Development of Floating-Mucoadhesive Microsphere for Site Specific Release of Metronidazole.

Md Lutful Amin,Md Abdul Mannan,Tajnin Ahmed

doi:10.15171/apb.2016.027

Md Lutful Amin, Md Abdul Mannan + Show 1 more

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https://doi.org/10.15171/apb.2016.027

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Abstract

The purpose of this study was to develop and evaluate metronidazole loaded floating-mucoadhesive microsphere for sustained drug release at the gastric mucosa. Alginate gastroretentive microspheres containing metronidazole were prepared by ionic gelation method using sodium bicarbonate as gas forming agent, guar gum as mucoadhesive polymer, and Eudragit L100 as drug release modifier. Carbopol was used for increasing the bead strength. The microspheres were characterized by scanning electron microscopy and evaluated by means of drug entrapment efficiency, in vitro buoyancy, and swelling studies. In vitro mucoadhesion and drug release studies were carried out in order to evaluate site specific sustained drug release. All formulations showed 100% buoyancy in vitro for a prolonged period of time. Amount of guar gum influenced the properties of different formulations. The formulation containing drug and guar gum at a ratio of 1:0.5 showed the best results with 76.3% drug entrapment efficiency, 61.21% mucoadhesion, and sustained drug release. Carbopol was found to increase surface smoothness of the microspheres. Metronidazole mucoadhesive-floating microspheres can be effectively used for sustained drug release to the gastric mucosa in treatment of upper GIT infection.

Highlights

Metronidazole is a nitroimidazole antimicrobial which is effective against a variety of anaerobic bacteria.[1,2] It is actively used as an adjunct in the treatment of H.pylori infection, responsible for developing gastric ulcers.[3]Treatment of upper gastro-intestinal tract (GIT) infection is challenging due to the location of the infection site in stomach mucus lining.[4]
In case of formulations containing guar gum, guar gum was added to the Eudragit-Carbopol mixture
The underlying mechanism involves crosslinking of the carboxylate groups of the alginate molecules by divalent calcium ions.[18]

Summary

Introduction

Metronidazole is a nitroimidazole antimicrobial which is effective against a variety of anaerobic bacteria.[1,2] It is actively used as an adjunct in the treatment of H.pylori infection, responsible for developing gastric ulcers.[3]. Treatment of upper gastro-intestinal tract (GIT) infection is challenging due to the location of the infection site in stomach mucus lining.[4] Treatment of local gastric infection with conventional formulations becomes ineffective due to their short gastric residence time and non-targeted drug release. Gastric emptying, which is highly variable, transfer the conventional formulation quickly to the intestine without significant release of drug to the mucous site. Frequent dosing is required.[5,6]

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