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Int J Biol Macromol. 2016 Aug;89:622-31. doi: 10.1016/j.ijbiomac.2016.05.027. Epub 2016 May 10.

Floating mucoadhesive alginate beads of amoxicillin trihydrate: A facile approach for H. pylori eradication.

Author information

1
Division of Microbiology, Department of Pharmaceutical Technology, Jadavpur University, Kolkata 700032, India.
2
Department of Pharmaceutics, Dr. B. C. Roy College of Pharmacy and Allied Health Sciences, Bidhan Nagar, Durgapur 713206, India.
3
Division of Bacteriology, National Institute of Cholera and Enteric Diseases, Beleghata, Kolkata 700010, India.
4
Division of Microbiology, Department of Pharmaceutical Technology, Jadavpur University, Kolkata 700032, India. Electronic address: asamanta61@yahoo.co.in.

Abstract

This study investigates the design of sunflower oil entrapped floating and mucoadhesive beads of amoxicillin trihydrate using sodium alginate and hydroxypropyl methylcellulose as matrix polymers and chitosan as coating polymer to localize the antibiotic at the stomach site against Helicobacter pylori. Beads prepared by ionotropic gellation technique were evaluated for different physicochemical, in-vitro and in-vivo properties. Beads of all batches were floated for >24h with a maximum lag time of 46.3±3.2s. Scanning electron microscopy revealed that the beads were spherical in shape with few oil filled channels distributed throughout the surfaces and small pocket structures inside the matrix confirming oil entrapment. Prepared beads showed good mucoadhesiveness of 75.7±3.0% to 85.0±5.5%. The drug release profile was best fitted to Higuchi model with non fickian driven mechanism. The optimized batch showed 100% Helicobacter pylori growth inhibition in 15h in in-vitro culture. Furthermore, X-ray study in rabbit stomach confirmed the gastric retention of optimized formulation. The results exhibited that formulated beads may be preferred to localize the antibiotic in the gastric region to allow more availability of antibiotic at gastric mucus layer acting on Helicobacter pylori, thereby improving the therapeutic efficacy.

KEYWORDS:

Amoxicillin trihydrate; Floating; Helicobacter pylori; Sunflower oil; X-ray study

PMID:
27177460
DOI:
10.1016/j.ijbiomac.2016.05.027
[Indexed for MEDLINE]

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