Methods: The spray-dried microparticles were formulated into RMT’s using a wet granulation process. The Formulation and optimization of carvedilol loaded RMTs using nano and microparticulate chitosan based system (NMCS) was done by using 32 factorial designs. Results: Drug entrapment efficiency of about 64.9 % (w/w) and loading capacity of 14.44% (w/w) were achieved for the microparticles, which were ranged from 1 μm to 4 μm in diameter. Results of disintegration tests showed that the formulated RMTs could be completely dissolved within 40 seconds. Dissolution studies suggested that Carvedilol is released more slowly from tablets made using the microencapsulation process compared with tablets containing Carvedilol that is free or in the form of nanoparticles. Conclusion: Results shown that the development of new RMTs designed with crosslinked microparticle might be a rational way to overcome the unwanted taste of conventional RMTs and the side effects related to Carvedilol intrinsic characteristics. The development of Carvedilol NMCS using ludiflash as RMTs could be used as a promising approach for improving the solubility and oral bioavailability of water insoluble drug.

Keywords: Carvedilol, Chitosan, Nano and Microparticulate System, Spray-drying, Rapid melt tablets