Preparation, in vitro and in vivo evaluation of algino-pectinate bioadhesive microspheres: An investigation of the effects of polymers using multiple comparison analysis.
Ionotropic gelation was used to entrap aceclofenac into algino-pectinate bioadhesive microspheres as a potential drug carrier for the oral delivery of this anti-inflammatory drug. Microspheres were investigated in vitro for possible sustained drug release and their use in vivo as a gastroprotective system for aceclofenac. Polymer concentration and polymer/drug ratio were analyzed for their influence on microsphere properties. The microspheres exhibited good bioadhesive property and showed high drug entrapment efficiency. Drug release profiles exhibited faster release of aceclofenac from alginate microspheres whereas algino-pectinate microspheres showed prolonged release. Dunnet's multiple comparison analysis suggested a significant difference in percent inhibition of paw edema when the optimized formulation was compared to pure drug. It was concluded that the algino-pectinate bioadhesive formulations exhibit promising properties of a sustained release form for aceclofenac and that they provide distinct tissue protection in the stomach.
P. G. Department of Pharmaceutics, College of Pharmaceutical Sciences, Berhampur-760002 Orissa, India. santanu_nil@rediffmail.com
Santanu
S
Chakraborty
Madhusmruti
M
Khandai
Anuradha
A
Sharma
Nazia
N
Khanam
Ch Niranjan
ChN
Patra
Subas Chandra
SC
Dinda
Kalyan Kumar
KK
Sen
D000268:Adhesiveness; D000284:Administration, Oral; D000464:Alginates / Q000737:chemistry*; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000009:adverse effects / Q000494:pharmacology; D003692:Delayed-Action Preparations; D004008:Diclofenac / Q000008:administration & dosage / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000494:pharmacology; D004195:Disease Models, Animal; D004337:Drug Carriers / Q000737:chemistry; D004487:Edema / Q000188:drug therapy / Q000503:physiopathology; D020723:Glucuronic Acid / Q000737:chemistry; D006603:Hexuronic Acids / Q000737:chemistry; D007249:Inflammation / Q000188:drug therapy / Q000503:physiopathology; D008297:Male; D008863:Microspheres; D010368:Pectins / Q000737:chemistry*; D051381:Rats; D017208:Rats, Wistar; D013270:Stomach / Q000187:drug effects
D000464:Alginates; D000894:Anti-Inflammatory Agents, Non-Steroidal; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D006603:Hexuronic Acids; D004008:Diclofenac; D010368:Pectins; D020723:Glucuronic Acid; C056498:aceclofenac