Development and Evaluation of Multiple Particulate Floating Drug Delivery for Novel Sustained-Release Microbeads of Baclofen

Abstract

The objective of the work on a type of multiparticulate floating alginate microbeads was prepared by the Ionotropic gelation method with gas forming agent Calcium Carbonate. Attempts were made to enhance the drug encapsulation efficiency and delay the drug release by adding chitosan into the gelation medium and by coating with Eudragit, respectively. It was found that the drug encapsulation efficiency of chitosan-alginate microbeads was much higher than that of the calcium alginate microbeads. Floating alginate microbeads were formulated using baclofen a skeletal muscles relaxant as a drug. The formulation was prepared with Sodium alginate, gas forming agent like CaCO3 and chitosan was optimized for different weight ratios. The microbeads were for entrapment efficiency of the obtained formulations was in between 68.50-78.87% and in-vitro release of optimized formulation in 24 hrs. Fourier Transform Infrared Spectroscopy, Scanning Electron Microscopy, Differential Scanning Calorimetry and X-Ray studies were performed for optimized formulation. Drug and excipients compatibility was studied by Fourier Transform Infrared Spectroscopy and no incompatibility was observed. From the results of Scanning Electron Microscopy it’s revealed that microsbeads was found in spherical and porous nature. From the Differential Scanning Calorimetry attributed to the fact that the incorporated drug was embedded in a molecular dispersed from inside the cross-linked particle matrix. X-ray studies in healthy human male which showed the position of beads in the upper part of the stomach. Coating microbeads was able to continuously float over the simulated gastric fluid (SGF) for 24h in vitro. In the present study, a multiparticulate system with excellent floating ability, optimum drug entrapment efficiency and suitable sustain release formulation has been developed.