Mucoadhesive Microspheres Containing Amoxicillin for Clearance of
            <i>Helicobacter pylori</i>

Nagahara, Naoki; Akiyama, Yohko; Nakao, Megumi; Tada, Mitsuru; Kitano, Megumi; Ogawa, Yasuyuki

doi:10.1128/aac.42.10.2492

Cited by 88 publications

(26 citation statements)

References 19 publications

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“…The synthetic polymer, poly(acrylic acid) (Ranga and Buri, 1989;Nagahara et al, 1998), can adhere to the mucous layer, as does chitosan, a biodegradable natural polymer (He et al, 1998). Therefore, we studied the controlled release of amoxicillin from composite particles of alginate and gelatin as the drug-loaded core beads, with chitosan as the coating material to improve the mucoadhesive properties and increase encapsulation efficiency.…”

Section: Introductionmentioning

confidence: 99%

Mucoadhesive and floating chitosan-coated alginate beads for the controlled gastric release of amoxicillin

2010

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This work focused on the development of mucoadhesive and floating chitosan-coated alginate beads as a gastroretensive delivery vehicle for amoxicillin, towards the effective eradication of Helicobacter pylori, a major causative agent of peptic ulcers. Alginate was used as the core bead core polymer and chitosan as the mucoadhesive polymer coating. Amoxicillin-loaded alginate beads coated with 0.5% (w/v) chitosan (ALG/0.5%CHI) exhibited excellent floating ability, high encapsulation efficiency, high drug loading capacity, and a strong in vitro mucoadhesion to the gastric mucosal layer. In vitro, amoxicillin was released faster in simulated gastric fluid (pH 1.2, HCl) than in simulated intestinal fluid (phosphate buffer, pH 7.4). ALG/0.5%CHI could be prepared with a > 90% drug encapsulation efficiency and exhibited more than 90% muco-adhesiveness, 100% floating ability, and achieved sustained release of amoxicillin for over six hours in SGF.

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Section: Introductionmentioning

confidence: 99%

Mucoadhesive and floating chitosan-coated alginate beads for the controlled gastric release of amoxicillin

2010

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“…[13] Mucoadhesive drug carriers may prolong the residence time in the GI tract because they can adhere to the mucus surface, resulting in an effective localized drug concentration. [14] Among the mucoadhesive drug carriers mucoadhesive microspheres have some advantages, e.g. a much more intimate contact with the mucus layer, lightweight and a smaller dose variation due to the large number of microspheres administered.…”

Section: Introductionmentioning

confidence: 99%

Design and evaluation of controlled release mucoadhesive microspheres of amoxicillin for anti Helicobacter pylori therapy

Venkateswaramurthy¹,

Perumal²,

Sambathkumar³

2011

Asian J Pharm

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T he aim of this study was to develop controlled release mucoadhesive microspheres of amoxicillin trihydrate for the treatment of peptic ulcer disease caused by Helicobacter pylori (H. pylori). Microspheres were prepared by solvent evaporation technique using carbopol 974P, hydroxypropyl methyl cellulose K4M (HPMC K4M) and Eudragit RS 100. The prepared microspheres were subjected to evaluation for particle size, incorporation efficiency, in vitro mucoadhesion and in vitro drug release characteristics. Absence of drug-polymer interaction was confirmed using differential scanning calorimetry analysis and fourier transform infrared spectrophotometry. The prepared microspheres showed a strong mucoadhesive property. The polymer concentration influenced the in vitro drug release significantly in 0.1N HCl. The particle sizes of systems ranged between 123±8.35 μm and 524±11.54 μm. Percent drug entrapment and release profiles of amoxicillin trihydrate in 0.1 N HCl were determined using high-performance liquid chromatography. The percentage drug entrapment and percentage yield of formulations were about 56.71±1.66% to 88.32±0.65% and 39.20±1.62% to 92.40±1.32%, respectively. The stability of the drugs was assessed in 0.1 N HCl. The results further substantiated that mucoadhesive microspheres improved the gastric stability of amoxicillin trihydrate (due to entrapment within the microsphere). From the above results, it was concluded that the mucoadhesive microspheres of amoxicillin trihydrate has feasibility for eradicating H. pylori from the stomach more effectively because of the prolonged gastrointestinal residence time and controlled release of drug from the formulation.How to cite this article: Venkateswaramurthy N, Sambathkumar R, Perumal P. Design and evaluation of controlled release mucoadhesive microspheres of amoxicillin for anti Helicobacter pylori therapy. Asian J Pharm 2011;5:238-45.

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“…According to our results, unconjugated dihydroxy bile acids might be candidate drugs for H. pylori eradication, but there are no reports demonstrating the clinical efficacy of bile acids for H. pylori eradication. 15,16 Therefore, further investigations should be undertaken on the transfer of bile acids across the gastric mucosal barrier, how to maintain intragastric bile acid concentrations above the MIC after the administration of bile acid, 17 and the efficacy of combined therapy with bile acids and other drugs.…”

Section: Discussionmentioning

confidence: 99%

Antibacterial action of bile acids against Helicobacter pylori and changes in its ultrastructural morphology: effect of unconjugated dihydroxy bile acid

Itoh

Wada

Tan

et al. 1999

Journal of Gastroenterology

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Although it has been shown that bile acids possess antibacterial activity against Helicobacter pylori, few reports on their activity have been published. We determined the minimum inhibitory concentration at 72 h of various unconjugated and conjugated bile acids against laboratory standard strains and clinical isolates of H. pylori, and studied morphologic changes of H. pylori under the scanning electron microscope during treatment with deoxycholic acid and ursodeoxycholic acid at the minimum inhibitory concentrations for 24 h. We found that only the unconjugated form of dihydroxy bile acid has antibacterial activity. The minimum inhibitory concentration of deoxycholic acid is 200-400 microg/ml, that of chenodeoxycholic acid is similar to that of deoxycholic acid, and that of ursodeoxycholic acid is 400-800 microg/ml. The morphology of H. pylori changed from its primary rodlike shape to a spherical shape with blebs on the cell surface, and was further degraded to an irregularly condensed mass, following an increase in bile acid. This morphologic change in H. pylori was different from the change to a spherical shape caused by amoxicillin. On the basis of these results, it seems that unconjugated dihydroxy bile acid might be a candidate drug for eradication of H. pylori, but further investigations of the clinical usefulness of bile acid for this purpose should be done.

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Mucoadhesive Microspheres Containing Amoxicillin for Clearance of Helicobacter pylori

Cited by 88 publications

References 19 publications

Mucoadhesive and floating chitosan-coated alginate beads for the controlled gastric release of amoxicillin

Mucoadhesive and floating chitosan-coated alginate beads for the controlled gastric release of amoxicillin

Design and evaluation of controlled release mucoadhesive microspheres of amoxicillin for anti Helicobacter pylori therapy

Antibacterial action of bile acids against Helicobacter pylori and changes in its ultrastructural morphology: effect of unconjugated dihydroxy bile acid

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