title: Aceclofenac-loaded unsaturated esterified alginate/gellan gum microspheres: in vitro and in vivo assessment.
abstract: Aceclofenac-loaded alginate/gellan gum microspheres for prolonged aceclofenac release were prepared through maleic anhydride-induced unsaturated esterification. The drug entrapment efficiency of these microspheres was found 39.30 ± 1.28% to 98.46 ± 0.40% and their average particle sizes were 270-490 μm. These microspheres were characterized by FTIR, DSC, P-XRD and SEM analysis. The in vitro dissolution indicated prolonged sustained release of aceclofenac over 6h, which also followed the Korsmeyer-Peppas model (R(2)=0.9571-0.9952). The microspheres prepared through 3% (w/v) maleic anhydride-induced esterification exhibited comparatively slower drug-release. Most of the microspheres were followed Fickian diffusion mechanism except the microspheres containing higher gellan gum content, which followed anomalous (non-Fickian) diffusion. The in vivo results showed sustained systemic absorption of aceclofenac in rabbits and excellent anti-inflammatory activity in carrageenan-induced rats after oral administration over prolonged period.
authors.affiliation: Department of Pharmaceutics, Gupta College of Technological Sciences, Asansol 713301, WB, India.
authors.forename: Sougata
authors.initials: S
authors.lastname: Jana
authors.forename: Arindam
authors.initials: A
authors.lastname: Das
authors.forename: Amit Kumar
authors.initials: AK
authors.lastname: Nayak
authors.forename: Kalyan Kumar
authors.initials: KK
authors.lastname: Sen
authors.forename: Sanat Kumar
authors.initials: SK
authors.lastname: Basu
mesh_terms: D000284:Administration, Oral; D000464:Alginates / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D001672:Biocompatible Materials / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D002351:Carrageenan / Q000633:toxicity; D003692:Delayed-Action Preparations / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D004008:Diclofenac / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D004195:Disease Models, Animal; D020723:Glucuronic Acid / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D006603:Hexuronic Acids / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D007249:Inflammation / Q000139:chemically induced / Q000188:drug therapy; D008297:Male; D008863:Microspheres; D011135:Polysaccharides, Bacterial / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D011817:Rabbits; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D000464:Alginates; D000894:Anti-Inflammatory Agents, Non-Steroidal; D001672:Biocompatible Materials; D003692:Delayed-Action Preparations; D006603:Hexuronic Acids; D011135:Polysaccharides, Bacterial; D004008:Diclofenac; C048288:gellan gum; D020723:Glucuronic Acid; D002351:Carrageenan; C056498:aceclofenac