Preparation of -pullulan-Based Semi-interpenetrating Polymer Network Gastroretentive Microspheres of Amoxicillin Trihydrate and Optimization by Response Surface Methodology.

OBJECTIVES

In this study, a novel and pullulan-based semi-interpenetrating polymer network gastroretentive microsphere formulation was prepared using the emulsion crosslinking method and optimized by central composite design.

MATERIALS AND METHODS

The effects of the amounts of glutaraldehyde, , and pullulan on the percent drug entrapment efficiency (EE), percent mucoadhesion at 12 h, and percent drug release at 12 h were optimized. The microspheres were characterized using scanning electron microscopy, fourier transform infrared spectroscopy, and differential scanning calorimetry.

RESULTS

The formulation containing 4% v/v glutaraldehyde, 8.28% w/v pullulan, and 2.14% w/v had 88.75±1.18% EE, 80.43±1.2% drug release at 12 h, and 81.73±1.50% mucoadhesion at 12 h, which was considered optimum and was used in an radiographic study.

CONCLUSION

Semi-interpenetrating polymer network microspheres loaded with amoxicillin trihydrate were successfully prepared using and pullulan. The prolonged retention of microspheres in the stomach with sustained drug release could effectively act against reservoirs in the stomach and improve the therapeutic effect of amoxicillin trihydrate against .