Preparation and characterization of spray-dried mucoadhesive microspheres of aceclofenac.

OBJECTIVE

Microencapsulation of the anti-inflammatory drug aceclofenac (ACE) was investigated as a means of controlling drug release and minimizing or eliminating local side effects.

METHOD

Microspheres were prepared by a spray-drying technique using solutions of ACE and three polymers, namely, carbopol, chitosan, and polycarbophil, in different weight ratios.

RESULTS

The spray-dried mucoadhesive microspheres were characterized in terms of shape (scanning electron microscope), size (6.60-8.40 mum), production yield (34.10-55.62%), and encapsulation efficiency (58.14-90.57%). In vitro release studies were performed in phosphate buffer (pH 6.8) up to 10 hours. The spray-drying process of solutions of ACE with polymeric blends can give prolonged drug release. The in vitro release data were well fit into Higuchi and Korsmeyer-Peppas model and followed Fickian diffusion mechanism. In vivo data showed that the administration of ACE in polymeric microspheres prevented the gastric side effects.

CONCLUSION

The formulations here described can be proposed for the oral administration of nonsteroidal anti-inflammatory drugs with minimal side effects on gastric mucosa.