Preparation, in vitro and in vivo evaluation of algino-pectinate bioadhesive microspheres: An investigation of the effects of polymers using multiple comparison analysis

Abstract

Aceclofenac (AC) is a phenyl acetic acid derivative [2-(2',6'-dichlorophenyl)amino] phenylacetoxyacetic acid], a novel NSAID indicated for the symptomatic treatment of pain and inflammation (1). The short biological half-life (about 4 h) and high frequency of dosing make aceclofenac an ideal candidate for sustained release. The bioadhesive microspheres of aceclofenac would prolong the residence time at the absorption site to facilitate intimate contact with the absorption surface and thereby improve and enhance bioavailability and increase patient compliance. Natural hydrophilic polymers like alginate and pectin are widely used in numerous biomedical applications for their bioadhesion properties. Alginic acid and pectin are natural polysaccharides that are widely 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.

Zinc and Calcium Cations Combination in the Production of Floating Alginate Beads as Prednisolone Delivery Systems

“…To assess the prolonged in vivo anti-inflammatory efficacy of #F4 in comparison with raw prednisolone, rats were treated by oral gavage with #F4 (Pred equivalent dose 3 mg kg −1 ) or with raw prednisolone [34], using the same doses. Samples were administered to rats in 1 mL of methylcellulose (MC) 0.5% w/v at the time 0.5, 5, or 15 h before the injection of the phlogistic agent.…”

Design and In Vivo Anti-Inflammatory Effect of Ketoprofen Delayed Delivery Systems

“…To assess the in vivo anti-inflammatory effectiveness of the optimized formulation F20 in comparison with the pure drug, rats were orally treated by gavage with F20 (ketoprofen equivalent dose 3 mg/kg) or pure ketoprofen (3 mg/kg) in 0.5% (w/v) methyl cellulose (MC). 16 Control groups received 0.5 mL of MC or blank Zn-alginate beads (F) in 0.5% (w/v) MC. Drugs were administered to rats (ketoprofen equivalent dose per os: 1, 3, and 10 mg/kg) at 5, 3, and 0.5 h before the injection of the phlogistic agent.…”

Losartan Potassium Loaded Bioadhesive Micro-Matrix System: An Investigation on Effects of Hydrophilic Polymeric Blend on Drug Release

“…Algino-guar polymeric micro matrix system of losartan potassium was fabricated by ionic gelation technique [9] ( Table 1). The polymeric excipients sodium alginate and guar gum solutions were separately prepared by dissolving both the polymers in sufficient amount of water under gentle agitation.…”

“…simulated gastric fluid whereas in simulated intestinal fluid, the carboxyl acid group and other functional groups present in sodium alginate get ionized which helps to increase its solubility and hydration property. The increase in solubility and hydration allows more solvent to penetrate the polymeric coat, produce a viscous gel and increase the bioadhesion property [9,22]. Similarly, guar gum also plays an important role in bioadhesion mechanism.…”