Formulation and in vitro evaluation of oil entrapped floating beads of azithromycin for the effective treatment of Helicobacter pylori

The objective of this investigation was to develop an intra gastric floating drug delivery system of azithromycin in order to localize the antibiotic at the site of infection to achieve bactericidal concentration against Helicobacter pylori. In the present investigation oil entrapped floating beads of azithromycin was formulated and effect of polymer and oil concentration on physico chemicaland in-vitro drug release properties are evaluated. The formulation was developed by emulsion gelation technique using two polymers: Sodium alginate and Hydroxy propyl methyl cellulose (HPMC) and Soybean oil. The developed beads were evaluated in term of diameter, surface morphology, floating lag time, encapsulation efficiency, and in-vitro drug release. It was found that formulation variables such as amount of polymer (% w/v), amount of soybean oil (% v/v), the ratio of drug to polymer (w/w), affected the bead size, floating and encapsulation efficiency of the beads. The scanning electron microscope photograph indicated that prepared beads were spherical in shape. All batches of beads floated for 24 hours with a very short lag time of 175–210 seconds. The drug release profile was best fitted with Higuchi and first order kinetic model and the release exponent (n) values were 0.71 to 0.813 indicating anomalous transport mechanism. FTIR study confirms that drug was compatible with the polymers. The results provides evidence that formulated beads may be preferred to localize the antibiotic in the gastric region to allow more of the antibiotic to penetrate through the gastric mucus layer to act on H. pylori and thereby improve the therapeutic efficacy.

Author(s): Sanjoy K Dey

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