Preparation and characterization of spray-dried mucoadhesive microspheres of aceclofenac

Abstract

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 μm), 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.

Keywords:

• Aceclofenac
• gastric side effects
• mucoadhesive microspheres
• spray-drying method

Acknowledgments

The authors are grateful to Pharmenza Herbals Pvt. Ltd., Kaniya, Anand, and SICART, Vallabh Vidyanagar, Anand, for providing necessary facilities. The authors are also grateful to Comed Chemicals Limited, Vadodara, India, for providing drug sample.

Declaration of interest: The authors report no conflicts of interest.