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.
Copyright © 2013 Elsevier B.V. All rights reserved.
MeSH terms
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Administration, Oral
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Alginates* / chemistry
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Alginates* / pharmacokinetics
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Alginates* / pharmacology
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Animals
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Anti-Inflammatory Agents, Non-Steroidal* / chemistry
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Anti-Inflammatory Agents, Non-Steroidal* / pharmacokinetics
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Anti-Inflammatory Agents, Non-Steroidal* / pharmacology
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Biocompatible Materials* / chemistry
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Biocompatible Materials* / pharmacokinetics
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Biocompatible Materials* / pharmacology
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Carrageenan / toxicity
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Delayed-Action Preparations / chemistry
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Delayed-Action Preparations / pharmacokinetics
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Delayed-Action Preparations / pharmacology
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Diclofenac / analogs & derivatives*
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Diclofenac / chemistry
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Diclofenac / pharmacokinetics
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Diclofenac / pharmacology
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Disease Models, Animal
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Glucuronic Acid / chemistry
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Glucuronic Acid / pharmacokinetics
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Glucuronic Acid / pharmacology
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Hexuronic Acids / chemistry
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Hexuronic Acids / pharmacokinetics
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Hexuronic Acids / pharmacology
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Inflammation / chemically induced
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Inflammation / drug therapy
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Male
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Microspheres*
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Polysaccharides, Bacterial* / chemistry
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Polysaccharides, Bacterial* / pharmacokinetics
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Polysaccharides, Bacterial* / pharmacology
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Rabbits
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Rats
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Rats, Sprague-Dawley
Substances
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Alginates
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Anti-Inflammatory Agents, Non-Steroidal
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Biocompatible Materials
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Delayed-Action Preparations
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Hexuronic Acids
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Polysaccharides, Bacterial
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Diclofenac
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gellan gum
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Glucuronic Acid
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Carrageenan
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aceclofenac