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.


METHODS
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.


CONCLUSIONS
The formulations here described can be proposed for the oral administration of nonsteroidal anti-inflammatory drugs with minimal side effects on gastric mucosa.
Nagda
Chirag
C
Indukaka Ipcowala College of Pharmacy, Beyond GIDC Phase IV, Vithal Udyognagar, New Vallabh Vidyanagar, Anand, Gujarat, India. cnagda_rx@rediffmail.com
Chotai
Narendra Prabhudas
NP
Patel
Upendra
U
Patel
Sandip
S
Soni
Tejal
T
Patel
Prateek
P
Hingorani
Lal
L
D000179:Acrylates / Q000737:chemistry; D000180:Acrylic Resins / Q000737:chemistry; D000284:Administration, Oral; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000009:adverse effects; D002626:Chemistry, Pharmaceutical / Q000379:methods; D048271:Chitosan / Q000737:chemistry; D003692:Delayed-Action Preparations; D004008:Diclofenac / Q000008:administration & dosage / Q000009:adverse effects / Q000031:analogs & derivatives*; D004058:Diffusion; D004337:Drug Carriers / Q000737:chemistry*; D008297:Male; D008855:Microscopy, Electron, Scanning; D008863:Microspheres; D051381:Rats; D017208:Rats, Wistar
D000179:Acrylates; D000180:Acrylic Resins; D000894:Anti-Inflammatory Agents, Non-Steroidal; D003692:Delayed-Action Preparations; D004337:Drug Carriers; C117167:carbopol 974P NF; D004008:Diclofenac; C030312:calcium polycarbophil; D048271:Chitosan; C056498:aceclofenac