MICROENCAPSULATION BISOPROLOL FUMARATE WITH EUDRAGIT E PO BY SOLVENT EVAPORATION METHOD

Abstract

Objective: This study aimed to develop and optimize the microcapsule formula of bisoprolol fumarate-Eudragit EPO by double-emulsion solvent evaporation.
 Methods: The preparation of bisoprolol fumarate-Eudragit EPO microcapsule was done in three different ratios 1: 3 (F1), 1: 4 (F2), and 1: 5 (F3), followed by characterization of each of the microcapsule formula using Fourier transform infrared, scanning electron microscopy, particle size analyzer. Further analysis included investigation of the drug loading, entrapment efficiency, solubility in pH 6.8, and the difference among dissolution profiles of each microcapsule using one-way ANOVA.
 Results: Infra-red spectrum showed no chemical interaction between bisoprolol fumarate and Eudragit E PO in microcapsules. The morphology and structure of F1 microcapsule was irregular spheres, while F2 and F3 were regular spheres. The average particle distribution of microcapsules was 24.765±0,236 μm (F1), 28.245±0,252 μm (F2), and 40.634±0,218 μm (F3). The drug loading was 7.691±0,087 % (F1), 8.922±0,056 % (F2), and 9.012±0,133% (F3). The encapsulation efficiency was 4.980 % (F1), 5.857%(F2), and 6,285 %(F3). The average amount of bisoprolol fumarate released in pH 6.8 was 2.113±0,289 % (F1), 1.954±0,015 % (F2), and 1.619±0,020 % (F3). The dissolution profile between each formula was statistically different (p value= 0,000).
 Conclusion: As the low value of drug loading and encapsulation efficiency in each formula, we concluded that the microencapsulation formula with Eudragit EPO by solvent evaporation method is not effective to entrap bisoprolol fumarate.